3rut - Revision history

OCA at 09:45, 1 March 2024

OCA — Fri, 01 Mar 2024 09:45:25 GMT

←Older revision		Revision as of 09:45, 1 March 2024
Line 3:		Line 3:
	<StructureSection load='3rut' size='340' side='right'caption='[[3rut]], [[Resolution\|resolution]] 3.00Å' scene=''>		<StructureSection load='3rut' size='340' side='right'caption='[[3rut]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3rut]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RUT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RUT FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3rut]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RUT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RUT FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=59G:6-(4-{[3-(2,6-DICHLOROPHENYL)-5-(PROPAN-2-YL)-1,2-OXAZOL-4-YL]METHOXY}PHENYL)-1-BENZOTHIOPHENE-3-CARBOXYLIC+ACID'>59G</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene~~></td></tr>~~	+	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution\|Resolution]] 3Å</td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3ruu\|3ruu]], [[3rvf\|3rvf]]</div></td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=59G:6-(4-{[3-(2,6-DICHLOROPHENYL)-5-(PROPAN-2-YL)-1,2-OXAZOL-4-YL]METHOXY}PHENYL)-1-BENZOTHIOPHENE-3-CARBOXYLIC+ACID'>59G</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BAR, FXR, HRR1, NR1H4, RIP14 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>	+
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span></td></tr>	+
	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3rut FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rut OCA], [https://pdbe.org/3rut PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rut RCSB], [https://www.ebi.ac.uk/pdbsum/3rut PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rut ProSAT]</span></td></tr>		<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3rut FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rut OCA], [https://pdbe.org/3rut PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rut RCSB], [https://www.ebi.ac.uk/pdbsum/3rut PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rut ProSAT]</span></td></tr>
	</table>		</table>
-	== Disease ==
-	[[https://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Note=A chromosomal aberration involving NCOA1 is a cause of rhabdomyosarcoma. Translocation t(2;2)(q35;p23) with PAX3 generates the NCOA1-PAX3 oncogene consisting of the N-terminus part of PAX3 and the C-terminus part of NCOA1. The fusion protein acts as a transcriptional activator. Rhabdomyosarcoma is the most common soft tissue carcinoma in childhood, representing 5-8% of all malignancies in children.
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/NR1H4_HUMAN NR1H4_HUMAN]] Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxylase gene (CYP7A1) through the induction of NR0B2 or FGF19 expression, via two distinct mechanisms. Activates the intestinal bile acid-binding protein (IBABP). Activates the transcription of bile salt export pump ABCB11 by directly recruiting histone methyltransferase CARM1 to this locus.<ref>PMID:10334992</ref> <ref>PMID:10334993</ref> <ref>PMID:12815072</ref> <ref>PMID:15471871</ref> <ref>PMID:12718892</ref> <ref>PMID:18621523</ref> <ref>PMID:19410460</ref> <ref>PMID:19586769</ref> [[https://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Nuclear receptor coactivator that directly binds nuclear receptors and stimulates the transcriptional activities in a hormone-dependent fashion. Involved in the coactivation of different nuclear receptors, such as for steroids (PGR, GR and ER), retinoids (RXRs), thyroid hormone (TRs) and prostanoids (PPARs). Also involved in coactivation mediated by STAT3, STAT5A, STAT5B and STAT6 transcription factors. Displays histone acetyltransferase activity toward H3 and H4; the relevance of such activity remains however unclear. Plays a central role in creating multisubunit coactivator complexes that act via remodeling of chromatin, and possibly acts by participating in both chromatin remodeling and recruitment of general transcription factors. Required with NCOA2 to control energy balance between white and brown adipose tissues. Required for mediating steroid hormone response. Isoform 2 has a higher thyroid hormone-dependent transactivation activity than isoform 1 and isoform 3.<ref>PMID:9427757</ref> <ref>PMID:7481822</ref> <ref>PMID:9223431</ref> <ref>PMID:9296499</ref> <ref>PMID:9223281</ref> <ref>PMID:10449719</ref> <ref>PMID:12954634</ref>	+	[https://www.uniprot.org/uniprot/NR1H4_HUMAN NR1H4_HUMAN] Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxylase gene (CYP7A1) through the induction of NR0B2 or FGF19 expression, via two distinct mechanisms. Activates the intestinal bile acid-binding protein (IBABP). Activates the transcription of bile salt export pump ABCB11 by directly recruiting histone methyltransferase CARM1 to this locus.<ref>PMID:10334992</ref> <ref>PMID:10334993</ref> <ref>PMID:12815072</ref> <ref>PMID:15471871</ref> <ref>PMID:12718892</ref> <ref>PMID:18621523</ref> <ref>PMID:19410460</ref> <ref>PMID:19586769</ref>
-	~~<div style="background-color:#fffaf0;">~~	+
-	~~== Publication Abstract from PubMed ==~~	+
-	To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene 1f and the indole 1g display the optimal orientation of the carboxylate for enhanced FXR agonist potency.	+
-		+
-	Conformationally constrained farnesoid X receptor (FXR) agonists: Alternative replacements of the stilbene.,Akwabi-Ameyaw A, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, Miller AB, Navas F 3rd, Parks DJ, Spearing PK, Todd D, Williams SP, Wisely GB Bioorg Med Chem Lett. 2011 Aug 11. PMID:21890356<ref>PMID:21890356</ref>	+
-		+
-	~~From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~	+
-	~~</div>~~	+
-	~~<div class="pdbe-citations 3rut" style="background-color:#fffaf0;"></div~~>	+

	==See Also==		==See Also==
Line 30:		Line 17:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Histone acetyltransferase]]~~	+	[[Category: Homo sapiens]]
-	~~[[Category: Human~~]]	+
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Madauss~~, K P~~]]	+	[[Category: Madauss KP]]
-	[[Category: Williams~~, S P]]~~	+	[[Category: Williams SP]]
-	~~[[Category: Alpha-helical sandwich]]~~	+
-	~~[[Category: Bile acid]]~~	+
-	~~[[Category: Farnesoid]]~~	+
-	~~[[Category: Nuclear receptor]]~~	+
-	~~[[Category: Rxr]]~~	+
-	~~[[Category: Transcription co-factor]]~~	+
-	~~[[Category: Transcription factor]]~~	+
-	~~[[Category: Transcription regulator~~]]	+

OCA at 10:26, 22 June 2022

OCA — Wed, 22 Jun 2022 10:26:07 GMT

←Older revision		Revision as of 10:26, 22 June 2022
Line 1:		Line 1:

	==FXR with SRC1 and GSK359==		==FXR with SRC1 and GSK359==
-	<StructureSection load='3rut' size='340' side='right' caption='[[3rut]], [[Resolution\|resolution]] 3.00Å' scene=''>	+	<StructureSection load='3rut' size='340' side='right'caption='[[3rut]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3rut]] is a 2 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RUT OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3RUT FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3rut]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RUT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RUT FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=59G:6-(4-{[3-(2,6-DICHLOROPHENYL)-5-(PROPAN-2-YL)-1,2-OXAZOL-4-YL]METHOXY}PHENYL)-1-BENZOTHIOPHENE-3-CARBOXYLIC+ACID'>59G</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=59G:6-(4-{[3-(2,6-DICHLOROPHENYL)-5-(PROPAN-2-YL)-1,2-OXAZOL-4-YL]METHOXY}PHENYL)-1-BENZOTHIOPHENE-3-CARBOXYLIC+ACID'>59G</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3ruu\|3ruu]], [[3rvf\|3rvf]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3ruu\|3ruu]], [[3rvf\|3rvf]]</div></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BAR, FXR, HRR1, NR1H4, RIP14 ([~~http~~://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BAR, FXR, HRR1, NR1H4, RIP14 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [~~http~~://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span></td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3rut FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rut OCA], [~~http~~://pdbe.org/3rut PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3rut RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3rut PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=3rut ProSAT]</span></td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3rut FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rut OCA], [https://pdbe.org/3rut PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rut RCSB], [https://www.ebi.ac.uk/pdbsum/3rut PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rut ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
-	[[~~http~~://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Note=A chromosomal aberration involving NCOA1 is a cause of rhabdomyosarcoma. Translocation t(2;2)(q35;p23) with PAX3 generates the NCOA1-PAX3 oncogene consisting of the N-terminus part of PAX3 and the C-terminus part of NCOA1. The fusion protein acts as a transcriptional activator. Rhabdomyosarcoma is the most common soft tissue carcinoma in childhood, representing 5-8% of all malignancies in children.	+	[[https://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Note=A chromosomal aberration involving NCOA1 is a cause of rhabdomyosarcoma. Translocation t(2;2)(q35;p23) with PAX3 generates the NCOA1-PAX3 oncogene consisting of the N-terminus part of PAX3 and the C-terminus part of NCOA1. The fusion protein acts as a transcriptional activator. Rhabdomyosarcoma is the most common soft tissue carcinoma in childhood, representing 5-8% of all malignancies in children.
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/NR1H4_HUMAN NR1H4_HUMAN]] Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxylase gene (CYP7A1) through the induction of NR0B2 or FGF19 expression, via two distinct mechanisms. Activates the intestinal bile acid-binding protein (IBABP). Activates the transcription of bile salt export pump ABCB11 by directly recruiting histone methyltransferase CARM1 to this locus.<ref>PMID:10334992</ref> <ref>PMID:10334993</ref> <ref>PMID:12815072</ref> <ref>PMID:15471871</ref> <ref>PMID:12718892</ref> <ref>PMID:18621523</ref> <ref>PMID:19410460</ref> <ref>PMID:19586769</ref> [[~~http~~://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Nuclear receptor coactivator that directly binds nuclear receptors and stimulates the transcriptional activities in a hormone-dependent fashion. Involved in the coactivation of different nuclear receptors, such as for steroids (PGR, GR and ER), retinoids (RXRs), thyroid hormone (TRs) and prostanoids (PPARs). Also involved in coactivation mediated by STAT3, STAT5A, STAT5B and STAT6 transcription factors. Displays histone acetyltransferase activity toward H3 and H4; the relevance of such activity remains however unclear. Plays a central role in creating multisubunit coactivator complexes that act via remodeling of chromatin, and possibly acts by participating in both chromatin remodeling and recruitment of general transcription factors. Required with NCOA2 to control energy balance between white and brown adipose tissues. Required for mediating steroid hormone response. Isoform 2 has a higher thyroid hormone-dependent transactivation activity than isoform 1 and isoform 3.<ref>PMID:9427757</ref> <ref>PMID:7481822</ref> <ref>PMID:9223431</ref> <ref>PMID:9296499</ref> <ref>PMID:9223281</ref> <ref>PMID:10449719</ref> <ref>PMID:12954634</ref>	+	[[https://www.uniprot.org/uniprot/NR1H4_HUMAN NR1H4_HUMAN]] Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxylase gene (CYP7A1) through the induction of NR0B2 or FGF19 expression, via two distinct mechanisms. Activates the intestinal bile acid-binding protein (IBABP). Activates the transcription of bile salt export pump ABCB11 by directly recruiting histone methyltransferase CARM1 to this locus.<ref>PMID:10334992</ref> <ref>PMID:10334993</ref> <ref>PMID:12815072</ref> <ref>PMID:15471871</ref> <ref>PMID:12718892</ref> <ref>PMID:18621523</ref> <ref>PMID:19410460</ref> <ref>PMID:19586769</ref> [[https://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Nuclear receptor coactivator that directly binds nuclear receptors and stimulates the transcriptional activities in a hormone-dependent fashion. Involved in the coactivation of different nuclear receptors, such as for steroids (PGR, GR and ER), retinoids (RXRs), thyroid hormone (TRs) and prostanoids (PPARs). Also involved in coactivation mediated by STAT3, STAT5A, STAT5B and STAT6 transcription factors. Displays histone acetyltransferase activity toward H3 and H4; the relevance of such activity remains however unclear. Plays a central role in creating multisubunit coactivator complexes that act via remodeling of chromatin, and possibly acts by participating in both chromatin remodeling and recruitment of general transcription factors. Required with NCOA2 to control energy balance between white and brown adipose tissues. Required for mediating steroid hormone response. Isoform 2 has a higher thyroid hormone-dependent transactivation activity than isoform 1 and isoform 3.<ref>PMID:9427757</ref> <ref>PMID:7481822</ref> <ref>PMID:9223431</ref> <ref>PMID:9296499</ref> <ref>PMID:9223281</ref> <ref>PMID:10449719</ref> <ref>PMID:12954634</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 23:		Line 23:
	</div>		</div>
	<div class="pdbe-citations 3rut" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 3rut" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Bile acid receptor 3D structures\|Bile acid receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 29:		Line 32:
	[[Category: Histone acetyltransferase]]		[[Category: Histone acetyltransferase]]
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Madauss, K P]]		[[Category: Madauss, K P]]
	[[Category: Williams, S P]]		[[Category: Williams, S P]]

OCA at 09:30, 8 November 2017

OCA — Wed, 08 Nov 2017 09:30:27 GMT

←Older revision		Revision as of 09:30, 8 November 2017
Line 23:		Line 23:
	</div>		</div>
	<div class="pdbe-citations 3rut" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 3rut" style="background-color:#fffaf0;"></div>
-
-	==See Also==
-	*[[Bile acid receptor\|Bile acid receptor]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 23:18, 5 August 2016

OCA — Fri, 05 Aug 2016 23:18:53 GMT

←Older revision		Revision as of 23:18, 5 August 2016
Line 1:		Line 1:
		+
	==FXR with SRC1 and GSK359==		==FXR with SRC1 and GSK359==
	<StructureSection load='3rut' size='340' side='right' caption='[[3rut]], [[Resolution\|resolution]] 3.00Å' scene=''>		<StructureSection load='3rut' size='340' side='right' caption='[[3rut]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3rut]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Homo_sapiens Homo sapiens~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RUT OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RUT FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3rut]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RUT OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RUT FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=59G:6-(4-{[3-(2,6-DICHLOROPHENYL)-5-(PROPAN-2-YL)-1,2-OXAZOL-4-YL]METHOXY}PHENYL)-1-BENZOTHIOPHENE-3-CARBOXYLIC+ACID'>59G</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=59G:6-(4-{[3-(2,6-DICHLOROPHENYL)-5-(PROPAN-2-YL)-1,2-OXAZOL-4-YL]METHOXY}PHENYL)-1-BENZOTHIOPHENE-3-CARBOXYLIC+ACID'>59G</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3ruu\|3ruu]], [[3rvf\|3rvf]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3ruu\|3ruu]], [[3rvf\|3rvf]]</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BAR, FXR, HRR1, NR1H4, RIP14 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 ~~Homo sapiens~~])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BAR, FXR, HRR1, NR1H4, RIP14 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span></td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3rut FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rut OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rut RCSB], [http://www.ebi.ac.uk/pdbsum/3rut PDBsum]</span></td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3rut FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rut OCA], [http://pdbe.org/3rut PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3rut RCSB], [http://www.ebi.ac.uk/pdbsum/3rut PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3rut ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
Line 21:		Line 22:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
		+	<div class="pdbe-citations 3rut" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 29:		Line 31:
	</StructureSection>		</StructureSection>
	[[Category: Histone acetyltransferase]]		[[Category: Histone acetyltransferase]]
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Madauss, K P]]		[[Category: Madauss, K P]]
	[[Category: Williams, S P]]		[[Category: Williams, S P]]

OCA at 11:01, 19 December 2014

OCA — Fri, 19 Dec 2014 11:01:50 GMT

←Older revision		Revision as of 11:01, 19 December 2014
Line 1:		Line 1:
-	~~{{STRUCTURE_3rut~~\| ~~PDB~~=3rut \| ~~SCENE~~= }}	+	==FXR with SRC1 and GSK359==
-	===FXR ~~with SRC1 and GSK359~~===	+	<StructureSection load='3rut' size='340' side='right' caption='[[3rut]], [[Resolution\|resolution]] 3.00Å' scene=''>
-	~~{{ABSTRACT_PUBMED_21890356}}~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[3rut]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RUT OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RUT FirstGlance]. <br>
-	==Disease==	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=59G:6-(4-{[3-(2,6-DICHLOROPHENYL)-5-(PROPAN-2-YL)-1,2-OXAZOL-4-YL]METHOXY}PHENYL)-1-BENZOTHIOPHENE-3-CARBOXYLIC+ACID'>59G</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3ruu\|3ruu]], [[3rvf\|3rvf]]</td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BAR, FXR, HRR1, NR1H4, RIP14 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span></td></tr>
		+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3rut FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rut OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rut RCSB], [http://www.ebi.ac.uk/pdbsum/3rut PDBsum]</span></td></tr>
		+	</table>
		+	== Disease ==
	[[http://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Note=A chromosomal aberration involving NCOA1 is a cause of rhabdomyosarcoma. Translocation t(2;2)(q35;p23) with PAX3 generates the NCOA1-PAX3 oncogene consisting of the N-terminus part of PAX3 and the C-terminus part of NCOA1. The fusion protein acts as a transcriptional activator. Rhabdomyosarcoma is the most common soft tissue carcinoma in childhood, representing 5-8% of all malignancies in children.		[[http://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Note=A chromosomal aberration involving NCOA1 is a cause of rhabdomyosarcoma. Translocation t(2;2)(q35;p23) with PAX3 generates the NCOA1-PAX3 oncogene consisting of the N-terminus part of PAX3 and the C-terminus part of NCOA1. The fusion protein acts as a transcriptional activator. Rhabdomyosarcoma is the most common soft tissue carcinoma in childhood, representing 5-8% of all malignancies in children.
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/NR1H4_HUMAN NR1H4_HUMAN]] Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxylase gene (CYP7A1) through the induction of NR0B2 or FGF19 expression, via two distinct mechanisms. Activates the intestinal bile acid-binding protein (IBABP). Activates the transcription of bile salt export pump ABCB11 by directly recruiting histone methyltransferase CARM1 to this locus.<ref>PMID:10334992</ref> <ref>PMID:10334993</ref> <ref>PMID:12815072</ref> <ref>PMID:15471871</ref> <ref>PMID:12718892</ref> <ref>PMID:18621523</ref> <ref>PMID:19410460</ref> <ref>PMID:19586769</ref> [[http://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Nuclear receptor coactivator that directly binds nuclear receptors and stimulates the transcriptional activities in a hormone-dependent fashion. Involved in the coactivation of different nuclear receptors, such as for steroids (PGR, GR and ER), retinoids (RXRs), thyroid hormone (TRs) and prostanoids (PPARs). Also involved in coactivation mediated by STAT3, STAT5A, STAT5B and STAT6 transcription factors. Displays histone acetyltransferase activity toward H3 and H4; the relevance of such activity remains however unclear. Plays a central role in creating multisubunit coactivator complexes that act via remodeling of chromatin, and possibly acts by participating in both chromatin remodeling and recruitment of general transcription factors. Required with NCOA2 to control energy balance between white and brown adipose tissues. Required for mediating steroid hormone response. Isoform 2 has a higher thyroid hormone-dependent transactivation activity than isoform 1 and isoform 3.<ref>PMID:9427757</ref> <ref>PMID:7481822</ref> <ref>PMID:9223431</ref> <ref>PMID:9296499</ref> <ref>PMID:9223281</ref> <ref>PMID:10449719</ref> <ref>PMID:12954634</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene 1f and the indole 1g display the optimal orientation of the carboxylate for enhanced FXR agonist potency.

-	~~==Function==~~	+	Conformationally constrained farnesoid X receptor (FXR) agonists: Alternative replacements of the stilbene.,Akwabi-Ameyaw A, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, Miller AB, Navas F 3rd, Parks DJ, Spearing PK, Todd D, Williams SP, Wisely GB Bioorg Med Chem Lett. 2011 Aug 11. PMID:21890356<ref>PMID:21890356</ref>
-	[[http://www.uniprot.org/uniprot/NR1H4_HUMAN NR1H4_HUMAN]] Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxylase gene (~~CYP7A1~~) ~~through the induction~~ of ~~NR0B2 or FGF19 expression, via two distinct mechanisms. Activates~~ the ~~intestinal bile acid-binding protein (IBABP)~~. Activates the transcription of bile salt export pump ABCB11 by directly recruiting histone methyltransferase CARM1 to this locus.<ref>PMID:10334992</ref><ref>PMID:10334993</ref><ref>PMID:12815072</ref><ref>PMID:15471871</ref><ref>PMID:12718892</ref><ref>PMID:18621523</ref><ref>PMID:19410460</ref><ref>PMID:19586769</ref> [[http://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Nuclear receptor coactivator that directly binds nuclear receptors and stimulates the transcriptional activities in a hormone-~~dependent fashion. Involved in the coactivation of different nuclear receptors~~, ~~such as for steroids (PGR~~, ~~GR and ER)~~, ~~retinoids (RXRs)~~, ~~thyroid hormone (TRs) and prostanoids (PPARs). Also involved in coactivation mediated by STAT3~~, ~~STAT5A~~, STAT5B and STAT6 transcription factors. Displays histone acetyltransferase activity toward H3 and H4; the relevance of such activity remains however unclear. Plays a central role in creating multisubunit coactivator complexes that act via remodeling of chromatin, ~~and possibly acts by participating in both chromatin remodeling and recruitment of general transcription factors~~. ~~Required with NCOA2 to control energy balance between white and brown adipose tissues~~. ~~Required for mediating steroid hormone response. Isoform 2 has a higher thyroid hormone-dependent transactivation activity than isoform 1 and isoform 3.<ref>~~PMID:~~9427757</ref><ref>PMID:7481822</ref><ref>PMID:9223431</ref><ref>PMID:9296499</ref><ref>PMID:9223281</ref><ref>PMID:10449719</ref>~~<ref>PMID:~~12954634~~</ref>	+

-	~~==About this Structure==~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[3rut]] is~~ a ~~2 chain structure with sequence from [http://en~~.~~wikipedia~~.~~org/wiki/Homo_sapiens Homo sapiens]~~. ~~Full crystallographic information is available from [http:~~/~~/oca.weizmann.ac.il/oca-bin/ocashort?id=3RUT OCA].~~	+	</div>

-	==~~Reference~~==	+	==See Also==
-	~~<ref group~~=~~"xtra">PMID:021890356</ref>~~<references ~~group="xtra"~~/><~~references~~/>	+	*[[Bile acid receptor\|Bile acid receptor]]
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
	[[Category: Histone acetyltransferase]]		[[Category: Histone acetyltransferase]]
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
-	[[Category: Madauss, K P.]]	+	[[Category: Madauss, K P]]
-	[[Category: Williams, S P.]]	+	[[Category: Williams, S P]]
	[[Category: Alpha-helical sandwich]]		[[Category: Alpha-helical sandwich]]
	[[Category: Bile acid]]		[[Category: Bile acid]]

OCA at 07:14, 25 March 2013

OCA — Mon, 25 Mar 2013 07:14:27 GMT

←Older revision		Revision as of 07:14, 25 March 2013
Line 1:		Line 1:
-	[[Image:3rut.png\|left\|200px]]
-
-	<!--
-	The line below this paragraph, containing "STRUCTURE_3rut", creates the "Structure Box" on the page.
-	You may change the PDB parameter (which sets the PDB file loaded into the applet)
-	or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-	or leave the SCENE parameter empty for the default display.
-	-->
	{{STRUCTURE_3rut\| PDB=3rut \| SCENE= }}		{{STRUCTURE_3rut\| PDB=3rut \| SCENE= }}
-
	===FXR with SRC1 and GSK359===		===FXR with SRC1 and GSK359===
		+	{{ABSTRACT_PUBMED_21890356}}

		+	==Disease==
		+	[[http://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Note=A chromosomal aberration involving NCOA1 is a cause of rhabdomyosarcoma. Translocation t(2;2)(q35;p23) with PAX3 generates the NCOA1-PAX3 oncogene consisting of the N-terminus part of PAX3 and the C-terminus part of NCOA1. The fusion protein acts as a transcriptional activator. Rhabdomyosarcoma is the most common soft tissue carcinoma in childhood, representing 5-8% of all malignancies in children.

-	~~<!--~~	+	==Function==
-	~~The line below this paragraph~~, ~~{{ABSTRACT_PUBMED_21890356}}, adds~~ the ~~Publication Abstract to~~ the ~~page~~	+	[[http://www.uniprot.org/uniprot/NR1H4_HUMAN NR1H4_HUMAN]] Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxylase gene (CYP7A1) through the induction of NR0B2 or FGF19 expression, via two distinct mechanisms. Activates the intestinal bile acid-binding protein (IBABP). Activates the transcription of bile salt export pump ABCB11 by directly recruiting histone methyltransferase CARM1 to this locus.<ref>PMID:10334992</ref><ref>PMID:10334993</ref><ref>PMID:12815072</ref><ref>PMID:15471871</ref><ref>PMID:12718892</ref><ref>PMID:18621523</ref><ref>PMID:19410460</ref><ref>PMID:19586769</ref> [[http://www.uniprot.org/uniprot/NCOA1_HUMAN NCOA1_HUMAN]] Nuclear receptor coactivator that directly binds nuclear receptors and stimulates the transcriptional activities in a hormone-dependent fashion. Involved in the coactivation of different nuclear receptors, such as for steroids (PGR, GR and ER), retinoids (RXRs), thyroid hormone (TRs) and prostanoids (PPARs). Also involved in coactivation mediated by STAT3, STAT5A, STAT5B and STAT6 transcription factors. Displays histone acetyltransferase activity toward H3 and H4; the relevance of such activity remains however unclear. Plays a central role in creating multisubunit coactivator complexes that act via remodeling of chromatin, and possibly acts by participating in both chromatin remodeling and recruitment of general transcription factors. Required with NCOA2 to control energy balance between white and brown adipose tissues. Required for mediating steroid hormone response. Isoform 2 has a higher thyroid hormone-dependent transactivation activity than isoform 1 and isoform 3.<ref>PMID:9427757</ref><ref>PMID:7481822</ref><ref>PMID:9223431</ref><ref>PMID:9296499</ref><ref>PMID:9223281</ref><ref>PMID:10449719</ref><ref>PMID:12954634</ref>
-	(~~as it appears on PubMed at~~ http://www.~~pubmed~~.~~gov~~), ~~where 21890356 is~~ the ~~PubMed ID number~~.	+
-	-->	+
-	~~{{ABSTRACT_PUBMED_21890356}}~~	+

	==About this Structure==		==About this Structure==
Line 22:		Line 13:

	==Reference==		==Reference==
-	<ref group="xtra">PMID:021890356</ref><references group="xtra"/>	+	<ref group="xtra">PMID:021890356</ref><references group="xtra"/><references/>
	[[Category: Histone acetyltransferase]]		[[Category: Histone acetyltransferase]]
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]

OCA at 05:40, 5 October 2011

OCA — Wed, 05 Oct 2011 05:40:59 GMT

←Older revision		Revision as of 05:40, 5 October 2011
Line 1:		Line 1:
-	[[Image:3rut.~~jpg~~\|left\|200px]]	+	[[Image:3rut.png\|left\|200px]]

	<!--		<!--

OCA at 05:54, 21 September 2011

OCA — Wed, 21 Sep 2011 05:54:38 GMT

←Older revision		Revision as of 05:54, 21 September 2011
Line 1:		Line 1:
-	~~'''Unreleased structure'''~~	+	[[Image:3rut.jpg\|left\|200px]]

-	The ~~entry 3rut~~ is ~~ON HOLD~~ ~~until Paper Publication~~	+	<!--
		+	The line below this paragraph, containing "STRUCTURE_3rut", creates the "Structure Box" on the page.
		+	You may change the PDB parameter (which sets the PDB file loaded into the applet)
		+	or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
		+	or leave the SCENE parameter empty for the default display.
		+	-->
		+	{{STRUCTURE_3rut\| PDB=3rut \| SCENE= }}

-	~~Authors: Williams, S.P., Madauss, K.P.~~	+	===FXR with SRC1 and GSK359===

-	~~Description~~: ~~FXR~~ with ~~SRC1 and GSK359~~	+
		+	<!--
		+	The line below this paragraph, {{ABSTRACT_PUBMED_21890356}}, adds the Publication Abstract to the page
		+	(as it appears on PubMed at http://www.pubmed.gov), where 21890356 is the PubMed ID number.
		+	-->
		+	{{ABSTRACT_PUBMED_21890356}}
		+
		+	==About this Structure==
		+	[[3rut]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RUT OCA].
		+
		+	==Reference==
		+	<ref group="xtra">PMID:021890356</ref><references group="xtra"/>
		+	[[Category: Histone acetyltransferase]]
		+	[[Category: Homo sapiens]]
		+	[[Category: Madauss, K P.]]
		+	[[Category: Williams, S P.]]
		+	[[Category: Alpha-helical sandwich]]
		+	[[Category: Bile acid]]
		+	[[Category: Farnesoid]]
		+	[[Category: Nuclear receptor]]
		+	[[Category: Rxr]]
		+	[[Category: Transcription co-factor]]
		+	[[Category: Transcription factor]]
		+	[[Category: Transcription regulator]]

OCA at 05:09, 25 May 2011

OCA — Wed, 25 May 2011 05:09:55 GMT

←Older revision		Revision as of 05:09, 25 May 2011
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 3rut is ON HOLD	+	The entry 3rut is ON HOLD until Paper Publication

	Authors: Williams, S.P., Madauss, K.P.		Authors: Williams, S.P., Madauss, K.P.

	Description: FXR with SRC1 and GSK359		Description: FXR with SRC1 and GSK359

OCA at 05:16, 18 May 2011

OCA — Wed, 18 May 2011 05:16:01 GMT

←Older revision		Revision as of 05:16, 18 May 2011
Line 3:		Line 3:
	The entry 3rut is ON HOLD		The entry 3rut is ON HOLD

-	Authors: Williams, ~~Shawn~~ P., Madauss, ~~Kevin~~ P.	+	Authors: Williams, S.P., Madauss, K.P.

	Description: FXR with SRC1 and GSK359		Description: FXR with SRC1 and GSK359