| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Various combinations of GR 1 , GR 2 , AF 1 , and AF 2 were fused to the chloramphenicol acetyltransferase ( CAT ) reporter gene and cotransfected with a glucocorticoid receptor expression plasmid ( pSVGR 1 ) into H4IIE cells to identify the functional GRU . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| The response unit spans a 100 bp segment and includes two glucocorticoid receptor binding sites ( GR 1 and GR 2 ) and two accessory factor binding sites ( AF 1 and AF 2 ) , all of which are required for a maximal glucocorticoid response . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| The glucocorticoid response is mediated by a complex regulatory unit that consists of two glucocorticoid receptor ( GR ) binding sites ( GR 1 and GR 2 ) and two adjacent accessory factor elements ( AF 1 and AF 2 ) . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| We show that a full response to glucocorticoids requires two DNA segments : 1 ) a glucocorticoid response unit ( GRU ) , centered at about position 400 , which contains two accessory factor elements ( AF 1 and AF 2 ) and two glucocorticoid receptor binding sites ( GR 1 and GR 2 ) , and 2 ) a basal promoter / cyclic AMP response element ( E / CRE ) at about position 90 , which binds the transcription factor CREB . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| The transactivation function AF 1 in the N terminal half of GR is required for ligand dependent induction and acts constitutively in truncated GR lacking the ligand binding domain . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| The glucocorticoid response is mediated by a complex glucocorticoid response unit that consists of two glucocorticoid receptor ( GR ) binding sites ( GR 1 and GR 2 ) and two accessory factor binding sites ( AF 1 and AF 2 ) . ^^^ These are : AF 1 ( hepatic nuclear factor 4 / chicken ovalbumin upstream promoter transcription factor ) , AF 2 ( HNF 3 ) , GR 1 ( GR ) , and GR 2 ( GR ) . . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| The phosphoenolpyruvate carboxykinase ( PEPCK ) gene promoter contains a glucocorticoid response unit ( GRU ) that includes , as a linear array , two accessory factor binding sites ( AF 1 and AF 2 ) and two glucocorticoid receptor binding sites . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Experiments with glucocorticoid receptor truncation and point mutants indicated that GRIP 1 interacted with and enhanced the activity of the C terminal AF 2 but not the N terminal AF 1 transactivation domain of the glucocorticoid receptor . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Deletion of the ligand binding domain of the glucocorticoid receptor does not impede cooperation with Stat 5 , whereas deletion of the AF 1 transactivation domain does prevent cooperation . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Glucocorticoids induce PEPCK gene transcription through a complex glucocorticoid response unit that consists of , from 5 ' to 3 ' , accessory factor elements AF 1 and AF 2 ; two noncanonical glucocorticoid receptor binding sites , GR 1 and GR 2 ; a third accessory factor element , AF 3 ; and a cAMP response element , CRE . ^^^ AF 2 is still needed for a maximal glucocorticoid response when GR 1 is converted to a high affinity GR binding element , but AF 1 and AF 3 are not required . . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| The phosphoenolpyruvate carboxykinase ( PEPCK ) gene promoter contains a glucocorticoid response unit ( GRU ) that includes three accessory factor binding sites ( AF 1 , AF 2 , and AF 3 ) , two glucocorticoid receptor binding sites ( GR 1 and GR 2 ) , and a cAMP response element . ^^^ By contrast , the distance and orientation requirements of AF 1 and AF 3 with respect to GR 1 are more flexible . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| The GRU is comprised of two glucocorticoid receptor ( GR ) binding sites ( GR 1 and GR 2 ) and four accessory factor binding sites [ AF 1 , AF 2 , AF 3 , and cAMP response element ( CRE ) ] that bind distinct transcription factors . ^^^ These results suggest that the regulation of the PEPCK gene by glucocorticoids requires specific interactions between GR , accessory factors , and coactivators , and that the transactivation domains of AF 1 and AF 2 are of fundamental importance in the assembly of this multiprotein complex . . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| GR mutants and ligands that disrupt individual transcriptional activation functions ( activation function 1 [ AF 1 ] and AF 2 ) or receptor dimerization fail to fully inhibit cellular proliferation and , remarkably , discriminate between the targets of GR ' s cytostatic action , the cyclin dependent kinase inhibitors p 21 ( Cip 1 ) and p 27 ( Kip 1 ) . ^^^ Induction of p 21 ( Cip 1 ) is agonist dependent and requires AF 2 but not AF 1 or GR dimerization . ^^^ In contrast , induction of p 27 ( Kip 1 ) is agonist independent , does not require AF 2 or AF 1 , but depends on GR dimerization . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Here we report that the C terminal region of p 160 coactivators glucocorticoid receptor interacting protein 1 ( GRIP 1 ) , steroid receptor coactivator 1 ( SRC 1a ) , and SRC 1e binds the N terminal AF 1 activation function of the androgen receptor ( AR ) , and p 160 coactivators can thereby enhance transcriptional activation by AR . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Differential regulation of glucocorticoid receptor transcriptional activation via AF 1 associated proteins . ^^^ The hormone activated glucocorticoid receptor ( GR ) , through its N and C terminal transcriptional activation functions AF 1 and AF 2 , controls the transcription of target genes presumably through interaction ( s ) with transcriptional regulatory factors . ^^^ Utilizing a modified yeast two hybrid approach , we have identified the tumor susceptibility gene 101 ( TSG 101 ) and the vitamin D receptor interacting protein 150 ( DRIP 150 ) as proteins that interact specifically with a functional GR AF 1 surface . ^^^ In yeast and mammalian cells , TSG 101 represses whereas DRIP 150 enhances GR AF 1 mediated transactivation . ^^^ Thus , GR AF 1 is capable of recruiting both positive and negative regulatory factors that differentially regulate GR transcriptional enhancement . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Estrogen responses at AP 1 sites require the integrity of the ERalpha AF 1 and AF 2 activation surfaces and the complementary surfaces on the p 160 coactivator GRIP 1 ( glucocorticoid receptor interacting protein 1 ) , the NID / AF 1 region , and NR boxes . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Src potentiates activation functions in CREB binding protein ( CBP ) and glucocorticoid receptor interacting protein 1 ( GRIP 1 ) , and we discuss the possibility that the Src / JNK pathway enhances the activity of these coactivators , which are known to mediate AF 1 action . . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| The glucocorticoid receptor ( GR ) contains several activation domains , tau 1 ( AF 1 ) , tau 2 , and AF 2 , which were initially defined using transiently transfected reporter constructs . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| This protein , named ANT 1 ( AR N terminal domain transactivating protein 1 ) , enhanced the ligand independent autonomous AF 1 transactivation function of AR or glucocorticoid receptor but did not enhance that of estrogen receptor alpha . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| The mutant GR through its intact AF 1 domain bound to a p 160 coactivator , but failed to do so through its AF 2 domain . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| In contrast , the repression by mutant GR depended on the intact AF 1 site in the gene promoter , whereby mutation of the AF 1 element abolished the repression . . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Partial deletions in the ligand binding domain ( LBD ) , including the tau 2 and tauc regions , greatly reduced or eliminated GR repression , whereas deletion of the N terminal AF 1 ( tau 1 ) domain and substitution mutations in the DNA binding domain had little or no effect . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| A mutation ( C644G ) in the ligand binding domain ( LBD ) of the mouse GR has provided information regarding the steps required in the derepression / activation process and in the functional significance of the two major transcriptional activation domains , AF 1 and AF 2 . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Glucocorticoid receptor containing a mutation in the carboxy terminal transcriptional activation domain , AF 2 , retained elevated basal activity , while mutation of the amino terminal transactivation domain , AF 1 , eliminated the elevated basal activity observed in ydj 1 mutant strains . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Androgen receptor ( AR ) , as well as glucocorticoid receptor ( GR ) , is unique since most , if not all , of its activities are mediated via the constitutive activity of the activation function 1 ( AF 1 ) function . ^^^ We herein report the isolation of ANT 1 ( AR N terminal domain ( NTD ) transactivating protein 1 ) enhancing autonomous AF 1 transactivation function of AR or GR , but not of estrogen receptor alpha ( ERalpha ) . ^^^ Our results suggest that ANT 1 may play a key role in the molecular interaction between two spatially distinct subnuclear compartments in a receptor specific fashion , and thereby induce the strong autonomous transactivation functions either of AR or GR AF 1 . . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| We found that GR targets differed in their requirements for AF 1 or AF 2 , and that the dimer interface was dispensable for activation of some genes in each class . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Data from `` domain swap ' ' experiments using GR chimeras indicated that the main target of the p 38 mediated ( but not JNK mediated ) inhibition is the ligand binding domain of GR ( spanning amino acids 525 795 ) , whereas the constitutively active N terminal AF 1 region ( spanning amino acids 106 237 ) is dispensable for the inhibitory effect of p 38 . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| We found that hGRbeta suppressed the transcriptional activity of both activation function ( AF ) 1 and AF 2 of hGRalpha , indicating that hGRbeta may exert its dominant negative effect by affecting the function of coactivators that are attracted to these transactivation domains . hGRbeta bound to one of the p 160 coactivators , the glucocorticoid receptor interacting protein 1 ( GRIP 1 ) via its preserved AF 1 but not via its defective AF 2 in vitro . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Over expression of a wild type GR restores glucocorticoid regulation of TAT 3 luciferase , and this is enhanced when the activation function ( AF ) 2 domain is deleted but much reduced when the AF 1 domain is deleted . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| TATA box binding protein induces structure in the recombinant glucocorticoid receptor AF 1 domain . ^^^ Expressed independently as a recombinant peptide , the N terminal transactivation domain ( AF 1 ) of the GR shows little structure and appears to exist as a collection of random coil configurations . ^^^ The GR AF 1 is known to interact with other transcription factors , including a critical component of the general transcription machinery proteins , the TATA box binding protein ( TBP ) . ^^^ We tested whether this interaction can lead to acquisition of structure in the GR AF 1 . ^^^ Our results show that recombinant GR AF 1 acquires a significant amount of helical content when it interacts with TBP . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| We now examine the role of the N terminal half of the glucocorticoid receptor ( GR ) including the activation domain ( AF 1 ) , the DNA binding site sequence , receptor contact with DNA , and coactivator binding on the expression of partial agonist activity in two cell lines for GRs bound by five antiglucocorticoids : dexamethasone mesylate ( Dex Mes ) , dexamethasone oxetanone ( Dex Ox ) , progesterone ( Prog ) , deoxycorticosterone ( DOC ) , and RU 486 . ^^^ Using truncated GRs , we find that the N terminal half of GR and the AF 1 domain are dispensable for the partial agonist activity of antiglucocorticoids . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Several studies have shown that AF 1 region is mostly unstructured and that it can acquire folded functional conformation under certain potentially physiological conditions , namely in the presence of osmolytes , when the GR DBD is bound to glucocorticoid response element ( GRE ) , and when AF 1 binds other transcription factor proteins . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| Finally , in glutathione S transferase pull down assays , hGRalphaG679S interacted with the glucocorticoid receptor interacting protein 1 coactivator in vitro only through its activation function ( AF ) 1 , unlike the hGRalphaR477H and hGRalpha , which interacted with the glucocorticoid receptor interacting protein 1 through both their AF 1 and AF 2 . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| TBP binds recombinant GR activation function 1 ( AF 1 ) with a 1 : 2 stoichiometry and a dissociation constant in the nanomolar range . ^^^ In vivo fluorescence resonance energy transfer experiments , using fluorescently labeled TBP and various GR constructs , transiently transfected into CV 1 cells , show GR TBP interactions , dependent on AF 1 . ^^^ |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|
| Interacting proteins: P38484 and P04150 |
Pubmed |
SVM Score :0.0 |
| NA |
|