Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Morphometric measurements were made on the vessels , and immunoreactivity to ET 1 and endothelin converting enzyme ( ECE 1 ) studied . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We conclude that BEAS 2B and A 549 cells are able to process either endogenous or exogenous Big ET 1 by ECE 1 and that isoforms 1b and 1c could be involved in this processing with no significant role of NEP . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
To clarify the mechanisms of FK 506 induced hypertension , we studied the chronic effects of FK 506 on the synthesis of endothelin 1 ( ET 1 ) , the expression of mRNA of ET 1 and endothelin converting enzyme 1 ( ECE 1 ) , the endothelial nitric oxide synthase ( eNOS ) activity , and the expression of mRNA of eNOS and C type natriuretic peptide ( CNP ) in rat blood vessels . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Larger peptides such as neurotensin , substance P , bradykinin , and the oxidized insulin B chain were hydrolyzed by ECE 1 as efficiently as big endothelin 1 , a known in vivo substrate . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The cDNA sequence encoding endothelin converting enzyme 1 ( ECE 1 ) , which produces the active form of ET 1 from big ET 1 , was recently reported . ^^^ To elicit the role of ECE 1 in the glomerular and tubular dysfunction induced by CsA , the effects of CsA on mRNA and protein expression of ECE 1 in rat kidney and on mRNA expression of prepro ET 1 and ET A and B type receptors in glomeruli were studied . ^^^ It is suggested that downregulation of glomerular and tubular ECE 1 expression may be caused by increased ET 1 synthesis in CsA induced acute renal failure . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Therefore , ECE 1 may be involved in other systems , such as the regulation of hormone secretion , rather than exclusively generating ET 1 from its precursor . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The present study suggests that the increase in ET 1 peptide level in the heart of the rats with CHF originated from upregulation of preproET 1 mRNA , which was not attendant with the alteration of ECE 1 mRNA expression , and that both the ETA and ETB receptor systems are greatly accelerated in the failing heart . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
There was no significant difference in mRNA expression for ppET 1 , ECE 1 , and ETA receptors , whereas a significant reduction of ETB receptor mRNA was observed in DCM hearts . 125I labeled ET 1 radioligand binding studies demonstrated a significant downregulation of ETB receptors , whereas ETA receptor density was increased in membranes from DCM hearts . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The expression of endothelin 1 and endothelin converting enzyme 1 ( ECE 1 ) are independently regulated in bovine aortic endothelial cells . ^^^ The endopeptidase called endothelin converting enzyme 1 ( ECE 1 ) is thought to play a physiological role in endothelin 1 ( ET 1 ) biosynthesis . ^^^ To investigate whether the expression of mRNAs for preproET 1 and ECE 1 are regulated in parallel , a variety of conditions were used to compare levels of ET 1 synthesis by bovine aortic endothelial cells ( BAECs ) with levels of mRNA for preproET 1 , ECE 1a , ECE 1c , and the combined ECE 1 isoforms ( ECE 1a / b / c ) . ^^^ This indicates that under the conditions investigated , expression of ECE 1 is not coordinated with ET 1 synthesis in BAECs . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Northern blot analysis showed that ECE 1 ( and not ECE 2 ) is specifically expressed in Sertoli cells ; competitive enzyme immunoassay of ET production showed that Sertoli cell monolayers are capable of cleaving big ET 1 , an activity inhibited by the ECE inhibitor phosphoramidon . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Phosphoramidon , an endothelin converting enzyme ( ECE ) inhibitor , drastically decreased the amount of ET 1 accumulating in the culture medium in basal conditions or after UVB irradiation . ^^^ Taken together , the results showed that normal human keratinocytes secrete and partly degrade ET 1 through ECE and NEP pathways and pointed out a differential regulation of ET 1 by UVB and UVA 1 radiations without any noticeable role for PGE2 . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Peptide bioavailability and potency can be regulated through hypoxic up and down regulation of synthesis or release , activation by converting enzymes ( ACE for AII and ECE for ET 1 ) , inactivation by neutral endopeptidase and proteases , or by interaction with nitric oxide ( NO ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.60118939 |
Differences in affinity between big ET 1 and big ET 3 for ECE 1 thus appear to be due solely to sequence variations in the local region of the cleavage site . . 0.60118939^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Inhibition of ET 1 activation by the endothelin converting enzymes 1 ( a ) ( ) ( d ) ( ECE 1 ( a ) ( ) ( d ) ; EC 3 . 4 . 24 . 71 ) represents another approach to block the ET 1 effect in cancer . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Because these characteristics of ECE 2B are very similar to those of ET 1 converting enzyme ( ECE 1 ) in endothelial cells , these results raise the possibility that ECE 2B is identical to ECE 1 and that a single ECE physiologically converts all big ETs to the corresponding ETs in ET producing cells . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ECE 2 resembles ECE 1 in that it is inhibited in vitro by phosphoramidon and FR 901533 but not by thiorphan or captopril , and it converts big ET 1 more efficiently than big ET 2 or big ET 3 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In the present study , we have investigated the localization of endothelin 1 ( ET 1 ) and endothelin converting enzyme 1 ( ECE 1 ) messenger RNAs ( mRNAs ) and immunoreactivities in the human nasal mucosa by immunohistochemistry and in situ hybridization . ^^^ Immunostaining for ET 1 and ECE 1 was seen in the surface epithelium , endothelial cells , submucosal glands , and infrequently in vascular smooth muscle cells , in all subjects . ^^^ There was significantly more staining for ET 1 and ECE 1 in nasal glands and inflammatory cells in patients with chronic inflammation than in those with normal nasal mucosa . ^^^ In situ hybridization showed abundant expression of ET 1 and ECE 1 mRNAs over the surface epithelium , glands , vessels , and inflammatory cells . ^^^ Both immunohistochemistry and in situ hybridization demostrated the expression of ET 1 and ECE 1 immunoreactivities and mRNAs in similar sites , and also independently . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In this study , we examined the expression and localization of endothelin converting enzyme 1 ( ECE 1 ) , the final key enzyme of endothelin 1 processing , in rat carotid arteries after balloon injury and in human coronary atherosclerotic lesions . ^^^ Thus , ECE 1 may contribute to the process of injury induced neointimal formation and atherosclerosis through the autocrine / paracrine effects of endothelin 1 . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ECE 1 : a membrane bound metalloprotease that catalyzes the proteolytic activation of big endothelin 1 . ^^^ When transfected into cultured cells that normally secrete only big ET 1 , the ECE 1 cDNA conferred the ability to secrete mature ET 1 . ^^^ In transfected cells , ECE 1 processes endogenously synthesized big ET 1 as well as exogenously supplied big ET 1 , which interacts with ECE 1 on the cell surface . ^^^ ECE 1 may provide a target for pharmacological intervention to alter ET 1 production . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The increases in ECE 1 , ET 1 , and ET 3 and their receptor expression after balloon angioplasty suggest that these proteins play an active role in the pathogenesis of neointimal formation . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Temporal expression of ECE 1 , ET 1 , ET 3 , ETA , and ETB receptor mRNAs after balloon angioplasty in the rat . ^^^ The data suggest that ECE 1 , ET 1 , ET 3 , and ETA and ETB receptors play an active role in the pathogenesis of neointima formation . . ^^^ The temporal expressions of endothelin converting enzyme 1 ( ECE 1 ) , preproendothelin 1 ( preproET 1 ) , preproET 3 , and ETA , ETB receptor mRNAs were studied in rat carotid artery after balloon angioplasty using quantitative reverse transcription and the polymerase chain reaction ( RT PCR ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
These isoforms of ECE 1 show similar specificity converting big endothelin 1 ( ET 1 ) to ET 1 but big ET 2 and big ET 3 are converted much less efficiently . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Here , we investigate the expression of ECE 1 , big ET 1 , and ET 1 in the lungs of patients with idiopathic pulmonary fibrosis ( IPF ) and compare it to those of normal subjects using immunohistochemistry and in situ hybridization . ^^^ Serous bronchial glands also expressed ET 1 and ECE 1 . ^^^ ECE 1 immunostaining was colocalized to big ET 1 and ET 1 immunostaining , and correlated with disease activity ( P < 0 . 05 ) . ^^^ To study regulatory mechanisms of ET 1 and ECE 1 expression , human normal bronchial epithelial ( NBE ) cells were treated with cytokines and analyzed by radioimmunoassay and Northern blot . ^^^ These findings demonstrated the colocalization of the precursor and active ET 1 , and ECE 1 in the same cell , and that ECE 1 expression is elevated in IPF . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Although a high molecular mass form of endothelin 1 is produced by processing by ECE 1 without cleavage at Arg 52 , it did not evoke Ca2+ transient in endothelinA receptor expressing cells . ^^^ In conclusion , prior cleavage at Arg 92 by furin like convertase is absolutely necessary for cleavage by ECE 1 at Trp 73 to produce mature endothelin 1 . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In particular , ECE 1 , through the paracrine effects of ET 1 , may contribute to the proliferation of smooth muscle after angioplasty and to the development of human atherosclerosis . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
After 28 d , right upper lobes were fixed for immunohistochemistry ( IHC ) and sections were stained with antisera to ET 1 and ECE 1 and graded semiquantitatively . ^^^ By IHC , we found increased ET 1 immunoreactivity ( ir ) in airway epithelium and inflammatory cells , and ECE 1 ir in airway epithelium , type 2 pneumocytes and endothelial cells ( p < 0 . 05 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) is formed from its precursor preproET 1 via the cleavage of the intermediate bigET 1 by endothelin converting enzyme ( ECE 1 ) . ^^^ Endothelin 1 ( ET 1 ) is formed from its precursor preproET 1 via the cleavage of the intermediate bigET 1 by endothelin converting enzyme ( ECE 1 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The porcine tracheal SMCs and EpCs also expressed pre pro ET 1 ( ppET 1 ) , ppET 3 , and endothelin converting enzyme 1 ( ECE 1 ) mRNAs . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Because synthesis of bioactive endothelin 1 requires endothelin converting enzyme 1 ( ECE 1 ) , we investigated whether renal ECE 1 gene expression is altered in the kidney of SHR . ^^^ We conclude that high ECE 1 gene expression in the nephron , via increase of endothelin 1 synthesis , may promote sodium retention that contributes to the development and / or maintenance of hypertension in SHR . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) catalyzes the proteolytic activation of big endothelin 1 to endothelin 1 ( ET 1 ) in vitro . ^^^ ECE 1 / term embryos exhibited craniofacial and cardiac abnormalities virtually identical to the defects seen in ET 1 and endothelin A receptor ( ETA ) deficient embryos . ^^^ Surprisingly , large amounts of mature ET 1 peptide are found in ECE 1 / embryos , indicating that non ECE 1 protease ( s ) can activate ET 1 at certain sites . ^^^ These findings reveal that ECE 1 is a bona fide activating protease for both big ET 1 and big ET 3 in vivo , and that the cell cell communication pathways represented by the ET 1 / ECE 1 / ETA axis and the ET 3 / ECE 1 / ETB axis are each involved in the development of distinct subsets of neural crest cell lineages . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Phe 21 ] big endothelin 1 ( 18 34 ) and [ Ala 31 ] big endothelin 1 ( 18 34 ) inhibit the human endothelin converting enzyme 1 ( ECE 1 ) expressed in CHO K 1 cells in a different fashion . ^^^ Endothelin converting enzyme 1 ( ECE 1 ) is one of the most important enzymes to convert big endothelin 1 ( big ET 1 ) to ET 1 . ^^^ To identify the inhibitors of ECE 1 , we examined the effects of variously substituted analogues of big ET 1 on ECE 1 activity using solubilized membranes prepared from human ECE 1 expressed CHO K 1 cells . ^^^ Among the big ET 1 analogues tested , [ Phe 21 ] big ET 1 ( 18 34 ) and [ Ala 31 ] big ET 1 ( 18 34 ) exhibited a significant inhibition of ECE 1 . ^^^ These results not only support the concept that ECE 1 recognizes big ET 1 both at the P 1 position and at the C terminal region but also revealed that these two regions are recognized by this enzyme in a different manner . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) mRNA was detected in PE cells and not in PS cells ; however , big ET 1 was the predominant immunoreactive ET 1 secretory product of PE cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET 1 , endothelin converting enzyme 1 ( ECE 1 ) , and iNOS staining was widespread and intense in alveolar and pulmonary arterial endothelium . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Although without cleavage at Arg 52 a high molecular weight form of ET 1 , designated Large ET 1 , is produced by processing by ECE 1 , it did not evoke a Ca2+ transient in ETA receptor expressing cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
BACKGROUND : The lung expresses large amounts of endothelin converting enzyme 1 ( ECE 1 ) , which catalyzes a step in the biosynthesis of potent vasoactive endothelin 1 ( ET 1 ) from the inactive intermediate big ET 1 . ^^^ Because there has been no report concerning a possible relationship between ET 1 and ECE 1 , we investigated the effects of ET 1 on ECE 1 expression in cultured rat pulmonary endothelial cells . ^^^ Incubation with ET 1 for 6 hours caused a significant decrease in ECE 1 mRNA expression . ^^^ The action of ET 1 on ECE 1 mRNA expression was antagonized by pretreatment with BQ 788 , a specific ETB receptor antagonist , but not by pretreatment with BQ 123 , a specific ETA receptor antagonist . ^^^ The expression of ECE 1 protein was also inhibited at 6 hours after incubation with ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) is produced from inactive precursor big ET 1 by endothelin converting enzyme 1 ( ECE 1 ) , a membrane bound metalloprotease , structurally similar to another metalloprotease , neutral endopeptidase 24 . 11 ( NEP ) . ^^^ Endothelin 1 ( ET 1 ) is produced from inactive precursor big ET 1 by endothelin converting enzyme 1 ( ECE 1 ) , a membrane bound metalloprotease , structurally similar to another metalloprotease , neutral endopeptidase 24 . 11 ( NEP ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Data are also presented to show that this series of inhibitors are effective in inhibiting ECE 1 in intact cells and in attenuating the increase in perfusion pressure induced by big ET 1 in isolated rat mesentery . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
To more fully comprehend the pathogenesis of chronic rejection , we investigated the expression of endothelin 1 ( ET 1 ) and endothelin converting enzyme 1 ( ECE 1 ) in inadequately immuno suppressed rat lung allografts ( n = 15 ) at monthly intervals after transplantation and compared these findings with those in normal rat lung ( n = 5 ) , using immunohistochemistry . ^^^ These findings suggest a causal role for ET 1 and ECE 1 in the inflammatory and proliferative damage associated with chronic rejection after lung transplantation . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Hemodynamic forces have been shown to modulate the expression of endothelin ( ET 1 ) and endothelin converting enzyme ( ECE 1 ) in endothelial cells . ^^^ A range of flow induced pressure ( 80 160 mm Hg ) was not able to further augment ET 1 or ECE 1 gene expression . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Big endothelin 1 ( big ET 1 ) is converted into an active form , ET 1 , by endothelin converting enzyme 1 ( ECE 1 ) . ^^^ To assess the mechanism of substrate recognition by ECE 1 , we examined the effects of variously substituted analogues of big ET 1 on ECE 1 activity , using solubilized membranes prepared from human ECE 1 expressed CHO K 1 cells . ^^^ Among the big ET 1 analogues tested , [ 21Phe ] big ET 1 [ 18 34 ] and [ 31Ala ] big ET 1 [ 18 34 ] exhibited significant inhibition of ECE 1 . ^^^ These results suggested that ECE 1 recognizes big ET 1 at the P 1 position and the C terminal region in a different manner and that modification of these regions can produce ECE 1 inhibitors . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The cDNA was used as a template in a multiplex PCR reaction containing primers specific for ET 1 , ET 2 , and ET 3 , ET converting enzyme 1 ( ECE 1 ) and ECE 2 , and ETA and ETB receptors . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Northern blot analysis of preproendothelin 1 ( preproET 1 ) and endothelin converting enzyme 1 ( ECE 1 ) expression revealed a significant ( p < 0 . 05 ) 20 % decrease in preproET 1 mRNA in the mRen 2 rats in the RV and in the LV , compared to SD rats . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In this study we determined sites of ET 1 synthesis and production in the failing human myocardium by immunohistochemistry and in situ hybridization for ET 1 and endothelin converting enzyme 1 ( ECE 1 ) . ^^^ In both failing and nonfailing hearts , apparent immunoreactivity for ET 1 and ECE 1 was consistently seen in cardiac myocytes . ^^^ Endothelial cells of intramyocardial coronary arteries and veins had only weak or focal ET 1 and apparent ECE 1 immunoreactivities . ^^^ On the other hand , in situ hybridization showed strong signals for ET 1 and ECE 1 mRNAs in vascular endothelial cells but a lesser intensity of signals in cardiac myocytes . ^^^ Apparent immunoreactivity and strong hybridization signals for both ET 1 and ECE 1 were seen in macrophages , which were abundant in infarcted regions of ischemic cardiomyopathy and in myocardium of septic patients but were rare in healthy hearts . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzymes ( ECEs ) , the enzymes that convert big endothelin 1 ( ET 1 ) to ET 1 , have recently been isolated and the corresponding proteins have been termed ECE 1 and ECE 2 . ^^^ In this study , to elucidate the role of ECE 1 under shear stress we examined the effect of physiologic shear stress on the mRNA expression of ECE 1 and ET 1 in cultured bovine carotid artery endothelial cells ( BAECs ) and human umbilical veins ( HUVECs ) , and also ECE 1 alpha mRNA expression in HUVECs . ^^^ ET 1 mRNA expression showed a concordant decrease with ECE 1 mRNA expression . ^^^ These results suggest that shear stress induced gene regulation of ET 1 and ECE 1 mRNA expression can contribute to the decrease of ET 1 peptide level by shear stress . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) plays a substantial role in activation of the endothelin ( ET ) system by cleaving the precursor , big ET 1 , to the active peptide ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Confocal microscopy revealed intense immunofluorescence staining for big ET 1 and the 2 isoforms of ECE 1 ( ECE 1alpha and ECE 1beta ) in the perinuclear region and in Weibel Palade bodies of the human umbilical vein endothelial cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ECE 1 cleaves its biologically inactive native substrate , big endothelin 1 , to generate a powerful vasoactive 21 amino acid peptide , endothelin 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In this study , we examined the expression of endothelin converting enzyme 1 ( ECE 1 ) on human follicles and CL , which is a membrane bound endopeptidase and is known to convert big endothelin 1 to endothelin 1 . ^^^ The activity of ECE 1 was also detected on cultured luteinizing granulosa cells by measuring endothelin 1 production from its precursor . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) is a type 2 membrane protein that catalyzes the proteolytic activation of big endothelin 1 to endothelin 1 ( ET 1 ) . ^^^ The subcellular distribution of ECE 1 , and hence the exact site of physiological activation of big ET 1 , remains controversial . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
This study demonstrates that even though overexpression of ECE 1 in itself does not lead to systemic hypertension , the enzyme can be a crucial rate limiting factor in the production of mature ET 1 in vivo . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 converting enzyme ( ECE 1 ) cleaves the precursor , big endothelin 1 , to the active peptide endothelin 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) is proteolytically generated from its inactive precursor by endothelin converting enzyme 1 ( ECE 1 ) and acts on the endothelin A ( ETA ) receptor . ^^^ Endothelin 1 ( ET 1 ) is proteolytically generated from its inactive precursor by endothelin converting enzyme 1 ( ECE 1 ) and acts on the endothelin A ( ETA ) receptor . ^^^ Genetic disruption of this ET 1 / ECE 1 / ETA pathway results in defects in branchial arch derived craniofacial tissues , as well as defects in cardiac outflow and great vessel structures , which are derived from cephalic ( cardiac ) neural crest . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) is a membrane bound metalloprotease which specifically converts the inactive precursor big endothelin 1 ( big ET 1 ) to the vasoactive endothelin 1 ( ET 1 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We investigated the role of endothelin converting enzyme 1 ( ECE 1 ) , which mediates the conversion of big ET 1 to mature ET 1 , in the development of alpha 1 adrenergic stimulated hypertrophy in cultured neonatal rat cardiac myocytes . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In this study , we have examined the regulatory role of ECE 1 , a critical enzyme involved in ET 1 synthesis , in the two major cellular sources of hepatic ET 1 . ^^^ Thus , during hepatic wound healing , differential regulation of ECE 1 mRNA and protein appears to be critical in controlling ET 1 production . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Further characterization of the enzymatic activity of ECE 1 ( conversion of Big ET 1 to ET 1 ) using the plasma membrane fraction of HNPE cells was performed by a novel assay involving ( 125 ) 1 Big ET 1 ( substrate ; 80 fmoles mg ( 1 ) protein ) and polyclonal antibodies specific for Big ET 1 . ^^^ Mean ECE 1 activity ( expressed as fmoles ( 125 ) 1 ET 1 produced mg protein ( 1 ) time ( 1 ) ) increased linearly with time and was similar to that observed in rat lung tissue . ^^^ ECE 1 activity was enhanced with increasing concentrations of substrate ( ( 125 ) 1 Big ET 1 ; 30 200 fmoles mg protein ( 1 ) 180 min ( 1 ) ) as well as with increasing concentrations of protein ( 5 20 microgram proteins at the substrate concentration of 80 fmoles mg protein ( 1 ) 180 min ( 1 ) ) . ^^^ These results suggest that the ECE 1 localized in HNPE cells , is a neutral pH sensitive metalloprotease which is similar in its activity to that observed in lung tissue and is essential for the production of ET 1 in HNPE cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Expression levels of ET converting enzyme 1 ( ECE 1 ) and prepro ET 1 mRNA were significantly increased at 7 and 14 days after virus inoculation . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We thus studied ET 1 , ET ( A ) receptor , and endothelin converting enzyme ( ECE 1 ) mRNA regulation as well as the effects of ET 1 on coronary resistance , LV contractility and relaxation in hypertrophied rat hearts . ^^^ ET 1 mRNA levels reached a second peak at 84 days of pressure overload ( +60 % , P < 0 . 05 ) , at the later time point in conjunction with elevated ECE 1 mRNA levels ( +20 % , P < 0 . 05 ) . ^^^ Thus , the cardiac expression of ET 1 , ET ( A ) , and ECE 1 mRNAs displays a distinct pattern during early and advanced cardiac pressure overload . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ECE 1 generates endothelin 1 ( ET 1 ) , the most potent vasoconstrictor yet discovered , by specific proteolytic processing of a precursor peptide , big ET 1 . ^^^ Despite apparent structural similarities , ECE 1 cleaves big ET 1 exclusively between Trp ( 21 ) and Val ( 22 ) , in contrast to neprilysin , which cleaves big ET 1 at various sites . ^^^ This result indicates that secondary / tertiary structure of big ET 1 induced by disulfide bonds is essential for the specific cleavage of the Trp ( 21 ) Val ( 22 ) bond by ECE 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Potent and selective non peptidic inhibitors of human endothelin converting enzyme 1 ( ECE 1 ) have been designed as potential modulators of endothelin ( ET 1 ) production in vivo . ^^^ Although additional gains in intrinsic ECE 1 inhibitory potency could occasionally be achieved by addition of a P ( 1 ) side chain , these compounds ( e . g . 43a ) showed poor functional activity in vivo in the big ET 1 pressor test . ^^^ Functionally , 27and 29 were the two most efficacious compounds from this study , producing sustained inhibition of ECE 1 activity in rats , as measured by their ability to block the hypertensive effects induced by big ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
OBJECTIVE : The purpose of this study is to determine the effects of alpha chemokines ( IL 8 and melanoma growth stimulating activator ) , beta chemokines ( monocyte chemotactic protein 1 , macrophage inflammatory protein 1alpha [ MIP 1alpha ] , MIP 1beta , and RANTES ) , and proinflammatory cytokines ( IL 1beta , TNF alpha , and IFN gamma ) on the expression of both ET 1 and endothelin converting enzyme 1 ( ECE 1 ) by human umbilical vein endothelial cells . ^^^ RESULTS : Incubation with the alpha chemokines melanoma growth stimulating activity and IL 8 did not significantly increase ET 1 and ECE 1 messenger ( m ) RNA expression and had no effect on ET 1 release . ^^^ Monocyte chemotactic protein 1 exerted the most potent increase in ET 1 and ECE 1 mRNA and ET 1 release among all chemokines studied ( P < . 05 ) . ^^^ The cytomix resulted in a significant increase in ET 1 and ECE 1 mRNA expression ( P < . 05 ) . ^^^ CONCLUSION : These data demonstrate that , like cytokines , chemokines can induce endothelial ET 1 and ECE 1 in vitro and suggest a possible role for these inflammatory mediators in the induction of the ET system in inflammatory and vascular diseases . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) is a vasoactive peptide produced from a biologically inactive big ET 1 by the action of endothelin converting enzyme 1 ( ECE 1 ) . ^^^ Endothelin 1 ( ET 1 ) is a vasoactive peptide produced from a biologically inactive big ET 1 by the action of endothelin converting enzyme 1 ( ECE 1 ) . ^^^ The histologic pattern of inflammation reached a maximum on the 4th day following the lipopolysaccharide and was accompanied by a 4 . 1 fold enhancement in the expression of ECE 1 activity and a significant elevation in ET 1 ( 3 . 1 fold ) , TNF alpha ( 8 . 8 fold ) , and apoptosis ( 11 . 6 fold ) . ^^^ A 41 . 5 % decrease in the severity of mucosal inflammation by the 10th day following the lipopolysaccharide was reflected in a 62 . 3 % reduction in the mucosal expression of ECE 1 and a decline in TNF alpha , ET 1 , and apoptosis . ^^^ Thus , H . pylori infection causes up regulation of gastric mucosal ECE 1 expression , which leads to the enhancement of ET 1 production , induction of TNF alpha , and triggering the apoptotic events that exacerbate the inflammatory process . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
By immunohistochemical analysis and immunofluorescence , endothelin converting enzyme 1 ( ECE 1 ) , the enzyme that synthesizes ET 1 , is localized to five distinct cell populations in the human placenta : ( 1 ) the endothelial cells lining the maternal basal plate blood vessels , ( 2 ) the intermediate trophoblasts , ( 3 ) the endothelial cells lining the chorionic villous blood vessels , ( 4 ) the chorionic villous stromal cells and ( 5 ) the chorionic villous trophoblasts . ^^^ The localization of ECE 1 corresponds with the previously reported distribution of ET 1 in the human placenta and is in accordance with the function of this enzyme in regulating vascular tone through synthesis of ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Using reverse transcription / polymerase chain reaction ( RT PCR ) , enzyme linked immunosorbent assay , and immunocytochemistry , we screened a panel of lung cancer cell lines for ET 1 , its receptors , and endothelin converting enzyme 1 ( ECE 1 ) , which generates the active form of ET 1 . ^^^ The intracellular isoform of ECE 1 , important in processing ET 1 if an autocrine growth loop is to function , was downregulated in the lung cancer cell lines as compared with expression of the extracellular isoform . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We examined the ET 1 and endothelin converting enzyme 1 ( ECE 1 ) system in cells cultured from two adjacent layers , subendothelial ( L 1 ) and inner medial ( L 2 ) , of normal sheep main pulmonary artery and the response of this system to exogenous ET 1 and transforming growth factor beta 1 ( TGF beta 1 ) . ^^^ End points include assessment of preproET 1 ( ppET 1 ) and ECE 1 gene coexpression , measurement of intracellular and released ET 1 , and ECE 1 activity . ^^^ TGF beta 1 downregulated ET 1 stimulated ppET 1 and ECE 1 transcripts but only in L 2 cells . ^^^ RT PCR analysis revealed that ppET 1 and ECE 1 transcripts were greater in L 1 than in L 2 cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) is a 21 amino acid vasoactive peptide produced from a 39 amino acid biologically inactive peptide , big ET 1 , by the action of endothelin converting enzyme 1 ( ECE 1 ) . ^^^ Endothelin 1 ( ET 1 ) is a 21 amino acid vasoactive peptide produced from a 39 amino acid biologically inactive peptide , big ET 1 , by the action of endothelin converting enzyme 1 ( ECE 1 ) . ^^^ The extent of gastric mucosal damage reached a maximum 4 h following the drug , and was accompanied by a 3 . 9 fold enhancement in the expression of ECE 1 activity and a significant elevation in ET 1 ( 4 . 5 fold ) , TNF alpha ( 11 . 3 fold ) , and apoptosis ( 29 . 9 fold ) . ^^^ A 37 . 2 % decrease in the severity of lesion 16 h following the drug was associated with a 44 . 5 % reduction in the mucosal expression of ECE 1 activity and a decline in TNF alpha ( 64 % ) , ET 1 ( 65 . 2 % ) , and apoptosis ( 72 . 3 % ) . ^^^ The results demonstrate that gastric mucosal injury by indomethacin is associated with up regulation of ECE 1 expression , which leads to the enhancement of ET 1 production , induction of TNF alpha , and triggering apoptotic events that disrupt gastric mucosal homeostasis . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Among the factors affecting the efficiency of soft oral tissue healing is endothelin 1 ( ET 1 ) , a potent vasoactive peptide produced from a biologically inactive big ET 1 by the action of endothelin converting enzyme 1 ( ECE 1 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 and 2 ( ECE 1 and 2 ) are membrane bound metalloproteases that can cleave biologically the inactive endothelin 1 ( ET 1 ) precursor to form active ET 1 in vitro . ^^^ Levels of mature ET 1 and ET 2 in whole ECE 1 ( / ) ; ECE 2 ( / ) embryos at E12 . 5 do not differ appreciably from those of ECE 1 ( / ) embryos . ^^^ The significant residual ET 1 / ET 2 in the ECE 1 ( / ) ; ECE 2 ( / ) embryos indicates that proteases distinct from ECE 1 and ECE 2 can carry out ET 1 activation in vivo . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Renal endothelin converting enzyme ( ECE ) activity , ET 1 , and ECE 1 mRNA expressions were significantly increased in the renal medullary area of DOCA Salt rats . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
By in situ hybridization and immunohistochemistry , we found gene and protein expression of ET 1 and its converting enzyme ECE 1 in both fetal olfactory mucosa and FNC B 4 cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The present results indicate that ECE 1 converts the endothelin 1 ( ET 1 ) from precursor big ET 1 to mature ET 1 in the PVN / SON . ^^^ The big ET 1 existing in the posterior pituitary gland is thought to be escaped from the converting by ECE 1 in the hypothalamus . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
BACKGROUND : Endothelin converting enzyme 1 ( ECE 1 ) processes big endothelin 1 ( ET 1 ) to ET 1 , a peptide implicated in atheroma formation . ^^^ We sought to demonstrate the distribution of the 2 ECE 1 isoforms in experimental atherosclerosis , to determine the effects of chronic NEP 1 on plasma cGMP concentrations , vascular wall ECE 1 activity , and ET 1 concentration , and to correlate these actions with atheroma formation . ^^^ Our hypothesis was that chronic NEP 1 , in association with augmented cGMP , would inhibit ECE 1 conversion of big ET 1 to active ET 1 , thus reducing tissue ET 1 concentrations and associated atheroma formation . ^^^ Compared with control values , plasma cGMP concentrations were increased ( 2 . 8+ / 0 . 6 versus 8 . 4+ / 1 . 2 pmol / mL , P < 0 . 05 ) , ECE 1 activity was attenuated ( 68+ / 3 % versus 32+ / 8 % , P < 0 . 05 ) , aortic tissue ET 1 concentrations were reduced ( 4 . 6+ / 0 . 5 versus 3 . 2+ / 0 . 3 pg / mg protein , P < 0 . 05 ) , and atheroma formation was attenuated ( 62+ / 6 % versus 34+ / 5 % , P < 0 . 01 ) by NEP 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET ( A ) and ET ( B ) receptor mRNAs were mainly in the lamina propria , pericryptal myofibroblasts , microvessels , and mononuclear cells , with ET ( A ) mRNA more abundant than ET ( B ) mRNA . ( 125 ) 1 ET 1 binding showed ET ( B ) along the crypts and in nerve fibers descending from the ganglionic plexus that contained PPET 1 , ECE 1 , and ET ( B ) transcripts , whereas glia contained ET ( A ) receptors . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) is a type 2 membrane protein that is important for the proteolytic activation of big endothelin 1 to endothelin 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
BACKGROUND : Endothelin 1 , a key mediator of inflammatory processes , is produced from its biologically inactive precursor , big ET by the action of endothelin converting enzyme 1 ( ECE 1 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
A major in vivo function of ECE 1 is the proteolytic conversion of big endothelin 1 to endothelin 1 , one of the most potent vasconstricting peptides known . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET ( A ) receptors mediate vasoconstriction and cell proliferation , whereas ET ( B ) receptors are important for the clearance of ET 1 , endothelial cell survival , the release of nitric oxide and prostacyclin , and the inhibition of ECE 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ECE 1 hydrolyzes the small peptide hormones bradykinin and substance P with acidic pH optima of 5 . 6 5 . 8 , which sharply contrasts the neutral pH optimum with big ET 1 as substrate . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) is a type 2 membrane protein that cleaves big endothelin 1 ( big ET 1 ) to endothelin 1 ( ET 1 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
CGS 35066 also exhibited a potent and sustained ECE 1 inhibitory activity in vivo , blocking the pressor response to big ET 1 by 84 % . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The mRNA levels of ppET 1 and ECE 1 increased with persistent upregulation of mRNA levels of ETA and ETB receptors , and immunohistochemical staining for ET 1 was found at endothelial cells and myocytes . ^^^ Although preproET 1 ( ppET 1 ) and ET converting enzyme 1 ( ECE 1 ) mRNA levels were not increased , mRNA levels of ET type A ( ETA ) and ET type B ( ETB ) receptors were increased . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
To evaluate the potential role of the endothelin system in glioblastoma we first determined the cellular distribution of the mRNA and proteins of the components of the endothelin system , preproendothelin 1 ( PPET 1 ) , endothelin converting enzyme 1 ( ECE 1 ) , and ET ( A ) and ET ( B ) receptors in human glioblastoma tissue and glioblastoma cell lines . ^^^ PPET 1 , ECE 1 , and ET ( A ) receptor were highly expressed in glioblastoma vessels and in some scattered glioblastoma areas whereas ET ( B ) receptor was mainly found in cancer cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Interestingly , hepatocytes were found to contain preproET 1 mRNA , ECE 1 mRNA and ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The gene expression of ETA and ETB receptors ET 1 , ET 3 and ECE 1 was evaluated using relative multiplex reverse transcription / PCR . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In this study using phosphoramidon , a potent inhibitor of endothelin converting enzyme 1 ( ECE 1 ) , we investigated the influence of ET 1 on the expression of constitutive ( cNOS ) and inducible nitric oxide synthase ( NOS 2 ) during gastric mucosal injury caused by indomethacin . ^^^ RESULTS : In the absence of phosphoramidon , indomethacin caused extensive multiple hemorrhagic lesions of glandular mucosa , accompanied by a 29 . 9 fold increase in epithelial cell apoptosis , a 13 . 3 fold increase in NOS 2 and a 5 . 5 fold decline in the activity of cNOS , while the mucosal expression of ECE 1 activity increased 4 fold and the level of ET 1 showed a 4 . 8 fold increase . ^^^ Pretreatment with phosphoramidon produced dose dependent reduction in the extent of mucosal damage caused by indomethacin , accompanied by a significant recovery in the expression of cNOS , and a marked decline in ECE 1 , epithelial cell apoptosis and the mucosal level of ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
CONCLUSIONS : This study showed that the biosynthetic pathway of ET 1 is activated in LV myocardium in the failing heart , and the myocardial processing of big ET 1 is highly specific for ECE 1 . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Immunohistochemical staining was performed using the labeled streptavidin biotin method to detect the localization of big endothelin 1 ( BET 1 ) , ET 1 and endothelin converting enzyme 1 ( ECE 1 ) . ^^^ Immunoreactivity for BET 1 , ET 1 and ECE 1 was localized to the small vessels of the bony labyrinth adjacent to the spiral ligament . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
CONCLUSION : Both A 549 and HUVEC produce and release endothelin 1 through a specific enzymatic pathway , whether or not ECE 1 is the only enzyme involved remains to be determined . ^^^ Both HUVEC and A 549 cells express the mRNAs for ppET 1 , ET A , and ET B receptor subtypes and ECE 1 ( isoforms ECE 1b , c and / or d ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin ET ( A ) receptors mediate vasoconstriction and cell proliferation , whereas ET ( B ) receptors are involved in the clearance of ET 1 , inhibition of endothelial apoptosis , release of nitric oxide and prostacyclin , and inhibition of ECE 1 expression . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
METHODS AND RESULTS : To evaluate ECE 1 immunoreactivity concerning big ET 1 / ET 1 , we performed qualitative and quantitative immunohistochemistry in normal internal mammary arteries ( n=10 ) , in coronary arteries with adaptive intimal fibrosis ( n=10 ) , in aortic fatty streaks ( n=10 ) , and in distinct regions of advanced carotid plaques ( n=15 ) . ^^^ All ET 1 ( + ) cells were simultaneously ECE 1 ( + ) . ^^^ CONCLUSION : Together with ET 1 , ECE 1 is abundantly present in human arteries and at different stages of atherosclerotic plaque evolution . ^^^ The upregulation of the ECE 1 / ET 1 system is closely linked to the presence of chronic inflammation and is present in very early stages of plaque evolution . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
On the other hand , inhibition of ERK 1 and ERK 2 activation by PD 98059 ( 50 micromol / L ) prevented the upregulation of ECE 1 expression by thrombin as well as the increase in ECE activity and ET 1 accumulation in the medium . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We have examined the effects of treatment with PGF ( 2alpha ) during the early and midluteal phases on three components of the endothelin system : endothelin converting enzyme 1 ( ECE 1 ) , ET type A receptor ( ET ( A ) ) , and ET 1 in the bovine corpus luteum ( CL ) . ^^^ Semiquantitative reverse transcriptase polymerase chain reaction was used to evaluate the mRNA encoding ECE 1 , ET ( A ) , and ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The specific involvement of ET 1 in the angiogenic effect mediated by CHO ET 1 was demonstrated by the reduction or abolition of neovascularized CHO ET 1 nodules by ( 1 ) bosentan , a mixed antagonist of ET ( A ) / ET ( B ) receptors , ( 2 ) an ET ( A ) receptor antagonist ( Ru 69986 ) and ( 3 ) phosporamidon , an inhibitor of endothelin converting enzyme 1 ( ECE 1 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) is the key enzyme that synthesizes ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In cardiac biopsies of both ICM and DCM patients , ET 1 , VEGF C , CPT 1 , and CARAT mRNA were up regulated , whereas ECE 1 mRNA was down regulated ( P < 0 . 05 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We also examined the distribution of ET 1 and the regulation of endothelin converting enzyme 1 ( ECE 1 ) , the rate limiting enzyme in ET 1 production . ^^^ We performed immunohistochemistry for the assessment of tissue ET 1 and ECE 1 . ^^^ Distribution of ECE 1 followed that of ET 1 on immunohistochemistry . ^^^ In conclusion , the amount of ECE 1 mRNA and protein parallel those of ET 1 . ^^^ Endotoxemia is associated with a marked increase in plasma ET 1 and an increase in ppET 1 and ECE 1 mRNA in multiple tissues ; however , there was no significant change in tissue ET 1 except in the pulmonary artery . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The presence of the endothelin converting enzyme 1 ( ECE 1 ) and ET 1 suggests that there is a local ET system in the adrenal cortex , but the in situ synthesis of ET 1 remains to be confirmed . ^^^ Polymerase chain reaction studies gave strong signals for ECE 1 mRNA and the mRNAs for endothelin type A ( ET ( A ) ) and B ( ET ( B ) ) receptors and faint signals for prepro ET 1 mRNA . ^^^ ECE 1 mRNA and protein were ubiquitous and abundant in secretory cells ( score , +++ ) and vascular structures ( score , ++ ) ; the enzyme was active on big ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Analysis using in situ hybridization and enriched luteal cell subpopulations showed that both steroidogenic and endothelial cells of the CL expressed high levels of ECE 1 mRNA ; prepro ET 1 mRNA , on the other hand , was only expressed by resident endothelial cells . ^^^ In the mature CL , ECE 1 mRNA increase occurred both in steroidogenic and endothelial cells and was accompanied by a significant rise in ET 1 peptide . ^^^ However , in contrast to ECE 1 , prepro ET 1 mRNA levels were similar in early and midluteal phase CL . ^^^ Low ECE 1 levels during the early luteal phase , restricting the production of active ET 1 , may explain why the immature CL is able to withstand PGF ( 2 alpha ) induced luteolysis . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Vascular tissue ET 1 levels and ECE 1 activity were also augmented in African American patients . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The expression levels of ET 1 , ET 3 , ET receptor subtypes and endothelin converting enzyme 1 ( ECE 1 ) mRNAs were assessed by relative multiplex reverse transcription polymerase chain reaction ( RT PCR ) . ^^^ In addition , RT PCR data show an upregulation in the expression of ETB receptor subtype , ET 1 and ECE 1 mRNA in both regions , and a downregulation in the expression of ETA receptor subtype mRNA in the dorsolateral region of the castrated rat prostate . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) expression and endothelin 1 peptide level was upregulated in myocardium of heart failure patients without ACE inhibition . ^^^ ACE inhibitor therapy prevented upregulation of ECE 1 and endothelin 1 in failing myocardium . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Although ET 1 [ 1 21 ] is generated from bigET 1 by an ET converting enzyme ( ECE 1 ) , there is evidence of an alternative chymase mediated biosynthetic pathway leading to the production of an ET 1 [ 1 31 ] peptide , the role of which in adrenal pathophysiology is largely unknown . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
A remarkable increase in the number of Weibel Palade ( WP ) bodies , storage sites of ET 1 and ECE 1 , occurred in the hypoxic group when compared to the normoxic group . ^^^ Immunoreactivities for ET 1 and ECE 1 , and signals for preproET 1 mRNA were seen along the endothelia of both groups , but the intensities were significantly elevated in the hypoxic group . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
A major in vivo function of ECE 1 is the generation of endothelin 1 , a potent vasoconstrictor , from big endothelin 1 . ^^^ In this study we have used substrates based on the sequence of the COOH terminal half of big endothelin 1 to examine the subsite specificity of recombinant ECE 1 . ^^^ The big endothelin 1 [ 16 38 ] peptides were systematically varied at either position 21 ( P ( 1 ) ) or position 22 ( P ' ( 1 ) ) and used in steady state kinetic analyses of ECE 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) is a potent vasoconstrictor and smooth muscle comitogen that is produced by endothelin converting enzyme 1 ( ECE 1 ) in endothelium and smooth muscle of the vascular wall in adult pulmonary arteries . ^^^ Endothelin 1 ( ET 1 ) is a potent vasoconstrictor and smooth muscle comitogen that is produced by endothelin converting enzyme 1 ( ECE 1 ) in endothelium and smooth muscle of the vascular wall in adult pulmonary arteries . ^^^ We speculate that alterations in ECE 1 contribute to the changes in ET 1 levels during the perinatal period and that the majority of ET 1 produced in the fetal lamb pulmonary vasculature is produced by the vascular endothelium . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET 1 gene is transcribed as prepro ET 1 ( ppET 1 ) and the active form of peptide is derived from the inactive intermediate big ET 1 , by endothelin converting enzyme 1 ( ECE 1 ) , therefore alterations in mature ET 1 levels can be achieved by modulating the expression of ppET 1 and / or ECE 1 . ^^^ Collectively , these studies demonstrate that : ( a ) the various components of ET 1 system ( ET 1 / ECE 1 / ETA ) are dynamically and independently regulated during bovine luteal life span . ( b ) The CL becomes PGF2alpha responsive only when both ppET 1 and ECE 1 genes are expressed at a level which enable an uninterrupted ET 1 biosynthesis . . ^^^ ET 1 gene is transcribed as prepro ET 1 ( ppET 1 ) and the active form of peptide is derived from the inactive intermediate big ET 1 , by endothelin converting enzyme 1 ( ECE 1 ) , therefore alterations in mature ET 1 levels can be achieved by modulating the expression of ppET 1 and / or ECE 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET 1 induced vaso constriction , however , can be treated effectively at the level of endothelin 1 converting enzyme ( ECE 1 ) by ECE 1 inhibitors because ECE 1 converts biologically almost inactive big endothelin to endothelin 1 ( ET 1 ) , the most potent vasoconstrictor known . ^^^ ET 1 induced vaso constriction , however , can be treated effectively at the level of endothelin 1 converting enzyme ( ECE 1 ) by ECE 1 inhibitors because ECE 1 converts biologically almost inactive big endothelin to endothelin 1 ( ET 1 ) , the most potent vasoconstrictor known . ^^^ Therefore , it should be possible to treat ET 1 induced vaso constriction in the eye using ECE 1 inhibitors , especially in diseases like hypertensive vasculopathy , vasospasm , vaso occlusions or low tension glaucoma . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
A remarkable increase in the number of Weibel Palade ( WP ) bodies , enhanced immunoreactivities for ET 1 and ECE 1 along the endothelium , and elevated concentrations of ET 1 in the blood plasma as well as in homogenized thoracic aortae were observed in the cadmium treated groups . ^^^ By immunoelectron microscopy , immunoreactivities for ET 1 and ECE 1 were much more pronounced in the increased WP bodies . ^^^ Since WP bodies are involved in the extracellular release of ET 1 in the manner of a regulated pathway , these findings indicate that cadmium administration induces the enhanced release of ET 1 , which is actively processed by ECE 1 in the WP bodies . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
PgPepO possesses similar substrate specificity to ECE 1 and has been shown to cleave big endothelin 1 ( big ET 1 ) , big ET 2 and big ET 3 , converting the substrates into their respective mature endothelin peptides . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The effects on ECE 1 and NEP were assessed by determining the inhibition of big endothelin 1 ( big ET 1 ) induced increases in mean arterial pressure ( MAP ) and increases in plasma atrial natriuretic peptide ( ANP ) concentrations respectively , in conscious rats . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Our results support an upregulation of ET 1 synthesis by induction of ECE 1 in failing atrial myocardium . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) is a key enzyme in the biosynthesis of endothelin 1 ( ET 1 ) , a potent regulator of ovarian function . ^^^ Thus , the spatial and temporal pattern of ECE 1 expression determines the site of big ET 1 activation and the bioavailability of ET 1 . ^^^ Using enriched follicular and luteal cell subpopulations and in situ hybridization techniques , we showed that the ECE 1 gene is expressed by both endothelial and steroidogenic cells ; however , the intracellular ECE 1a isoform was present only in ET 1 expressing endothelial cells . ^^^ In contrast , ET 1 and LH downregulated ECE 1 in steroidogenic cells . ^^^ The hormonal regulation and intracellular localization of bovine ECE 1 isoforms revealed in this study may provide new insights into ET 1 biosynthesis and mode of action in different cellular microenvironments within the ovary . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) , the protease involved in the final step of post translational processing of ET 1 , cleaves the inactive precursor big ET 1 at the Trp ( 21 ) Val ( 22 ) peptide bond . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Immunohistochemical studies indicated that , beside endothelial cells ( EC ) , SMC of the human adult and fetal penis also express ET 1 and its converting enzyme , ECE 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
While neutral endopeptidase ( NEP ) and matrix metalloproteinase 2 ( MMP 2 ) are able to process big ET 1 , inhibitors of NEP ( thiorphan ) and MMP ( batimistat ) did not affect ECE 1 activity . ^^^ In conclusion , the enzymatic pathway essential for generating vascular ET 1 is activated in the vasculature of both AA and CA diabetic patients and this activation is highly specific for ECE 1 . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
METHODS : To measure plasma ET 1 ( 51 patients ) , big ET 1 immunoreactivity ( 22 patients ) , and serum ECE 1 activity ( 13 patients ) , blood samples were obtained on admission , in the morning after aneurysm surgery , and during the 2nd week after hemorrhage in 51 consecutive patients ( 28 men and 23 women , with a mean age of 50 . 8 years ) with aneurysmal SAH . ^^^ Plasma concentrations of ET 1 and big ET 1 as well as the ET 1 / big ET 1 ratio did not change significantly with elapsed time following SAH ; however , serum ECE 1 activity during the 2nd week after SAH was higher in patients with SAH than that in controls ( 162 + / 43 compared with 121 + / 56 pg / ml , respectively ; p = 0 . 028 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Whereas a functional role of ET in the valve formation can be proposed because of the simultaneous presence of all the components of the endothelin system ( ET 1 / ECE 1 / ET ( A ) ) , this seems not to be the case for the formation of the ventricular septum where endocardial cells do not express ET 1 , and only a weak ET ( A ) hybridization signal was detected in the surrounding myocardium . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Immunoreactivity was observed for both ET 1 and ECE 1 in endothelial cells , smooth muscle cells , and macrophages within lesions . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In this study , to elucidate the role of shear stress in endothelin production by endothelial cells , we examined the effect of physiological shear stress on the mRNA expression of endothelin converting enzyme 1 ( ECE 1 ) as well as endothelin 1 ( ET 1 ) in cultured bovine carotid artery endothelial cells ( BAECs ) and human umbilical vein endothelial cells ( HUVECs ) , using a parallel plate type flow chamber . ^^^ ET 1 mRNA expression decreased together with ECE 1 mRNA expression . ^^^ Shear stress at 15 dyn / cm ( 2 ) for 30 min induced a significant increase in the intracellular peroxide concentration , and the down regulation of ECE 1 and ET 1 mRNA expression by shear stress was attenuated almost completely on treatment with N acetyl cysteine ( NAC ) , an antioxidant ( 20 mM ) . ^^^ Furthermore , when H ( 2 ) O ( 2 ) ( 0 . 5 to 2 mM ) was added to BAECs in static culture , the ECE 1 as well as ET 1 mRNA expression was attenuated in proportion to the concentration of H ( 2 ) O ( 2 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ACE mRNA expression ( RT PCR ) increased continuously and peaked at 12 , 24 hr ; ECE 1 ( endothelin converting enzyme ) peaked at 12 hr , and both peptides in tissue ( Ang 2 and ET 1 ) increased significantly and peaked at 24 hr . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Determined by real time RT PCR , ET 1 , ET 3 , ECE 1 and ET receptor subtype ( ET ( A ) and ET ( B ) ) mRNAs were shown to be higher in bladders of 3 week compared to 3 month or 22 month old rats . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Finally , ECE 1 mRNAs were generally observed in neuronal populations known to express the pre proendothelin 1 gene , confirming the function of the metallopeptidase in endothelin 1 generation . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
It is unclear whether myoFbs generate ET peptides and consequentially regulate pathophysiological functions de novo through expression of the ET 1 precursor ( prepro ET 1 ) , ET converting enzyme 1 ( ECE 1 ) , a metalloprotease that is required to convert Big ET 1 to ET 1 and ET receptors . ^^^ In cultured cells , we found : 1 ) expression of mRNA for ET precursor gene ( ppET 1 ) , ECE 1 , and ETA and ETB receptors by semiquantitative RT PCR ; 2 ) phosphoramidon sensitive ECE 1 activity , which converts Big ET 1 to biologically active peptide ET 1 ; 3 ) expression of ETA and ETB receptors ; 4 ) elaboration of Big ET 1 and ET 1 peptides in myoFb culture media ; and 5 ) upregulation of type 1 collagen gene expression and synthesis by ET , which was blocked by bosentan ( a nonselective ETA and ETB receptor blocker ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
This latter process has been linked to enhanced expression of endothelin converting enzyme 1 ( ECE 1 , the enzyme that converts precursor ET 1 to the mature peptide ) in activated stellate cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) is generated from big ET 1 by endothelin converting enzyme 1 ( ECE 1 ) . ^^^ Endothelin 1 ( ET 1 ) is generated from big ET 1 by endothelin converting enzyme 1 ( ECE 1 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Expression levels of ETA and ETB receptor subtypes , ET 1 , ET 3 and ECE 1 mRNAs were assessed by relative multiplex reverse transcription polymerase chain reaction ( RT PCR ) . ^^^ In addition , RT PCR showed an up regulation in the expression of ETA and ETB receptor subtypes , ET 1 and ECE 1 mRNAs in the seminal vesicle of the castrated rat . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
RESULTS : The expression of prepro ET 1 , ET converting enzyme 1 ( ECE 1 ) , and ET A receptor mRNAs , but not ET B receptor mRNA , in the glomeruli was increased in rats with nephrotic syndrome . ^^^ CONCLUSION : These data suggest that an activated ET 1 ET A receptor pathway in glomeruli and / or an increased ECE 1 mRNA expression in distal segments may participate in sodium and water retention , but not in the occurrence of nephrotic syndrome . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
OBJECTIVE : The biosynthesis of endothelin 1 ( ET 1 ) , the most potent vasoconstrictor with mitogenic properties , involves the processing of intermediate protein big ET 1 by a unique metalloprotease , endothelin converting enzyme 1 ( ECE 1 ) . ^^^ METHODS AND RESULTS : ECE 1 localization was studied using confocal microscopy , which provides evidence for the first time that both ET 1 and ECE 1a are also found in the nuclear compartment in transiently transfected cells as well as in native endothelial cells that endogenously possess the ET system . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We therefore applied real time PCR using SYBR Green 1 to quantify ET 1 , ET 3 , ET converting enzyme 1 ( ECE 1 ) , and ETA and ETB receptor subtype mRNA expression in the rat genitourinary tract . ^^^ DISCUSSION : We demonstrated that significant quantitative variations existed in the expression levels of ET 1 , ET 3 , ECE 1 , and ETA and ETB receptor subtype mRNAs within a tissue and between different regions of the genitourinary tract and that the predominant expression of ETs and their receptor mRNAs in all tissues studied were ET 1 and the ETA receptor subtype , respectively . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We , therefore , studied genes pertinent to early embryologic development of the ANS including mammalian achaete scute homolog 1 ( MASH 1 ) , bone morphogenic protein 2 ( BMP 2 ) , engrailed 1 ( EN 1 ) , TLX 3 , endothelin converting enzyme 1 ( ECE 1 ) , endothelin 1 ( EDN 1 ) , PHOX2a , and PHOX2b in 67 probands with CCHS , and gender and ethnicity matched controls . ^^^ No disease defining mutations were identified in MASH 1 , BMP 2 , EN 1 , TLX 3 , ECE 1 , EDN 1 , or PHOX2a . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Real time quantitative PCR was used for determinations of tissue prepro ET 1 ( ppET 1 ) , ET 1 converting enzyme ( ECE 1 ) , and ETA and ETB receptor mRNA . ^^^ These changes were tightly correlated to myocardial ppET 1 and renal ETA receptor mRNA and less so to myocardial ECE 1 mRNA , and they occurred before any increase in plasma and urinary ET 1 ( P < 0 . 05 from week 4 ) and clinical signs of heart failure . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Genotyping of the EDN 1 K198N polymorphism showed that this variant was not associated with BP values in either men or women , but interacted with the ECE 1 variant to influence systolic and mean BP levels in women . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET receptors were characterized and quantified at the protein level by radioligand receptor binding , and gene transcript levels of ET 1 , ET 3 , ET converting enzyme 1 ( ECE 1 ) , and ET ( A ) and ET ( B ) receptor subtypes were quantified by real time reverse transcription polymerase chain reaction ( RT PCR ) . ^^^ Furthermore , ET 1 , ET 3 , ECE 1 , and ET ( A ) and ET ( B ) receptor subtype mRNAs are expressed at higher levels in the 3 weeks old rats as compared with the other two age groups . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
To have a better insight into their synthesis and action , members of the ET system ( ET 1 , ET converting enzyme ( ECE 1 ) isoforms a d , ETA and ETB receptors ) along with NO synthase ( NOS ) isoforms endothelial ( e ) NOS and inducible ( 1 ) NOS were quantified in CL derived endothelial cells ( CLEC ) . ^^^ Freshly isolated EC from mid cycle CL exhibited high ET 1 receptor expression ( both ETA and ETB ) , low ET 1 synthesizing ability ( both prepro ( pp ) ET 1 and ECE 1 ) , but elevated iNOS the high throughput NOS isoform . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The mRNA and protein expressions of nitric oxide synthase ( NOS ) , endothelin converting enzyme 1 ( ECE 1 ) , and endothelin 1 ( ET 1 ) were also investigated . ^^^ The eNOS , ECE 1 , and ET 1 mRNA expressions were assayed by Northern blot . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
CONCLUSION : The findings suggest that upregulation of ECE 1 , leading to increased generation of ET 1 in the renal medulla , may be a compensatory mechanism promoting enhanced sodium excretion by the kidney in response to high salt intake . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET 1 , and particularly ECE 1 , might constitute a target in this regulation . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We therefore studied genes pertinent to early embryologic development of the ANS , including MASH 1 , BMP 2 , PHOX2a , PHOX2b , RET , ECE 1 , EDN 1 , TLX 3 , and EN 1 in 92 probands with SIDS and 92 gender and ethnicity matched control subjects . ^^^ Four protein changing common polymorphisms were identified in BMP 2 , RET , ECE 1 , and EDN 1 , but the allele frequency did not differ between SIDS cases and control subjects . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) activates ET 1 and may thus contribute to the regulation of vascular tone and cell growth during atherosclerosis . ^^^ We evaluated the presence of ECE 1 and big ET 1 / ET 1 and the activity of ECE 1 in different plaque types . ^^^ Together with ET 1 , ECE 1 is present in endothelial cells ( ECs ) , vascular smooth muscle cells ( VSMCs ) and Mphi ' s . ^^^ ECE 1 activity and ET 1 immunoreactivity ( IR ) both are upregulated during the progression of atherosclerosis from a non inflammatory to an inflammatory stage . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Fasting influences steroidogenesis , vascular endothelial growth factor ( VEGF ) levels and mRNAs expression for VEGF , VEGF receptor type 2 ( VEGFR 2 ) , endothelin 1 ( ET 1 ) , endothelin receptor type A ( ET A ) and endothelin converting enzyme 1 ( ECE 1 ) in newly formed pig corpora lutea . ^^^ This study was designed to verify whether fasting influences vascular endothelial growth factor ( VEGF ) production and VEGF , VEGF receptor 2 ( VEGFR 2 ) as well as endothelin ( ET ) system members ( endothelin converting enzyme 1 , ECE 1 ; ET 1 ; endothelin receptor type A , ET A ) mRNA expression in pig corpora lutea ; furthermore , we wanted to assess whether fasting affects steroidogenesis in luteal cells . ^^^ VEGF and steroid levels in luteal tissue were determined by ELISA and RIA , respectively ; VEGF , VEGFR 2 , ET 1 , ET A and ECE 1 mRNAs expression was measured by real time PCR . ^^^ VEGF , VEGFR 2 , ET 1 and ECE 1 ( but not ET A ) mRNA expression was significantly lower ( P < 0 . 05 ) in fasted versus normally fed animals . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) is a 21 amino acid peptide produced from a biologically inactive big ET 1 by the action of endothelin converting enzyme 1 ( ECE 1 ) that acts through G protein coupled ETA and ETB receptors . ^^^ Endothelin 1 ( ET 1 ) is a 21 amino acid peptide produced from a biologically inactive big ET 1 by the action of endothelin converting enzyme 1 ( ECE 1 ) that acts through G protein coupled ETA and ETB receptors . ^^^ Using mucous cells of sublingual salivary gland , we show that P . gingivalis lipopolysaccharide ( LPS ) inhibitory effect on salivary mucin synthesis is accompanied by a marked increase in ET 1 generation and the enhancement in ECE 1 activity . ^^^ Inhibition of ECE 1 with phosphoramidon led to the impedance of the LPS induced ET 1 generation as well as countered the detrimental effect of the LPS on mucin synthesis . ^^^ Our findings are the first to demonstrate that P . gingivalis LPS detrimental effect on salivary mucin synthesis is intimately linked to the events controlled by EGFR transactivation , triggered by upregulation in ECE 1 , enhancement in ET 1 production , and G protein coupled ETA receptor activation . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The ' endothelin axis ' consists of three 21 amino acid peptides ( ET 1 , ET 2 and ET 3 ) , two G protein coupled receptors ( ET RA and ET RB ) , and two activating peptidases or endothelin converting enzymes ( ECE 1 and ECE 2 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
To have a better insight on its synthesis and action , members of ET system ( ET 1 , ET converting enzyme ECE 1 and ET ( A ) and ET ( B ) receptors ) were quantified in LEC . ^^^ The characteristic phenotype of these cells , identified by high ET 1 receptor expression ( both ET ( A ) , ET ( B ) ) and low ET 1 and ECE 1 levels , was gradually lost during culture suggesting that luteal microenvironment sustains the selective phenotype of its resident endothelial cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET 1 , formed by proteolysis of the propeptide big ET 1 by endothelin converting enzyme 1 ( ECE 1 ) , mediates its cellular actions through ETA and ETB receptors . ^^^ Because only immunoreactive ET 1 has been observed within human astrocytic tumor cells , the authors investigated the localization of the entire ET 1 system ( ET 1 mRNA , ET 1 , ECE 1 , ETA and ETB receptors ) in surgical samples of human diffuse astrocytomas WHO Grade 2 ( n = 6 ) . ^^^ Polyclonal antibodies were used to localize ET 1 , ECE 1 , ETA and ETB receptors by immunocytochemistry . ^^^ Up to 75 % of tumor cells displayed intense ET 1 and ECE 1 immunolabeling distributed throughout their cytoplasm . ^^^ CONCLUSIONS : The presence of ET 1 mRNA , ECE 1 , and ET 1 within tumor astrocytes suggests local ET synthesis and processing . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The effect of native and oxidized low density lipoproteins ( nLDL , oxLDL ) on expression of ECE 1 , prepro endothelin 1 , and endothelin 1 peptide was studied in primary cultures of human endothelial cells . ^^^ Furthermore , ECE 1 protein expression , prepro endothelin 1 mRNA , and endothelin 1 peptide release were increased in response to nLDL or oxLDL . ^^^ Induction of ECE 1 by nLDL and of prepro endothelin 1 by oxLDL was reduced by protein kinase C inhibition . ^^^ Increased expression of ECE 1 mRNA by oxLDL and of prepro endothelin 1 by nLDL was blocked by an angiotensin 2 receptor type 1 antagonist . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We show that P . gingivalisLPS detrimental effect on salivary mucin synthesis , associated with up regulation ( 3 . 9 fold ) in ET 1 generation and the enhancement ( 3 . 2 fold ) in endothelin converting enzyme 1 ( ECE 1 ) activity , was subject to a dose dependent suppression by leptin . ^^^ However , while the blockade of ERK led also to amplification in the impedance by leptin of the LPS induced expression of ECE 1 and ET 1 , the effect was not observed in the presence of wortmannin . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The mRNA expressions for cycloxygenase 2 ( Cox 2 ) , prostaglandin F synthase ( PGFS ) , prostaglandin E synthase ( PGES ) , prepro ET 1 , endothelin converting enzyme 1 ( Ece 1 ) , angiotensin converting enzyme 1 ( Ace 1 ) , VEGF and its receptors were investigated using real time RT PCR . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Therapeutic administration of phosphoramidon , an inhibitor of ECE 1 activity , led to a 61 . 2 % decline in the mucosal ET 1 level and a 64 . 1 % reduction in leptin , while the severity of mucosal inflammatory involvement increased by 28 . 6 % . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
OBJECTIVE : Endothelin 1 ( ET 1 ) , a key mediator of inflammatory processes associated with bacterial infection , is a 21 amino acid peptide produced from a biologically inactive big ET 1 by the action of endothelin converting enzyme 1 ( ECE 1 ) that acts through G protein coupled ET ( A ) and ET ( B ) receptors . ^^^ RESULTS : The LPS inhibitory effect on gastric mucin synthesis was accompanied by a marked increase in ET 1 generation and enhancement in ECE 1 activity . ^^^ Inhibition of ECE 1 with phosphoramidon not only led to the impedance of LPS induced ET 1 generation , but also countered the detrimental effect of LPS on mucin synthesis . ^^^ CONCLUSIONS : Our findings are the first to show that the detrimental effect of H . pylori on gastric mucin synthesis is intimately linked to the events associated with ECE 1 up regulation , enhancement in ET 1 production , and G protein coupled ET ( A ) receptor activation that triggers the EGFR transactivation . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We observed the expression of ET 1 , ET ( A ) R , ET ( B ) R and all endothelin converting enzyme 1 ( ECE 1 ) isoforms in oral SCC cells , but only the expression of ET 1 , ET ( B ) R and ECE 1 was increased when compared to normal human epidermal keratinocytes . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Using groups of rats subjected to intragastric administration of indomethacin ( at 0 60 mg / kg ) , we show that gastric mucosal damage reached a maximum 4 h following the drug , and was accompanied by a marked elevation ( up to 3 . 5 fold ) in the mucosal leptin level , up to 4 fold enhancement in the expression of endothelin converting enzyme 1 ( ECE 1 ) activity and up to 4 . 5 fold increase in ET 1 generation . ^^^ Pretreatment with phosphoramidon , an inhibitor of ECE 1 activity , not only led to a decline in ECE 1 and ET 1 generation , but also produced a dose dependent reduction in the mucosal level of leptin and the extent of mucosal damage caused by indomethacin . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Expression of ET 1 , endothelin converting enzyme 1 ( ECE 1 ) and endothelin receptors ETA and ETB was examined in 201 non small cell lung carcinoma ( NSCLC ) and corresponding normal tissues using real time polymerase chain reaction ( RT PCR ) . ^^^ A higher number of cases with ET 1 , ECE 1 and ETA mRNA expression was observed in malignant lung tumours compared with normal lung tissues ( 45 . 7 % versus 33 % for ET 1 ( P < 0 . 0001 ) ; 38 . 3 % versus 16 . 5 % for ECE 1 ( P = 0 . 004 ) ; and 42 . 8 % versus 28 . 5 % for ETA ( P < 0 . 0001 ) ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
However , higher ECE 1 in A 549 cells after exposure to particles suggests an increased ability to process bigET 1 into the mature ET 1 peptide , while increased receptor expression implies higher responsiveness . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 ( ECE 1 ) is the main protease responsible for ET 1 generation by cleavage of its functionally inactive precursor . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET ( A ) receptors mediate vasoconstriction and cell proliferation , whereas ET ( B ) receptors are important for aldosterone secretion , endothelial cell ( EC ) migration , the release of nitric oxide ( NO ) and prostacyclin , the clearance of ET 1 , and the inhibition of ECE 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Gene expression of endothelin 1 , endothelin converting enzyme 1 , and endothelin receptors in human epididymis . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 , endothelin 1 , and endothelin 3 like immunoreactivity in the rat brain . ^^^ Neurons likely to use endothelin as a neurotransmitter / neurohormone were mapped in the rat brain using polyclonal antibodies directed against endothelin converting enzyme 1 , endothelin 1 , and endothelin 3 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme ( ECE 1 ) is a critical enzyme in the production of the potent vasoconstrictor peptide endothelin ( ET 1 ) . ^^^ It has previously been shown that the levels of both ET 1 and ECE 1 are raised in atherosclerosis , but the possible relevance of the isoforms of ECE 1 in these changes has not yet been investigated . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 increased prepro ET 1 and ECE 1 mRNA expression in hypertrophied neonatal cardiomyocytes , and this was reversed with EPA pretreatment . ^^^ Endothelin converting enzyme 1 ( ECE 1 ) was also increased in ET 1 administered cardiomyocytes by 42 % compared with the control group and was reversed in the EPA pretreated group . ^^^ Endothelin 1 increased prepro ET 1 and ECE 1 mRNA expression in hypertrophied neonatal cardiomyocytes , and this was reversed with EPA pretreatment . ^^^ Thus , EPA may play a crucial role in the regression of ET 1 induced cardiomyocyte hypertrophy , partly through the suppression of ET 1 and ECE 1 expression . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
This study investigated the effects of chronic allograft rejection on hepatic endothelin converting enzyme 1 ( ECE 1 ) gene expression and endothelin 1 ( ET 1 ) plasma clearance . ^^^ Using the Lewis F 344 minor histocompatibility mismatch model of heterotopic cardiac transplantation , hepatic ECE 1 gene expression was measured by real time polymerase chain reaction and host plasma clearance of ET 1 was measured 8 weeks after transplantation in the absence of immunosuppression . ^^^ In animals undergoing allograft rejection , hepatic ECE 1 gene expression increased 2 fold ( P < 0 . 05 ) , whereas no effect of rejection on ET 1 clearance from plasma was observed . ^^^ Because the liver represents both a key organ for cytokine production and for endothelin metabolism , increased hepatic ECE 1 mediated ET 1 synthesis may contribute to host responses and cytokine production during allograft rejection . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
CONCLUSIONS : Mice lacking telomerase activity show hypertension as a result of an increase in plasma ET 1 levels , which is a consequence of ECE 1 overexpression . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
There was overproduction of preproET 1 and endothelin converting enzyme 1 in carcinoma cells and stromal vessels , suggesting that they are a local source of ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
There was up regulation of preproendothelin 1 , preproET 3 , endothelin converting enzyme 1 , and ET ( A ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We compared the cortical and medullary renal expression of prepro endothelin 1 , endothelin converting enzyme 1 , and endothelin type A and type B receptors in patients who underwent nephrectomy after normal ( 108 mmol / d NaCl ; n=6 ) or low ( 20 mmol / d NaCl ; n=6 ) sodium diet and investigated whether sodium exerts a direct role on endothelin receptor binding in vitro . ^^^ With normal sodium diet prepro endothelin 1 mRNA was 3 fold higher in renal medulla than in cortex ( P < 0 . 01 ) , whereas endothelin converting enzyme 1 mRNA was equally distributed . ^^^ In the renal cortex , low sodium diet caused a 194 % increase in prepro endothelin 1 mRNA ( P < 0 . 05 ) , whereas endothelin converting enzyme 1 type B and type A receptors remained unchanged . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Plasma endothelin 1 and cGMP levels and lung NOS activity , cGMP , eNOS , preproendothelin 1 , endothelin converting enzyme 1 , endothelin A , and endothelin B receptor protein levels were similar in both groups . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme 1 [ the enzyme responsible for the production of active ET 1 from big ET 1 , mRNA ( 411 % , p < 0 . 05 ) ] and protein ( 170 % , p < 0 . 05 ) were increased in lung tissue prepared from shunt lambs , compared with age matched controls . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
To address this question , we examined ABP and ventilation in mutant mice deficient in ET 1 , ETA and ETB receptors and endothelin converting enzyme 1 , which were made by gene targeting . 2 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In vivo induction of cardiac Purkinje fiber differentiation by coexpression of preproendothelin 1 and endothelin converting enzyme 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
To determine the role of ET 1 in cardiovascular and respiratory derangement in a porcine model of endotoxemic shock we evaluated ET 1 plasma levels and ET 1 mRNA and protein levels in lung , liver , and heart as well as Endothelin Converting Enzyme 1 , ET ( A ) and ET ( B ) receptors mRNA in the same tissues . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
These effects were accompanied by the decreased circulation and intrarenal concentrations of endothelin 1 and transforming growth factor beta 1 ( TGF beta 1 ) , and down regulated overexpression of genes for ET 1 , endothelin converting enzyme 1 , TGF beta 1 , and the subunits of ATP sensitive potassium channels ( K ( ATP ) ) , Kir1 . 1 and Kir6 . 1 , in the kidney during hypertension . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Both pollutants individually increased preproET 1 , endothelin converting enzyme 1 , and endothelial nitric oxide synthase mRNA levels in the lungs shortly after exposure , consistent with the concomitant increase in plasma of the 21 amino acid ET 1 [ 1 21 ] peptide measured by HPLC fluorescence . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ECE activity was detected by a bioassay which depended upon the 10 , 000 fold difference in potency between bET 1 and ET 1 as stimulants of guanosine 3 ' : 5 ' cyclic monophosphate ( cyclic GMP ) accumulation in kidney epithelial ( PK 1 ) cells of the pig . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ECEs derived from these epithelial cells were very similar to the endothelial ECE in the following biochemical properties : 1 ) The optimum pH was 7 . 0 ; 2 ) the Km value for big ET 1 was approximately 30 microM ; 3 ) the enzyme was potently inhibited by EDTA , o phenanthroline and phosphoramidon ; and 4 ) the enzyme did not convert big ET 2 or big ET 3 . ^^^ These data suggest that phosphoramidon sensitive ECE is involved in the processing of big ET 1 to ET 1 in the renal tubule . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In addition , the ratio of ET 1 to ET 1 precursor ( big ET 1 ) was much higher in the t HUE 2 transformants than in normal endothelial cells , suggesting that t HUE 2 transformants ( for example t HUE 2 1 ) possess high levels of endothelin converting enzyme ( ECE ) . ^^^ The establishment of stable transformants producing high levels of ET 1 in serum free medium will be useful for the study of cell type specific translation and processing to mature ET 1 , and of the regulatory factors of ECE . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We further suggest that to induce the release of prostanoids in perfused lungs , human big ET needs to be converted to ET 1 by a phosphoramidon sensitive endothelin converting enzyme ( ECE ) . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In porcine aortic endothelial cells , the 21 amino acid peptide endothelin 1 ( ET 1 ) is formed from a 39 amino acid intermediate big endothelin ( big ET ) by a putative endothelin converting enzyme ( ECE ) that cleaves the 39 mer at the Trp 21 Val22 bond . ^^^ Because big ET has less than 1 % of the contractile activity of ET 1 , inhibition of ECE should effectively block the biological effects of big ET . ^^^ Big ET injected intravenously into anesthetized rats produces a sustained pressor response that presumably is due to conversion of big ET to ET 1 by ECE . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Further validation of the use of these assays has included the measurement of endothelin 1 ( ET 1 ) derived from big ET by in vitro enzymatic conversion by cathepsin E , which has demonstrated that cathepsin E possesses the appropriate specificity of cleavage to be considered the endothelin converting enzyme ( ECE ) . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
To determine whether cathepsin E is a physiologically relevant endothelin converting enzyme ( ECE ) , three novel and potent inhibitors of cathepsin E were administered to conscious rats prior to a pressor challenge with big ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The endothelin converting enzyme ( ECE ) activity present in endothelial cells and rat and human brains was characterized using a selective and rapid bioassay for endothelin 1 ( ET 1 ) or endothelin 3 ( ET 3 ) together with a sensitive enzyme linked immunosorbent assay . ^^^ In conclusion , our studies confirmed the presence of ECE activity within endothelial cells , and showed ECE to be localized in brain tissue in sites consistent with the selective distribution of the ET 1 synthetic pathway . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
This assay is based on measuring endothelin 1 generated from big endothelin 1 by endothelin converting enzyme ( ECE ) with radioimmunoassay using an endothelin C terminal specific antibody . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Cathepsin D , a candidate for endothelin converting enzyme ( ECE ) , was allowed to act on porcine big endothelin 1 ( big ET 1 , 1 39 ) . ^^^ Therefore , cathepsin D is by no means a specific ECE , although the proteinase does cleave the Trp 21 Val22 bond of big ET 1 ( 1 39 ) to produce mature ET 1 ( 1 21 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
These results demonstrate that endogenous production of endothelin 1 acts to sustain vascular tone in humans and indicate that ECE inhibitors and endothelium receptor antagonists may have therapeutic potential as vasodilators . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Present studies were performed to determine whether the cardiovascular effects of DCLHb are due to an increase in the conversion of proendothelin 1 ( 1 38 ) ( proET 1 ) to ET 1 by endothelin converting enzyme ( ECE ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
These findings suggest that a majority of the ECE activity in rat lung may be responsible for the intracellular conversion of big ET 1 during its transit through the secretory pathways . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) is produced from its precursor , big endothelin 1 ( BigET 1 ) , by a putative endothelin converting enzyme ( ECE ) , but it is not known whether the enzyme is present in the brain . ^^^ Endothelin 1 ( ET 1 ) is produced from its precursor , big endothelin 1 ( BigET 1 ) , by a putative endothelin converting enzyme ( ECE ) , but it is not known whether the enzyme is present in the brain . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Based on our previous findings that phosphoramidon sensitive endothelin ( ET ) converting enzyme ( ECE ) converts human big ET 1 but does not big ET 3 , we investigated structural requirement for substrate peptide . ^^^ These results suggest that the carboxyl terminal sequence at residues 32 37 of big ET 1 is important for conversion , whereas the amino terminal disulfide loop structure appears to interfere with access of ECE to big ET 1 . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In porcine aortic endothelial cells , the 21 amino acid peptide endothelin 1 ( ET 1 ) is formed from a 39 amino acid intermediate called `` big endothelin 1 ' ' ( big ET 1 ) by a putative ET converting enzyme ( ECE ) that cleaves the 39 mer at the bond between Trp 21 and Val 22 . ^^^ Since big ET 1 has only 1 / 100 1 / 150th the contractile activity of ET 1 , inhibition of ECE should effectively block the biological effects of ET 1 . ^^^ Big ET 1 injected intravenously into anesthetized rats produces a sustained pressor response that presumably is due to conversion of big ET 1 into ET 1 by ECE . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Our results , presented in the above mentioned models , illustrate the capacity of the phosphoramidon sensitive endothelin converting enzyme ( ECE ) to discriminate between human big ET 1 and big ET 3 . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Furthermore , big ET 1 ( 100 pmol ) caused toxic effects and delayed cardiovascular changes which were prevented by the prior i . t . administration of either BQ 123 ( 65 nmol ) or 100 nmol phosphoramidon , an endothelin converting enzyme ( ECE ) inhibitor . ^^^ These results suggest : ( 1 ) that the cardiovascular and toxic effects of i . t . endothelins are mediated by ETA receptors in the rat spinal cord ; ( 2 ) that the pressor response and bradycardia are likely due to the activation of the sympatho adrenal nervous system and to a vagal reflex mechanism , respectively ; and ( 3 ) that a phosphoramidon sensitive ECE converts big ET 1 to ET 1 in the rat spinal cord . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We have also used different protease inhibitors and / or epithelial cell removal to investigate the nature and the location of the endothelin converting enzyme ( ECE ) activity responsible for the conversion of porcine big ET 1 ( 1 39 ) in this isolated preparation . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Production of ET 1 then proceeds by cleavage of bigET 1 by the endothelin converting enzyme ( ECE ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Our results suggest the presence of a phosphoramidon sensitive endothelin converting enzyme ( ECE ) which is responsible for the conversion of big endothelin 1 and big endothelin 2 to their active moieties , endothelin 1 and 2 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
A number of studies have reported that the final processing step in ET 1 biosynthesis by the hypothetical endothelin converting enzyme ( ECE ) is inhibited by phosphoramidon ( PHOS ) . ^^^ The ECE activity associated with the peak of ET IR ( 2 . 67 pmol ET 1 / h / 10 ( 6 ) cells ) was insensitive to 100 microM PHOS . ^^^ However , the peak of ECE like activity ( 10 . 4 pmol ET 1 / h / 10 ( 6 ) cells ) localized in the 0 . 8 M sucrose band was inhibited by 79 % in the presence of 100 microM PHOS . ( ABSTRACT TRUNCATED AT 250 WORDS ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We have investigated further the role of the PHOS sensitive ECE in the conversion of big ET 1 to ET 1 . ^^^ These results are consistent with both cell types having a PHOS sensitive ECE that is readily accessible to exogenous big ET 1 and is therefore probably located on the plasma membrane . ^^^ Furthermore , another intracellular ECE may play a part in the endogenous intracellular formation of ET 1 in EA . hy 926 cells . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The aim of this study was to test the effects of the endothelin converting enzyme ( ECE ) inhibitor phosphoramidon on pressor responses to ET 1 and its precursor , big ET 1 , in isolated perfused rat kidneys and in pithed rats . ^^^ These data illustrate that the pressor responses to big ET 1 in the rat , both in vivo and in vitro , are due to its conversion into ET 1 by a phosphoramidon sensitive ECE . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Human and porcine big ET 1 and big ET 2 are similarly potent in contracting parenchymal strips of the guinea pig lung while big ET 3 is inactive , suggesting that the endothelin converting enzyme ( ECE ) which converts big ET 3 is not present and that at least two distinct ECE activities exist , one selective for big ET 1 and big ET 2 and one for big ET 3 . ^^^ Metalloendoprotease inhibitors ( phosphoramidon and DL thiorphan ) , but not captopril , inhibited the contractions elicited by human big ET 1 and big ET 2 but DL thiorphan was less active , suggesting that a non selective enzymatic process is involved in conversion of big ET 1 and big ET 2 in addition to a phosphoramidon sensitive ECE . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Both COS 1 cells expressing human ECE and its membrane fraction converted big ET 1 most efficiently among big ETs . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In both hormome dependent ( MCF 7 , T 47 D ) and hormone independent ( MDA MB 231 ) breast cancer cell lines the putative endothelin converting enzyme ( ECE ) exhibited apparent Michaelis Menten kinetics when converting added big ET 1 to ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme ( ECE ) is essential for generation of the biological effects of endothelin 1 ( ET 1 ) from a precursor , big endothelin 1 ( Big ET 1 ) . ^^^ ECE activity was determined using an ET 1 specific radioimmunoassay system . ^^^ None of the D amino acid containing Big ET 1 analogs were apparently cleaved by ECE , however , one of the synthetic peptides , [ D Val 22 ] Big ET 1 [ 16 38 ] , strongly inhibited the ECE activity . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Co expression of the cloned cDNA of bovine ECE with human preproET 1 cDNA in CHO K 1 cells resulted in the production of mature ET 1 and this production was inhibited by phosphoramidon . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
This report presents evidence that a permanent human endothelial cell line , EA . hy926 , preserves the ECE activity of HUVEC and is useful for the study of ECE and its regulation of ET 1 production . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Biosynthesis of ET 1 from its precursor big endothelin 1 ( BET 1 ) is mediated by endothelin converting enzyme ( ECE ) , a phosphoramidon sensitive metalloprotease . ^^^ At protein concentrations suitable for measurement of ECE activity ( 0 . 2 mg / ml ) , L GPLGM contains a high concentration of ET receptors and shows a rapid rate of ET 1 binding to the membrane preparation ( binding equilibrium in < 5 min ) . ^^^ Thus , we have utilized L GPLGM preparation for both ECE activity and measurement of ET 1 binding in a single step assay for the determination of enzyme activity . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin ( ET ) 1 is an endothelium derived vasoconstrictor and mitogen peptide generated from an intermediate form ( big ET 1 ) by endothelin converting enzyme ( s ) ( ECE ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Three compounds , ( 2 , 3 dimercapto 1 propanol ( DMP ) , toluene 3 , 4 dithiol ( TDT ) and 8 mercaptoquinoline ( 8 MQ ) ) , which inhibited ECE in in vitro studies , exhibited inhibitory activity towards big ET 1 induced sudden death in mice , while EDTA did not . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Aspergillomarasmine A and B ( AM A and B ) , which were isolated from the cultured broth of an unidentified fungus N 877 , showed apparent inhibition against endothelin converting enzyme ( ECE ) from bovine endothelial cells as measured by the formation of endothelin 1 ( ET 1 ) converted from big endothelin 1 ( bET 1 ) , with IC 50 values of 3 . 4 and 2 . 5 microM for AM A and B , respectively . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
A metalloproteinase inhibitor , phosphoramidon ( 10 mg kg 1 , i . v . ) , which inhibits the activity of endothelin converting enzyme ( ECE ) , delayed the onset of big ET 1 induced haemoconcentration , but failed to alter the maximal value and the duration of the haemoconcentration . 5 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) , a 21 amino acid peptide produced by endothelial cells , results from the cleavage of preproendothelin , generating Big ET 1 , which is then cleaved by the ET converting enzyme ( ECE ) to form ET 1 . ^^^ Endothelin 1 ( ET 1 ) , a 21 amino acid peptide produced by endothelial cells , results from the cleavage of preproendothelin , generating Big ET 1 , which is then cleaved by the ET converting enzyme ( ECE ) to form ET 1 . ^^^ Therefore , we studied the effects of Big ET 1 in isolated perfused lungs from 1 and 7 day old piglets using the ECE inhibitor , phosphoramidon , and the ETA receptor antagonist , BQ 123Na . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) , a 21 amino acid potent vasoconstrictor peptide , is produced from the biologically inactive intermediate big ET 1 via an endoproteolytic cleavage between Trp 21 and Val 22 by endothelin converting enzyme ( ECE ) . cDNA sequence analysis predicts that the two other members of the endothelin family , ET 2 and ET 3 , are also generated from the corresponding intermediates called big ET 2 and big ET 3 , respectively . ^^^ Endothelin 1 ( ET 1 ) , a 21 amino acid potent vasoconstrictor peptide , is produced from the biologically inactive intermediate big ET 1 via an endoproteolytic cleavage between Trp 21 and Val 22 by endothelin converting enzyme ( ECE ) . cDNA sequence analysis predicts that the two other members of the endothelin family , ET 2 and ET 3 , are also generated from the corresponding intermediates called big ET 2 and big ET 3 , respectively . ^^^ The metalloproteinase inhibitor phosphoramidon inhibited the conversion of big ET 1 into mature ET 1 both in vivo and in cultured endothelial cells , suggesting that ECE may be a neutral metalloproteinase . ^^^ Taken in conjunction with the previous finding that neither thiorphan nor bacitracin affected the conversion of endogenously synthesized big ET 1 in cultured endothelial cells , we conclude that physiologically relevant ECE found in the endothelial cells is more similar to M 1 than to M2 . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) converting enzyme ( ECE ) activity in the human serum lipoprotein fraction was studied using a sensitive enzyme immunoassay and reverse phase high performance liquid chromatography . ^^^ Endothelin 1 ( ET 1 ) converting enzyme ( ECE ) activity in the human serum lipoprotein fraction was studied using a sensitive enzyme immunoassay and reverse phase high performance liquid chromatography . ^^^ The ECE activity of cleaving synthetic human big ET 1 into ET 1 by the serum lipoprotein fraction was about 14 times greater than that by whole serum , and the activity was closely associated with lipoprotein itself . ^^^ These results suggest that the serum lipoprotein ECE may be involved in the processing of big ET 1 to ET 1 in the circulatory system . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Partial reduction of the pressor response to exogenously administered Big ET 1 was observed with selected rat lung ECE inhibitors . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 ( ET 1 ) is a potent endogenous vasoconstrictor peptide formed through a specific conversion of its intermediate precursor , big ET 1 , by an endothelin converting enzyme ( ECE ) . ^^^ Endothelin 1 ( ET 1 ) is a potent endogenous vasoconstrictor peptide formed through a specific conversion of its intermediate precursor , big ET 1 , by an endothelin converting enzyme ( ECE ) . ^^^ The present study evaluates the capacity of the ECE to convert the three big endothelins ( big ET 1 , big ET 2 , and big ET 3 ) , by comparing the pressor responses to these peptides with those induced by their respective metabolites ( ET 1 , 2 , and 3 ) in the rat in vivo , anesthetized either with a mixture of ketamine / xylazine or with urethane . ^^^ On the other hand , big ET 2 ( 1 38 ) , in contrast to ET 2 or big ET 1 , did not release prostacyclin from the rat perfused lung , thus indicating that big ET 2 ( 1 38 ) is poorly converted in the pulmonary vasculature , and that the phosphoramidon sensitive ECE responsible for the pressor effects of big ET 2 is localized elsewhere in the systemic circulation . ^^^ Nonetheless , even in what we consider as optimal conditions of anesthesia ( threshold dose for the pressor response to ET 1 in ketamine / xylazine treated rats : 0 . 01 nmol / kg ) , big ET 3 remains far less active than big ET 1 as a pressor peptide in the rat , suggesting a preferential processing of the latter by the ECE . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 is a potent endothelium derived vasoconstrictor peptide that is generated through cleavage of its precursor big endothelin 1 by ' endothelin converting enzyme ' ( ECE ) in resistance vessels , including those of the forearm vascular bed . ^^^ We examined whether ECE activity is present in human hand veins and whether endothelin 1 or big endothelin 1 potentiate sympathetically mediated venoconstriction . 2 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
These data confirm that exogenous big ET 1 is locally converted to ET 1 and CTF in the human forearm , at least in part by a phosphoramidon sensitive ECE . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The biologically inactive precursor proendothelin 1 ( proET 1 ) is initially processed intracellularly to the intermediate big endothelin peptide ( big ET 1 ) before its conversion to the endothelin 1 ( ET 1 ) peptide by the endothelin converting enzyme ( ECE ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
To develop a new family of endothelin converting enzyme ( ECE ) inhibitors , we assessed the inhibitory properties of an N and C terminal truncated analogue of big endothelin ( ET ) 1 [ 1 38 ] , [ Phe 22 ] big ET 1 [ 19 37 ] , on the renal vasoconstrictor properties of big ET 1 and ET 1 . ^^^ Our results suggest that [ Phe 22 ] big ET 1 [ 19 37 ] may be a useful lead molecule for the development of more selective and enzyme resistant inhibitors of the membrane bound ECE . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In conclusion , we can speculate that the big ET 1 contraction in RSA is mediated by an ECE , probably present on smooth muscle cells , which is susceptible to NEP inhibitors and is different from the ECE on endothelial cells . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
These results suggest that the putative endothelin converting enzyme ( ECE ) is involved in the conversion of big ET 1 to ET 1 in GPUB and the conversion of big ET 2 to ET 2 by a nonselective enzymatic process . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In an attempt to identify the organs involved in the ET 1 induced release of PGI 2 in vivo , we characterized the receptors responsible for the release of this eicosanoid and also monitored the activity of the endothelin converting enzyme ( ECE ) in rabbit pulmonary lobe . ^^^ Furthermore , the ECE localized in the rabbit pulmonary vasculature is relatively selective for big ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
As a prelude to developing affinity labels for studying the interaction between big ET 1 and endothelin converting enzyme ( ECE ) , the effect on biological activity of modifying human big ET 1 with the N hydroxysuccinimide esters of 3 ( p hydroxyphenyl ) propionic acid ( HPP ) or S acetylthioglycolic acid ( ATG ) was investigated . ^^^ Thus , incorporation of the HPP or ATG groups , or removal of disulphide bridges decreases the ability of plasma membrane ectoenzyme ECE activities to hydrolyze the Trp 21 Val22 bond of big ET 1 . ^^^ This indicates that the conformation of big ET 1 is important for obtaining an optimal rate of hydrolysis by ECE activities in vivo and in vitro . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We therefore investigated whether endothelin converting enzyme ( ECE ) activity could be demonstrated in human vessels , and the effects of inhibition of the generation or actions of ET 1 on vascular tone in healthy men . ^^^ Brachial artery infusion of local doses of big ET 1 caused a slow onset , dose dependent forearm vasoconstriction that was abolished by co infusion of the ECE inhibitor phosphoramidon . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Interestingly enough , both of the immortalized cells and the early passage HUVEC from which the immortalized cells were obtained biosynthesized and secreted the same levels of ET 1 suggesting full maintenance of its biosynthetic pathway including the presence of active ECE , which cleaves big endothelin 1 ( big ET 1 ) to ET 1 and regulation factors . ^^^ Obtaining these immortalized human endothelial cells without alteration of the differentiated characteristics constitutes a useful model : ( a ) to study ET 1 secretion , gene regulation , and human ECE , which may be an important therapeutic target in disease conditions in which ET 1 is to be implicated ; ( b ) to study L arginine transport , which is a key step in the formation of EDRF ; ( c ) to study IL 1 beta and IL 6 secretions , and gene regulations ; ( d ) to substitute large quantities of HUVEC ; and , finally , ( e ) to reproduce , starting with different primary endothelial cells both from human and animal origin . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Significant amount of endothelin 1 ( ET 1 ) production and endothelin converting enzyme ( ECE ) activity have been detected in cultured guinea pig airway epithelial cells . ^^^ Northern blot analysis revealed that mRNA level of ET 1 was increased in the LPS stimulated epithelial cells , but the effect on the ECE mRNA expression was obscure . ^^^ These data suggest that the ET 1 production in the airway epithelial cells is regulated by the level of ET 1 mRNA expression with a constitutive manner , and the level of ECE , which act at a key biosynthetic step of the conversion of big ET 1 to ET 2 , seems not to make a major contribution to the regulation of ET 1 release . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
CONCLUSIONS : These results demonstrate that the enhancement of ET 1 action , possibly caused by the activation of ECE , plays a primary role in regulating the retinal hemodynamic response to hyperoxia . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Incubation of strips of GPLP with the dual endothelin converting enzyme ( ECE ) and neutral endopeptidase ( NEP ) inhibitor , phosphoramidon ( 10 microM ) , as well as two other NEP inhibitors thiorphan ( 10 microM ) or SQ 28 , 603 ( 10 microM ) decreased by 43 % ( P < 0 . 05 ) , 42 % ( P < 0 . 05 ) and 40 % ( P < 0 . 05 ) the contractions induced by 30 nM of big ET 1 respectively . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme ( ECE ) from intact cells of a permanent human endothelial cell line , EA . hy926 , was studied by examining the effects of phosphoramidon , an endothelin converting enzyme inhibitor , on the levels of secreted endothelin 1 and big endothelin 1 . ^^^ The specific ECE activity was demonstrated by a phosphoramidon dose dependent decrease in ET 1 level with a concomitant increase in big ET 1 level . ^^^ Other serine , acid , and cysteine protease inhibitors had no effect on the endogenous synthesis of ET 1 and big ET 1 supporting the evidence that ECE is insensitive to these protease inhibitors as has been demonstrated with the isolated enzyme . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The enzyme responsible for converting Big ET 1 to ET 1 is a metalloprotease called endothelin converting enzyme ( ECE ) . ^^^ Intravenous administration or topical application of an active inhibitor of ECE , CGS 26303 , blocked vasoconstrictor responses to topically applied Big ET 1 but not to ET 1 . ^^^ In contrast , topical application of a structurally related compound that does not inhibit ECE , CGS 24592 , was ineffective in blocking vasoconstriction that was elicited by a topical application of Big ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Since the discovery of the most potent vasoconstrictor peptide , endothelin , in 1988 , explosive investigations have rapidly clarified much of the basic pharmacological , biochemical and molecular biological features of endothelin , including the presence and structure of isopeptides and their genes ( endothelin 1 , 2 and 3 ) , regulation of gene expression , intracellular processing , specific endothelin converting enzyme ( ECE ) , receptor subtypes ( ETA and ETB ) , intracellular signal transduction following receptor activation , etc . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
An obligatory step in the biosynthesis of endothelin 1 ( ET 1 ) is the conversion of its inactive precursor , big ET 1 , into the mature form by the action of specific , phosphoramidon sensitive , endothelin converting enzyme ( s ) ( ECE ) . ^^^ In renal cortical slices incubated with big ET 1 , pretreatment with phosphoramidon ( an ECE inhibitor ) reduced tissue immunoreactive ET 1 to a level similar to that of cortical tissue not exposed to big ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Three isoforms of ET , namely ET 1 , ET 2 and ET 3 , are generated from their respective intermediate precursors big ETs through specific endoproteolytic cleavage by endothelin converting enzyme ( ECE ) . ^^^ Pre incubation of tissue with a metalloprotease ECE inhibitor phosphoramidon ( 10 microM ) strongly inhibited the response to big ET 1 , but not to ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The biological activity of bET requires proteolytic cleavage to ET 1 by endothelin converting enzymes ( ECE ) and possibly other proteases such as neutral endopeptidase 24 . 11 ( NEP 24 . 11 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
However , at a high concentration , SQ 28 603 also inhibited the basal release of ET 1 , which would suggest a non selective inhibitory activity against ECE . ^^^ These data suggest that ET 1 is simultaneously produced and degraded by guinea pig tracheal epithelial cells via phosphoramidon sensitive ECE and NEP pathways , respectively . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
These findings demonstrate that inhibiting the conversion of Big ET 1 to ET 1 via intravenous administration of an ECE inhibitor can be an effective strategy for limiting angiographic vasospasm after SAH . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Responses to ET 1 were unaffected by either the neutral endopeptidase ( NEP ) inhibitor thiorphan ( 10 ( 5 ) M ) or by the dual NEP / ECE inhibitor phosphoramidon ( 10 ( 5 ) M ) . ^^^ To conclude we have demonstrated the presence of a phosphoramidon sensitive ECE on the smooth muscle layer of the human umbilical vein which can convert big ET 1 , big ET 2 ( 1 37 ) , big ET 2 ( 1 38 ) and big ET 3 to their mature biologically active forms . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
It is generated from its inactive intermediate , big ET 1 , through the action of endothelin converting enzyme ( ECE ) . ^^^ This is the first ultrastructural localization of ECE in lung and the first time big ET 1 and ECE have been colocalized by immunogold in a vesicular population , 50 to 100 nm in diameter . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
However phosphoramidon ( 100 microM ) , an inhibitor of ECE and NEP , almost abolished specific binding , indicating that both NEP and ECE cleave big ET 1 in the kidney . ^^^ We conclude that big ET 1 is processed by NEP and ECE in human kidney and that the cleaved product binds predominantly to the ET ( B ) receptor subtype . ^^^ ECE may be a therapeutic target in the attenuation of renal diseases in which ET 1 has been implicated . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelins ( ET ) are potent vasoactive peptides present in many ocular structures and are formed from precursor Big endothelins ( Big ET 1 ) by the action of an endothelin converting enzyme ( ECE ) . ^^^ Pre treatment with phosphoramidon ( 1 micron ) an ECE inhibitor , followed by TNF alpha stimulation , decreased ir ET 1 levels . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Here , the stimulated ( lipopolysaccharide or interleukin 1 beta ) production of ET 1 from guinea pig tracheal epithelial cells was abolished by CGS 26303 or CGS 26393 , two ECE / neutral endopeptidase ( NEP ) inhibitors , but was unaffected by CGS 24592 , a specific NEP inhibitor . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The distribution of ECE like immunoreactivity was also investigated to determine possible sites involved in the cleavage of big ET 1 to ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We studied effects of Ang 2 ( 200 ng / kg / min ) and ETA antagonist LU 135252 ( 50 mg / kg / d ) in WKY rats in vivo investigating vascular and renal ET 1 protein expression , functional endothelin converting enzyme ( ECE ) activity , and clearance of ( 125I ) ET 1 . ^^^ Infusion of Ang 2 for two weeks increased ET 1 protein content in aorta ( 4 . 7 fold ) and femoral artery ( 1 . 6 fold ) with and without endothelium and in kidneys ( 3 fold , p < 0 . 05 ) and enhanced functional ECE activity ( p < 0 . 05 ) . ^^^ The Ang 2 induced increase in tissue ET 1 content and functional ECE activity was completely prevented by LU 135252 ( p < 0 . 05 ) . ^^^ It is concluded that Ang 2 increases ET 1 protein and functional ECE activity in vascular smooth muscle and kidney through ETA receptors in vivo . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Therefore , we believed that the increase in ET 1 production in the failing heart originated from an increase in preproET 1 production rather than increase in ECE . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Membrane ECE activity was phosphoramidon sensitive , in contrast to the cytosolic activity capable of producing ET 1 from big ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 3 ( ET 3 ) , a potent vasoactive peptide , is considered to be produced from big ET 3 by endothelin converting enzyme ( ECE ) like the other members of the endothelin family ( ET 1 and ET 2 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The enhanced response of atherosclerotic human coronary arteries to big ET 1 appears to be due to up regulation of endothelin converting enzyme ( ECE ) activity rather than to an augmented response of the arteries to ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Since proET 1 is known to have approximately 1 / 100 the potency of ET 1 for contracting an isolated blood vessel , the change in the activity of endothelin converting enzyme ( ECE ) has been proposed as an important factor in the pathophysiology of various hypertensive diseases . ^^^ CONCLUSION : Differences in ET 1 / proET 1 ratio in relation to changes in MAP after a single intravenous administration of rHuEpo suggest a potential role for ECE in the pathogenesis of rHuEpo induced hypertension . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Aortas were excised and divided for determination of tissue ET 1 concentration by RIA and immunohistochemical analysis of ECE . ^^^ In addition , ECE immunoreactivity is increased in early atherosclerosis and may therefore contribute to the generation of local ET 1 in early experimental atherosclerosis . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
This is processed intracellularly to the inactive intermediate big ET 1 , which is hydrolyzed by endothelin converting enzyme ( ECE ) to generate ET 1 , but the precise identity of the physiologically relevant ECE has yet to be confirmed . ^^^ We describe here experimental investigations aimed at defining the regulation of ET 1 synthesis and its relationship to the biosynthesis of ECE . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
However , decreasing synthesis and release of ET 1 by blocking the endothelin converting enzyme ( ECE ) activity may also prove worthwhile . ^^^ In this study we have therefore investigated the effect of several putative ECE inhibitors in isolated rat basilar artery by measuring isometric contraction after application of big ET 1 , the precursor peptide which is not vasoactive in itself . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
When injected at 30 mg / kg i . v . in conscious rats , followed by a challenge with big ET 1 at 1 nmol / kg i . v . , this compound suppressed by 44 % the increase in mean arterial blood pressure owing to the generation of ET 1 by ECE . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
BACKGROUND Endothelin ( ET ) 1 is generated from big ET 1 by endothelin converting enzyme ( ECE ) . ^^^ Because selective enzymatic processing of ET 1 formation appears to be an important therapeutic target for CHF , we investigated the acute effects of a specific ECE inhibitor on cardiorenal and endocrine functions in CHF compared with those of a selective ETA receptor antagonist . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The endothelin system is composed of three endothelin isoforms ( ET 1 , ET 2 , and ET 3 ) , the endothelin receptors ETA and ETB , and the endothelin converting enzyme ( ECE ) . ^^^ Human ovaries and gonadotropin stimulated monkey ovaries were studied using immunohistochemistry for endothelin , and in situ hybridization with probes for ET 1 , ET 2 , ET 3 , ETA and ETB receptors , and ECE . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
This cytokine stimulated release of ET 1 was inhibited by a series of dual endothelin converting enzyme ( ECE ) / neutral endopeptidase inhibitors , phosphoramidon , CGS 26303 , and CGS 26393 , with an accompanying increase in big ET 1 release but with no effect on expression of mRNA for prepro ET 1 . ^^^ Thus VSMCs most probably contain , like endothelial cells , an intracellular ECE responsible for the endogenous synthesis of ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ECE activity was determined by conversion of exogenously added big endothelin 1 ( big ET 1 ) to ET 1 in subcellular fractions obtained by sucrose density gradient centrifugation of human umbilical vein endothelial cell homogenates . ^^^ Confocal microscopy revealed a punctate pattern of ECE 2 like immunoreactive staining in the cell cytosol , suggesting localization to secretory vesicles with a possible role in processing big ET 1 while in transit to the cell surface via the constitutive secretory pathway . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Big endothelin 1 ( big ET 1 ) is converted to 21 amino acid residue endothelin 1 ( ET 1 ) via a specific cleavage at Trp 21 Val22 by endothelin converting enzyme ( ECE ) . ^^^ ECE 1a , a unique membrane bound enzyme , processes big ET 1 more efficiently than other big ET isoforms , which mainly differ in the C terminal tail ( residues 22 38 ) . ^^^ The mutant and wild type cDNAs were transiently transfected into Chinese hamster ovary cells along with ECE 1a cDNAs , and concentrations of the resulting recombinant peptides , ET 1 and big ET 1 , in the transfection media were then measured . ^^^ These findings suggest that the C terminal tail has an important role in the intracellular processing of big ET 1 by ECE 1a . ^^^ Herein we also report that a recombinant big ET 1 analog we previously generated and characterized , ( Ala 21 ) big ET 1 , inhibits ECE 1a activity in a dose dependent ( K i=1 microM ) and competitive manner . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ProET 1 is acted on by a furin like enzyme to generate big ET 1 , a 38 39 amino acid peptide , which is converted to the mature 21 amino acid peptide ET 1 by ET converting enzyme ( ECE ) in endothelial cells , both intracellularly and on the cell membrane , and on the surface of underlying smooth muscle cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
With the putative ECE inhibitor phosphoramidon ( 10 ( 3 ) M ) in the bath a small rightwards shift of the CEC for big ET 1 was observed in control segments and a more marked one in de endothelialized segments . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
AIMS : The aims of this study were to define and characterize the different mechanisms and sites of clearance of plasma endothelin 1 ( ET 1 ) and big endothelin 1 ( BigET 1 ) and evaluate possible effects of ETA versus combined ETA and ETB receptor blockade or endothelin converting enzyme ( ECE ) inhibition . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We now show that superoxide can inhibit endothelin converting enzyme activity ( ECE ) and decrease endothelin 1 synthesis . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In the present study we investigated , in the renal tissue of PHRs and PNRs : ( 1 ) preproET 1 and preproET 3 mRNAs as well as ET 1 and ET 3 peptide distribution , ( 2 ) endothelin converting enzyme ( ECE ) 1 mRNA expression , and ( 3 ) ET receptors and their characteristics in membranes of glomeruli and papillae . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
OBJECTIVE : To explore the role of airway smooth muscle cells ( ASMC ) stimulated by inflammatory factors in the development of asthma and bronchial hyperresponsiveness ( BHR ) and the possible mechanism of low dose theophylline in the treatment of airway inflammation , the effects of GM CSF on endothelin 1 and endothelin converting enzyme ( ECE ) gene expression in human ASMC and theophylline on their expressions were investigated . ^^^ Endothelin 1 and ECE gene expresion were measured by RT PCR . ^^^ RESULT : There was no ET 1 gene expression in control group , but strong expression in GM CSF treated group ; theophylline entirely inhibited GM CSF induced ET 1 gene expression in the ASMC ; no significant difference of ECE gene expression was found in three groups . ^^^ CONCLUSION : GM CSF causes a strong ET 1 gene expression but not ECE gene expression in cultured human airway smooth muscle cells ; theophyllin inhibites this abnormal expression which may be one of the anti inflammatory mechanisms of low dose theophylline in the management of chronic airway inflammation . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Higher basal ET 1 concentrations in astrocyte media from ET ( B ) deficient ( sl / sl ) versus wildtype ( + / + ) rats suggested that altered ECE activity may be related to the absence of ET ( B ) receptors . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Increases in [ Ca2+ ] 1 caused by ET 1 ( 1 31 ) , big ET 1 and ET 2 ( 1 31 ) were completely inhibited by 10 ( 4 ) M phosphoramidon , a dual neutral endopeptidase ( NEP ) / endothelin converting enzyme ( ECE ) inhibitor , and 10 ( 5 ) M thiorphan , a NEP inhibitor . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
All three endothelin precursor peptides , i . e . big endothelin 1 ( big ET 1 ) , big endothelin 2 ( big ET 2 ) and big endothelin 3 ( big ET 3 ) , produced contractile responses in human isolated bronchi , demonstrating the presence of functional endothelin converting enzyme ( ECE ) in this tissue . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ECE inhibition was confirmed by increased big ET 1 to ET 1 ratio ( 0 . 23 + / 0 . 06 vs 0 . 05 + / 0 . 02 , ECE inhibitor vs control , p < 0 . 05 ) . ^^^ This study concludes that selective ECE inhibitor with FR 901533 reduces the conversion of big ET 1 to ET 1 in post MI rats and improves some parameters of cardiac remodeling early post MI . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET 1 in the myocardial interstitium : relation to myocyte ECE activity and expression . ^^^ Accordingly , myocardial interstitial ET 1 levels and myocyte endothelin converting enzyme ( ECE ) 1 activity and expression with the development of CHF were examined . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
CysA increased the production of ET 1 and the expression of ET 1 mRNA without affecting CNP synthesis and endothelin converting enzyme ( ECE ) 1 mRNA expression . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Therefore , compounds that can suppress the production of ET 1 by inhibiting ECE while simultaneously potentiating the levels of ANP by inhibiting NEP may be novel agents for the treatment of cardiovascular and renal dysfunction . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Vascular ECE activity was determined by conversion of exogenously added bigET 1 to ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The relationship between soluble and membrane bound endothelin converting enzyme ( ECE ) activity with the level of endothelin 1 ( ET 1 ) synthesis was investigated in cultured endothelial cells . ^^^ Escherichia coli lipopolysaccharide ( LPS ) was used to stimulate ET 1 synthesis , and brefeldin A , monensin , colchicine or cytochalasin B , which disrupt peptide biosynthetic pathways in a variety of ways , were tested for their ability to modify changes in ET 1 synthesis and ECE levels . ^^^ Levels of soluble ECE activity , but not those of membrane bound ECE activity , correlated with ET 1 synthesis . ^^^ These results suggest the soluble ECE activity is likely to play a role in ET 1 biosynthesis . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
However , none of the shorter peptides was able to inhibit the cleavage of big ET 1 by ECE , suggesting that they are not recognized by the enzyme . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The mRNAs of preproendothelin 1 and of endothelin converting enzyme ( ECE ) were expressed by cells , as shown by RT PCR studies . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
These results suggest that suppression of ET 1 production by ECE inhibitors may prove to be efficacious for the treatment of hemolysate induced cytotoxicity on cerebral endothelial cells . . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The increased ET 1 tissue concentration is not a result of an altered big ET 1 synthesis in biliary liver fibrosis , suggesting an increased activity of endothelin converting enzyme ( ECE ) in liver cirrhosis . . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
OBJECTIVE : To investigate the expressions of endothelin 1 ( ET 1 ) and endothelin converting enzyme ( ECE ) mRNA in bronchial mucosal biopsis from asthmatics , and the effect of inhaled corticosteroids on the expressions of ET 1 and ECE genes . ^^^ The expression of ECE mRNA in non steroid group was 0 . 31 + / 0 . 04 , and 0 . 30 + / 0 . 05 in control group , P = 0 . 238 . ( 2 ) The ET 1 and ECE mRNA expressions were 0 . 22 + / 0 . 01 and 0 . 16 + / 0 . 01 respectively in steroid treated group . ( 3 ) The naked eye bronchial mucosal inflammatory score was 6 . 0 + / 1 . 9 in non steroids treated group , moreover , the expression of ET 1 mRNA was positively correlated with the score ( r = 0 . 78 , P < 0 . 05 ) . ^^^ CONCLUSION : There was markedly higher ET 1 mRNA expression in the bronchial mucosa in asthmatics , but the ECE mRNA expression was unchanged significantly ; Inhaled corticosteroids obviously inhibited both ET 1 mRNA and ECE mRNA expressions in bronchial mucosa , which may be one of the anti inflammatory mechanisms of inhaled corticosteroid in management of bronchial asthma . . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The expression of big ET 1 , ET converting enzyme ( ECE ) and ET ( A ) receptors were examined in rat pulmonary arteries under normal and hypoxic conditions using an immunohistochemical method and Northern blot analysis . ^^^ Following exposure to hypoxia , messenger ribonucleic acid ( mRNA ) expression of ET 1 and ET ( A ) receptors were up regulated by two fold and immunoreactivities for big ET 1 , ECE , and ET ( A ) receptors significantly increased by two to five fold in the distal segments . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
This study investigated whether inhibition of big ET 1 processing by inhibition of endothelin converting enzyme ( ECE ) could , therefore , offer an alternative therapeutic strategy in the prevention of vein graft intimal hyperplasia . ^^^ ECE immunostaining was reduced in the ECE / NEP inhibited veins , although ET 1 staining was also present . ^^^ ET 1 expression was intense in the thickened neointimas of NEP inhibited veins , which also showed significant ECE staining . ^^^ Elevated levels of big ET 1 were measured in the ECE / NEP inhibited veins , consistent with reduced ECE activity . ^^^ CONCLUSION : There is a requirement for potent and selective inhibitors of ECE to evaluate fully the potential therapeutic benefits of blocking ET 1 biosynthesis . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Posthemorrhagic vasospasm can be counteracted by the administration of phosphoramidon , which blocks the endothelin converting enzyme ( ECE ) responsible for the conversion of big endothelin into a fully active ET 1 peptide . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
In conclusion , ET 1 plays a critical role in the structural deterioration of the vasculature during the progression of CHF , and ECE inhibitors can prevent the development of vascular remodeling . . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
There was no effect of the ECE inhibitor PD 159790 ( 30 microM ) , the ECE / NEP inhibitor phosphoramidon ( 100 microM ) or the serine protease inhibitor chymostatin ( 100 microM ) on ET 1 ( 1 31 ) responses in either artery . 5 . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The enhanced production of endothelin 1 ( ET 1 ) in atherosclerotic arteries may be related to increased activity of the endothelin converting enzyme ( ECE ) which converts big ET 1 to ET 1 . ^^^ In conclusion , administration of big ET 1 results in enhanced vasoconstriction and increased formation of ET 1 in patients with atherosclerosis as compared to healthy controls which may be due to increased activity of ECE . . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
OBJECTIVE : To explore the mechanism of TNF alpha induced ET 1 release and evaluate the effects of endothelin converting enzyme ( ECE ) antisense oligonucleotides ( oDNS ) on TNF alpha induced ET 1 release from airway smooth muscle cells ( ASMC ) . ^^^ TNF alpha induced ECE mRNA expression and ET 1 release from above cultured cells were determined by RT PCR and ELISA . ^^^ RESULTS : ET 1 levels ( 10 . 1 + / 0 . 3 ) ng / L and ECE expression ( ECE / beta actin : 0 . 228 + / 0 . 015 ) in cultured ASMC incubated with 1 , 000 U / ml TNF alpha were significantly higher than those in controls without TNF alpha incubation ( 7 . 3 + / 0 . 8 ) ng / L , ( 0 . 132 + / 0 . 032 , all P < 0 . 01 ) . ^^^ However , after transfecting antisence ECE oDNS in those cells , ET 1 levels and ECE expressions were significantly lower than those in control cells without antisense transfection . ^^^ CONCLUSIONS : Abnormal expression of ECE mRNA may be a keypoint responsible for TNF alpha induced ET 1 release in human ASMC ; TNF alpha induced ET 1 release and ECE mRNA expression from human ASMC are inhibited by antisense oligonucleotide of ECE . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
CONCLUSIONS : These findings suggest that the increased secretion of ET 1 leading to enhanced pigmentation in SK results from the co ordinated increased expression of TNF alpha and ECE 1alpha . . ^^^ |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
This increase is attributed to the higher conversion rate of big ET 1 to ET 1 because the ET converting enzyme ( ECE ) inhibitor phosphoramidon , at a concentration of 10 ( 6 ) mol / L , causes an inhibition in the response to big ET 1 by 52 . 6 % in normal kidneys , whereas this inhibition with the same concentration of phosphoramidon was found to be significantly decreased in kidneys isolated from GLY pretreated rabbits . 5 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
To clarify the potential involvement of ECE in the processing and secretion of ET 1 by human keratinocytes , we synthesized the N terminal peptide of human ECE 1alpha and generated a rabbit polyclonal antibody ( alphaPEPT 6 ) that specifically recognizes ECE 1alpha . ^^^ Collectively , our results demonstrate for the first time that ECE 1alpha is expressed at significant levels in various types of human skin cells ( including keratinocytes ) and that it plays a constitutive role in the processing and UVB inducible secretion of ET 1 by human keratinocytes , which leads to the stimulation of pigmentation in the epidermis . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We investigated urinary and plasma ET 1 ( uET 1 , pET 1 ) , BigET 1 ( uBigET 1 , pBigET 1 ) concentrations , and plasma soluble endothelin converting enzyme ( ECE ) concentrations in 381 adult caucasian kidney allograft recipients with graft survival of more than 2 years from the outpatients department of our clinic . ^^^ D . ; uET 1 / meanProt : 15+ / 24 versus 21+ / 40 pmol / g , P=0 . 139 ; uBigET 1 / meanProt : 34+ / 55 versus 19+ / 23pmol / g , P=0 . 248 ) . pET 1 elevation in patients receiving CI might be more likely to be due to elevated conversion of pBig ET 1 by more ECE , and not to higher concentrations of pBigET 1 . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
A selective endothelin converting enzyme ( ECE ) inhibitor , CGS 35066 ( 1 mg kg ( 1 ) ) , significantly reduced the second phase pressor response and increase in PIP triggered by ET 1 ( 1 31 ) . 3 . ^^^ We suggest that , in order to raise MAP , ET 1 ( 1 31 ) requires conversion to ET 1 , predominantly by ECE and to a lesser extent neutral endopeptidase 24 . 11 , whereas the reverse holds true regarding its pharmacological effects in airways . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Although the receptors mediating the effects of ET 1 human cerebrovasculature are well characterized , data concerning the functionally relevant ET converting enzyme ( ECE ) activity are scarce . ^^^ The level of ECE activity was analyzed by comparing the shift in the concentration effect curves obtained for ET 1 and its precursor , big ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET 1 is synthesized from preproET 1 by the action of ET converting enzyme ( ECE ) . ^^^ Using quantitative reverse transcription PCR , relative levels of ET 1 and ECE mRNA expression were measured and compared with a housekeeping gene ( ribosomal protein L 32 ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin ( ET ) converting enzyme ( ECE ) is a rate limiting step in ET 1 generation , and its expression and activity are increased significantly with the development of congestive heart failure ( CHF ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The present study examined the roles of endothelin converting enzyme ( ECE ) , neutral endopeptidase ( NEP ) and mast cell chymase as processors of the endothelin ( ET ) analogues ET 1 ( 1 21 ) , ET 1 ( 1 31 ) and big ET 1 in the trachea of allergic mice . ^^^ The ECE inhibitor CGS 35066 ( 10 microM ) inhibited contractions induced by big ET 1 ( 4 . 8 fold rightward shift of dose response curve ; P < 0 . 05 ) , but not those induced by either ET 1 ( 1 21 ) or ET 1 ( 1 31 ) . ^^^ These data suggest that big ET 1 is processed predominantly by a CGS 35066 sensitive ECE within allergic airways rather than by mast cell derived proteases such as chymase . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
We investigated urinary and plasma ET 1 ( uET 1 , pET 1 ) and BigET 1 ( uBigET 1 , pBigET 1 ) concentrations , and plasma soluble ET converting enzyme ( ECE ) concentration in 310 adult Caucasian kidney allograft recipients with graft survival of more than 2 years from the outpatients department of our clinic . ^^^ However , the actual concentration of ET 1 , soluble ECE , and BigET 1 in urine and plasma in our study is not associated with parameters for progression of chronic graft dysfunction . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
While ACE and ECE are respectively involved in the transformation of angiotensin 1 and Big ET into angiotensin 2 and ET 1 respectively , which possess vasoconstrictor and mitogenic properties , NEP is involved in the degradation of atrial natriuric factor ( ANF ) , which possesses vasorelaxant , diuretic / natriuretic and antihypertrophic properties . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
INTRODUCTION : The aim of this study was to investigate whether blocking functional endothelin converting enzyme ( ECE ) activity may offer a new approach to inhibit the development of cerebral vasopasm after subarachnoid hemorrhage ( SAH ) by preventing transformation of big Endothelin 1 ( big ET 1 ) to vasoactive Endothelin 1 ( ET 1 ) . ^^^ METHODS : In vitro , the effect of potential ECE inhibitors was determined by measurement of isometric contractions , induced by big ET 1 , in isolated rat basilar arteries . ^^^ Endothelium intact ( E+ ) and de endothelialized ( E ) segments were examined after pre incubated with the putative ECE inhibitors : Phosphoramidon ( 10 ( 4 ) M ) , Captopril ( 10 ( 3 ) M and 10 ( 4 ) M ) and [ ( 22 ) D Val ] big ET 1 ( 16 38 ) ( 10 ( 5 ) M and 10 ( 6 ) M ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The biosynthesis of ET 1 is a multi step process , involving the conversion of the relatively inactive precursor big ET 1 to the mature peptide by endothelin converting enzyme ( ECE ) , a metalloprotease . ^^^ Consequently , ECE inhibitors are expected to suppress the biosynthesis of ET 1 and reduce the pathologic impact resulting from overproduction of this peptide . ^^^ The purpose of the present study was to investigate the effects of an ECE inhibitor , CGS 26303 , on hemolysate induced injury of cerebral vessel endothelial cells as well as the production of ET 1 from these cells . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The formation of angiotensin 2 ( ATII ) or endothelin 1 ( ET 1 ) was blocked using inhibitors of angiotensin converting enzyme ( ACE ) and endothelin converting enzyme ( ECE ) , respectively . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The endothelin converting enzyme ( ECE ) is the main enzyme responsible for the genesis of the potent pressor peptide endothelin 1 ( ET 1 ) . ^^^ It is suggested that the ECE is pivotal in the genesis of ET 1 , considering that the knockout of both genes generates the same lethal developments during the embryonic stage . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The aim of this study was to investigate whether the blocking of endothelin converting enzyme ( ECE ) activity offers a new approach to inhibiting the development of cerebral vasospasm after subarachnoid hemorrhage ( SAH ) by preventing transformation of big endothelin 1 ( big ET 1 ) to vasoactive endothelin 1 ( ET 1 ) . ^^^ The effect of potential ECE inhibitors was determined in vitro by measurement of isometric contractions , induced by big ET 1 , in isolated rat basilar arteries . ^^^ Intact and de endothelialized endothelium ( E+ and E , respectively ) segments were examined after preincubation with the putative ECE inhibitors : phosphoramidon ( 10 ( 4 ) M ) , and [ 22D Val ] big ET 1 [ 16 38 ] ( 10 ( 5 ) M and 10 ( 6 ) M ) . ^^^ These results demonstrate that [ D Val 22 ] big ET 1 [ 16 38 ] has a potent ECE inhibitory effect , preventing cerebral vasospasm in rabbit basilar artery by inhibiting the transformation of big ET 1 to vasoactive ET 1 after intracisternal application in vivo , whereas no inhibitory effect was detectable in rat basilar artery in vitro . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Therefore , we investigated the regulation of proteins of the endothelin system ( ppET 1 , ECE and ETA R and ETB R ) in the hearts of female spontaneously hypertensive rats ( SHR ) with respect to E 2 . ( 2 ) Relative expression levels of the respective cardiac mRNA obtained from sham operated , ovariectomized and ovariectomized E 2 substituted SHR were quantified by real time PCR . ^^^ Ovariectomy led to a significant upregulation of the ETB R mRNA ( 2 . 6+ / 0 . 8 fold ) in the left ventricular myocardium , which was not attendant with an alteration of ETA R , ECE and ppET 1 mRNA expression . ( 3 ) An upregulation of the relative expression level of ETB R protein due to ovariectomy was also demonstrated by radioligand binding assay . ( 4 ) Upregulation of both ETB R mRNA and ETB R protein expression was completely inhibited by E 2 replacement . ( 5 ) To confirm these results in in vitro experiments , we quantified the mRNA of ET R subtypes from isolated cardiomyocytes in the presence and absence of E 2 ( 10 8 m , 24 h ) . ^^^ ETB R downregulation was not attendant with the alteration of ETA R , ECE and ppET 1 mRNA expression . ( 6 ) Taken together , these data demonstrate that estrogen regulates the expression of ETB R in rat ventricular myocardium in vivo and in vitro . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Female Spragure Dawly rats were randomly divided into three groups : sham operated group ( sham ) , ovariectomized group ( OVX ) and 17beta estradiol replacement group ( OVX + E 2 , 20 microg ( 1 ) . kg . d ( 1 ) , s . c . ) . 4 weeks after operation , the plasma concentration of ET 1 , clearance of ET 1 , functional ECE activity and preproET 1 mRNA expression in aorta were measured . ^^^ The present study have shown that estrogen down regulates plasma ET 1 levels by inhibiting the preproET 1 mRNA expression and functional ECE activity . ^^^ Inhibition of ET 1 production mediated by modulating ECE activity may be one of the novel mechanisms of the protective of estrogens on the cardiovascular system . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Only after the results of clinical testing of selective ET receptor antagonists or ECE inhibitors in asthma are available will we know definitively whether ET 1 has fulfilled its promise as a significant player in lung pathophysiology . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET 1 is produced from its precursor Big ET 1 ( 38 amino acids ) by endothelin converting enzyme ( ECE ) . ^^^ Although ET 1 and its receptors have been identified in the retina , little is known of the distribution of ECE at the optic nerve . ^^^ Unlike the PM ECE , cytosolic Big ET 1 converting activities were activated by acidification ( pH 6 . 4 ) , suggesting the involvement of ECE 2 like activity and / or cathepsin activity . ^^^ Pepstatin , a potent inhibitor of cathepsins , inhibited the optic nerve ( ON ) cytosolic conversion of Big ET 1 peptide by 50 % , and the combination of pepstatin and phosphoramidon , a potent inhibitor of ECE , inhibited the ON cytosolic activity by 86 % . ^^^ In summary , it appears that ET 1 could be produced in the retina and optic nerve by at least two ECE subtypes and , perhaps , cathepsins . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin 1 1 31 ( ET 1 1 31 ) , a novel member of the endothelin family comprising 31 amino acids and derived from the selective hydrolysis of big ET 1 by chymase , directly activates endothelin receptors or converts to ET 1 1 21 by ET converting enzyme ( ECE ) . ^^^ Endothelin 1 1 31 ( ET 1 1 31 ) , a novel member of the endothelin family comprising 31 amino acids and derived from the selective hydrolysis of big ET 1 by chymase , directly activates endothelin receptors or converts to ET 1 1 21 by ET converting enzyme ( ECE ) . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Frozen sections were stained with antibodies against ECE , ET 1 , ETA and ETB receptors , SMC , macrophages and endothelial cells . ^^^ RESULTS : At the early stage , less than 3 months after PCI , neointimal SMC were positive for ECE , ET 1 , ETA and ETB receptors . ^^^ The expression of ECE , ET 1 , ETA and ETB receptors in these neointimal SMC decreased markedly from 6 months onwards . ^^^ The ECE , ET 1 , ETA and ETB receptor positive cell areas were significantly ( P < 0 . 005 ) greater in the first 3 months after PCI compared with 6 months or more after PCI . ^^^ CONCLUSIONS : These observations strongly suggest that the expression of ECE , ET 1 , ETA and ETB receptors is enhanced in neointimal SMC at early stages after PCI injury in human coronary arteries . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Through the inhibition of ACE and ECE , it blocks the conversion of angiotensin 1 ( AI ) and big endothelin 1 ( big ET 1 ) into the two most potent peptidic vasoconstrictors , angiotensin 2 ( AII ) and ET 1 , respectively . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Additionally , by measuring the production of ET 1 ( 1 31 ) , we showed that a chymase like enzyme is involved in this process when ECE and NEP are inhibited by phosphoramidon . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET 1 is produced from its precursor , Big ET 1 , by endothelin converting enzyme ( ECE ) . ^^^ Pepstatin , a potent inhibitor of cathepsins , and phosphoramidon , a potent inhibitor of ECE , inhibited the cytosolic conversion of Big ET 1 peptide by 46 % and 35 % , respectively , whereas the combination of both inhibited the cytosolic activity by 93 % . ^^^ In summary , ET 1 production in RPE is regulated by at least two isoforms of ECE , ( cytosolic and PM ) as well as cathepsins . . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme ( ECE ) is a key enzyme in the process of ET 1 generation . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
Endothelin converting enzyme ( ECE ) 1 is a membrane bound metalloprotease responsible for production of vasoactive endothelin ( ET ) 1 from inactive big ET 1 . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
ET 1 is generated from big ET 1 by endothelin converting enzyme ( ECE ) 1 , which has four recognized isoforms , ECE 1a , ECE 1b , ECE 1c , and ECE 1d , differing only in their amino terminal regions . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
The brains of female C57BL / 6 mice with PbA infection were examined at Day 5 for the expression of ET 1 , endothelin converting enzyme ( ECE ) , and the endothelin receptors A and B ( ET ( A ) and ET ( B ) ) by both reverse transcription polymerase chain reaction ( RT PCR ) and quantitative real time PCR . ^^^ ET 1 and ECE mRNA expression was markedly increased by RT PCR in PbA infected mice . ^^^ |
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Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|
Interacting proteins: P42892 and P05305 |
Pubmed |
SVM Score :0.0 |
NA |
|