3plz - Revision history

OCA at 10:41, 21 February 2024

OCA — Wed, 21 Feb 2024 10:41:48 GMT

←Older revision		Revision as of 10:41, 21 February 2024
Line 3:		Line 3:
	<StructureSection load='3plz' size='340' side='right'caption='[[3plz]], [[Resolution\|resolution]] 1.75Å' scene=''>		<StructureSection load='3plz' size='340' side='right'caption='[[3plz]], [[Resolution\|resolution]] 1.75Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3plz]] is a 4 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=3PLZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PLZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3plz]] is a 4 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=3PLZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PLZ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=470:(3AS,6AR)-5-[(4E)-OCT-4-EN-4-YL]-N,4-DIPHENYL-2,3,6,6A-TETRAHYDROPENTALEN-3A(1H)-AMINE'>470</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</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]] 1.75Å</td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1yok\|1yok]]</div></td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=470:(3AS,6AR)-5-[(4E)-OCT-4-EN-4-YL]-N,4-DIPHENYL-2,3,6,6A-TETRAHYDROPENTALEN-3A(1H)-AMINE'>470</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">NR5A2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])~~</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=3plz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3plz OCA], [https://pdbe.org/3plz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3plz RCSB], [https://www.ebi.ac.uk/pdbsum/3plz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3plz 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=3plz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3plz OCA], [https://pdbe.org/3plz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3plz RCSB], [https://www.ebi.ac.uk/pdbsum/3plz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3plz ProSAT]</span></td></tr>
	</table>		</table>
-	== Disease ==
-	[[https://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Note=Chromosomal aberrations involving NCOA2 may be a cause of acute myeloid leukemias. Inversion inv(8)(p11;q13) generates the KAT6A-NCOA2 oncogene, which consists of the N-terminal part of KAT6A and the C-terminal part of NCOA2/TIF2. KAT6A-NCOA2 binds to CREBBP and disrupts its function in transcription activation.
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/~~NCOA2_HUMAN NCOA2_HUMAN~~]~~] Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of~~ the ~~steroid binding domain (AF~~-~~2) but not~~ of the ~~modulating N-terminal domain (AF-1). Required with NCOA1 to control energy balance between white and brown adipose tissues.<ref>PMID:9430642</ref>~~	+	[https://www.uniprot.org/uniprot/NR5A2_HUMAN NR5A2_HUMAN] Binds to the sequence element 5'-AACGACCGACCTTGAG-3' of the enhancer II of hepatitis B virus genes, a critical cis-element of their expression and regulation. May be responsible for the liver-specific activity of enhancer II, probably in combination with other hepatocyte transcription factors. Key regulator of cholesterol 7-alpha-hydroxylase gene (CYP7A) expression in liver. May also contribute to the regulation of pancreas-specific genes and play important roles in embryonic development.
-	~~<div style="background-color:#fffaf0;">~~	+
-	~~== Publication Abstract from PubMed ==~~	+
-	~~The crystal structure~~ of ~~LRH-1 ligand binding domain bound to our previously reported agonist 3-(E-oct-4-en-4-yl)-1-phenylamino-2-phenyl-~~cis-~~bicyclo[3~~.~~3.0]oct~~-~~2-ene 5 is described. Two new classes~~ of ~~agonists~~ in ~~which the bridgehead anilino group from our first series was replaced~~ with ~~an alkoxy or 1-ethenyl group were designed, synthesized, and tested for activity in a peptide recruitment assay~~. ~~Both new classes gave very active compounds, particularly against SF~~-~~1. Structure~~-~~activity studies led to excellent dual-LRH-1/SF-1 agonists~~ (~~e.g., RJW100) as well as compounds selective for LRH-1 (RJW101) and SF-1 (RJW102 and RJW103~~). ~~The series based on 1-ethenyl substitution was acid stable, overcoming a significant drawback of our original bridgehead anilino-substituted series. Initial studies on~~ the regulation of ~~gene expression in human cell lines showed excellent, reproducible activity at endogenous target~~ genes.	+
-		+
-	~~Small Molecule Agonists of the Orphan Nuclear Receptors Steroidogenic Factor-1 (SF-1, NR5A1)~~ and ~~Liver Receptor Homologue-1 (LRH-1, NR5A2)~~.~~,Whitby RJ, Stec J, Blind RD, Dixon S, Leesnitzer LM, Orband-Miller LA, Williams SP, Willson TM, Xu R, Zuercher WJ, Cai F, Ingraham HA J Med Chem. 2011 Mar 10. PMID:21391689<ref>PMID:21391689</ref>~~	+
-		+
-	~~From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~	+
-	~~</div>~~	+
-	~~<div class="pdbe-citations 3plz" style="background-color:#fffaf0;"></div>~~	+
-	~~== References ==~~	+
-	~~<references/>~~	+
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Williams~~, S P~~]]	+	[[Category: Williams SP]]
-	[[Category: Xu, R]]	+	[[Category: Xu R]]
-	[[Category: Zuercher~~, W J]]~~	+	[[Category: Zuercher WJ]]
-	~~[[Category: Alpha helical sandwhich]]~~	+
-	~~[[Category: Co-activator]]~~	+
-	~~[[Category: Family five]]~~	+
-	~~[[Category: Nuclear receptor]]~~	+
-	~~[[Category: Transcription factor]]~~	+
-	~~[[Category: Transcription-receptor-agonist complex~~]]	+

OCA at 08:45, 25 May 2022

OCA — Wed, 25 May 2022 08:45:03 GMT

←Older revision		Revision as of 08:45, 25 May 2022
Line 1:		Line 1:

	==Human LRH1 LBD bound to GR470==		==Human LRH1 LBD bound to GR470==
-	<StructureSection load='3plz' size='340' side='right' caption='[[3plz]], [[Resolution\|resolution]] 1.75Å' scene=''>	+	<StructureSection load='3plz' size='340' side='right'caption='[[3plz]], [[Resolution\|resolution]] 1.75Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3plz]] is a 4 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=3PLZ OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3PLZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3plz]] is a 4 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=3PLZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PLZ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=470:(3AS,6AR)-5-[(4E)-OCT-4-EN-4-YL]-N,4-DIPHENYL-2,3,6,6A-TETRAHYDROPENTALEN-3A(1H)-AMINE'>470</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=470:(3AS,6AR)-5-[(4E)-OCT-4-EN-4-YL]-N,4-DIPHENYL-2,3,6,6A-TETRAHYDROPENTALEN-3A(1H)-AMINE'>470</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1yok\|1yok]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1yok\|1yok]]</div></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">NR5A2 ([~~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">NR5A2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=3plz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3plz OCA], [~~http~~://pdbe.org/3plz PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3plz RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3plz PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=3plz 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=3plz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3plz OCA], [https://pdbe.org/3plz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3plz RCSB], [https://www.ebi.ac.uk/pdbsum/3plz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3plz ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
-	[[~~http~~://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Note=Chromosomal aberrations involving NCOA2 may be a cause of acute myeloid leukemias. Inversion inv(8)(p11;q13) generates the KAT6A-NCOA2 oncogene, which consists of the N-terminal part of KAT6A and the C-terminal part of NCOA2/TIF2. KAT6A-NCOA2 binds to CREBBP and disrupts its function in transcription activation.	+	[[https://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Note=Chromosomal aberrations involving NCOA2 may be a cause of acute myeloid leukemias. Inversion inv(8)(p11;q13) generates the KAT6A-NCOA2 oncogene, which consists of the N-terminal part of KAT6A and the C-terminal part of NCOA2/TIF2. KAT6A-NCOA2 binds to CREBBP and disrupts its function in transcription activation.
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of the steroid binding domain (AF-2) but not of the modulating N-terminal domain (AF-1). Required with NCOA1 to control energy balance between white and brown adipose tissues.<ref>PMID:9430642</ref>	+	[[https://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of the steroid binding domain (AF-2) but not of the modulating N-terminal domain (AF-1). Required with NCOA1 to control energy balance between white and brown adipose tissues.<ref>PMID:9430642</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 27:		Line 27:
	</StructureSection>		</StructureSection>
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Williams, S P]]		[[Category: Williams, S P]]
	[[Category: Xu, R]]		[[Category: Xu, R]]

OCA at 12:40, 4 August 2016

OCA — Thu, 04 Aug 2016 12:40:13 GMT

←Older revision		Revision as of 12:40, 4 August 2016
Line 1:		Line 1:
		+
	==Human LRH1 LBD bound to GR470==		==Human LRH1 LBD bound to GR470==
	<StructureSection load='3plz' size='340' side='right' caption='[[3plz]], [[Resolution\|resolution]] 1.75Å' scene=''>		<StructureSection load='3plz' size='340' side='right' caption='[[3plz]], [[Resolution\|resolution]] 1.75Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3plz]] is a 4 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=3PLZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PLZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3plz]] is a 4 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=3PLZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PLZ FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=470:(3AS,6AR)-5-[(4E)-OCT-4-EN-4-YL]-N,4-DIPHENYL-2,3,6,6A-TETRAHYDROPENTALEN-3A(1H)-AMINE'>470</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=470:(3AS,6AR)-5-[(4E)-OCT-4-EN-4-YL]-N,4-DIPHENYL-2,3,6,6A-TETRAHYDROPENTALEN-3A(1H)-AMINE'>470</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1yok\|1yok]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1yok\|1yok]]</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">NR5A2 ([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">NR5A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=3plz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3plz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3plz RCSB], [http://www.ebi.ac.uk/pdbsum/3plz 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=3plz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3plz OCA], [http://pdbe.org/3plz PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3plz RCSB], [http://www.ebi.ac.uk/pdbsum/3plz PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3plz ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
Line 20:		Line 21:
	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 3plz" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Williams, S P]]		[[Category: Williams, S P]]
	[[Category: Xu, R]]		[[Category: Xu, R]]

OCA at 10:38, 19 December 2014

OCA — Fri, 19 Dec 2014 10:38:19 GMT

←Older revision		Revision as of 10:38, 19 December 2014
Line 1:		Line 1:
-	~~{{STRUCTURE_3plz~~\| ~~PDB~~=3plz \| ~~SCENE~~= }}	+	==Human LRH1 LBD bound to GR470==
-	===~~Human LRH1 LBD bound to GR470~~===	+	<StructureSection load='3plz' size='340' side='right' caption='[[3plz]], [[Resolution\|resolution]] 1.75Å' scene=''>
-	~~{{ABSTRACT_PUBMED_21391689}}~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[3plz]] is a 4 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=3PLZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PLZ FirstGlance]. <br>
-	==Disease==	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=470:(3AS,6AR)-5-[(4E)-OCT-4-EN-4-YL]-N,4-DIPHENYL-2,3,6,6A-TETRAHYDROPENTALEN-3A(1H)-AMINE'>470</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1yok\|1yok]]</td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">NR5A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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=3plz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3plz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3plz RCSB], [http://www.ebi.ac.uk/pdbsum/3plz PDBsum]</span></td></tr>
		+	</table>
		+	== Disease ==
	[[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Note=Chromosomal aberrations involving NCOA2 may be a cause of acute myeloid leukemias. Inversion inv(8)(p11;q13) generates the KAT6A-NCOA2 oncogene, which consists of the N-terminal part of KAT6A and the C-terminal part of NCOA2/TIF2. KAT6A-NCOA2 binds to CREBBP and disrupts its function in transcription activation.		[[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Note=Chromosomal aberrations involving NCOA2 may be a cause of acute myeloid leukemias. Inversion inv(8)(p11;q13) generates the KAT6A-NCOA2 oncogene, which consists of the N-terminal part of KAT6A and the C-terminal part of NCOA2/TIF2. KAT6A-NCOA2 binds to CREBBP and disrupts its function in transcription activation.
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of the steroid binding domain (AF-2) but not of the modulating N-terminal domain (AF-1). Required with NCOA1 to control energy balance between white and brown adipose tissues.<ref>PMID:9430642</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The crystal structure of LRH-1 ligand binding domain bound to our previously reported agonist 3-(E-oct-4-en-4-yl)-1-phenylamino-2-phenyl-cis-bicyclo[3.3.0]oct-2-ene 5 is described. Two new classes of agonists in which the bridgehead anilino group from our first series was replaced with an alkoxy or 1-ethenyl group were designed, synthesized, and tested for activity in a peptide recruitment assay. Both new classes gave very active compounds, particularly against SF-1. Structure-activity studies led to excellent dual-LRH-1/SF-1 agonists (e.g., RJW100) as well as compounds selective for LRH-1 (RJW101) and SF-1 (RJW102 and RJW103). The series based on 1-ethenyl substitution was acid stable, overcoming a significant drawback of our original bridgehead anilino-substituted series. Initial studies on the regulation of gene expression in human cell lines showed excellent, reproducible activity at endogenous target genes.

-	~~==Function==~~	+	Small Molecule Agonists of the Orphan Nuclear Receptors Steroidogenic Factor-1 (SF-1, NR5A1) and Liver Receptor Homologue-1 (LRH-1, NR5A2).,Whitby RJ, Stec J, Blind RD, Dixon S, Leesnitzer LM, Orband-Miller LA, Williams SP, Willson TM, Xu R, Zuercher WJ, Cai F, Ingraham HA J Med Chem. 2011 Mar 10. PMID:21391689<ref>PMID:21391689</ref>
-	~~[[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator~~ of the ~~steroid binding domain~~ (AF-2) ~~but not of the modulating N~~-~~terminal domain~~ (AF-1). ~~Required with NCOA1 to control energy balance between white and brown adipose tissues~~.<ref>PMID:~~9430642~~</ref>	+
-		+
-	~~==About this Structure==~~	+
-	[[3plz]] is a 4 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=3PLZ OCA].	+

-	==~~Reference~~==	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~<ref group="xtra">PMID:021391689</ref>~~<references ~~group="xtra"~~/><~~references~~/>	+	</div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
-	[[Category: Williams, S P.]]	+	[[Category: Williams, S P]]
-	[[Category: Xu, R.]]	+	[[Category: Xu, R]]
-	[[Category: Zuercher, W J.]]	+	[[Category: Zuercher, W J]]
	[[Category: Alpha helical sandwhich]]		[[Category: Alpha helical sandwhich]]
	[[Category: Co-activator]]		[[Category: Co-activator]]

OCA at 18:40, 24 March 2013

OCA — Sun, 24 Mar 2013 18:40:19 GMT

←Older revision		Revision as of 18:40, 24 March 2013
Line 1:		Line 1:
-	[[Image:3plz.png\|left\|200px]]
-
-	<!--
-	The line below this paragraph, containing "STRUCTURE_3plz", 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_3plz\| PDB=3plz \| SCENE= }}		{{STRUCTURE_3plz\| PDB=3plz \| SCENE= }}
-
	===Human LRH1 LBD bound to GR470===		===Human LRH1 LBD bound to GR470===
		+	{{ABSTRACT_PUBMED_21391689}}

		+	==Disease==
		+	[[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Note=Chromosomal aberrations involving NCOA2 may be a cause of acute myeloid leukemias. Inversion inv(8)(p11;q13) generates the KAT6A-NCOA2 oncogene, which consists of the N-terminal part of KAT6A and the C-terminal part of NCOA2/TIF2. KAT6A-NCOA2 binds to CREBBP and disrupts its function in transcription activation.

-	~~<!--~~	+	==Function==
-	~~The line below this paragraph, {{ABSTRACT_PUBMED_21391689}}, adds the Publication Abstract to the page~~	+	[[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of the steroid binding domain (AF-2) but not of the modulating N-terminal domain (AF-1). Required with NCOA1 to control energy balance between white and brown adipose tissues.<ref>PMID:9430642</ref>
-	~~(as it appears on PubMed at~~ http://www.~~pubmed~~.~~gov~~)~~, where 21391689 is~~ the ~~PubMed ID number.~~	+
-	-->	+
-	~~{{ABSTRACT_PUBMED_21391689}}~~	+

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

	==Reference==		==Reference==
-	<ref group="xtra">PMID:~~21391689~~</ref><references group="xtra"/>	+	<ref group="xtra">PMID:021391689</ref><references group="xtra"/><references/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Williams, S P.]]		[[Category: Williams, S P.]]
	[[Category: Xu, R.]]		[[Category: Xu, R.]]
	[[Category: Zuercher, W J.]]		[[Category: Zuercher, W J.]]
		+	[[Category: Alpha helical sandwhich]]
		+	[[Category: Co-activator]]
		+	[[Category: Family five]]
		+	[[Category: Nuclear receptor]]
		+	[[Category: Transcription factor]]
		+	[[Category: Transcription-receptor-agonist complex]]

OCA at 06:17, 27 April 2011

OCA — Wed, 27 Apr 2011 06:17:13 GMT

←Older revision		Revision as of 06:17, 27 April 2011
Line 1:		Line 1:
-	[[Image:3plz.~~jpg~~\|left\|200px]]	+	[[Image:3plz.png\|left\|200px]]

	<!--		<!--

OCA: Protected "3plz" [edit=sysop:move=sysop]

OCA — Wed, 30 Mar 2011 08:02:25 GMT

Protected "3plz" [edit=sysop:move=sysop]

←Older revision

Revision as of 08:02, 30 March 2011

OCA at 08:02, 30 March 2011

OCA — Wed, 30 Mar 2011 08:02:18 GMT

←Older revision		Revision as of 08:02, 30 March 2011
Line 1:		Line 1:
-	~~'''Unreleased structure'''~~	+	[[Image:3plz.jpg\|left\|200px]]

-	The ~~entry 3plz~~ is ~~ON HOLD~~ ~~until Paper Publication~~	+	<!--
		+	The line below this paragraph, containing "STRUCTURE_3plz", 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_3plz\| PDB=3plz \| SCENE= }}

-	~~Authors: Williams, S.P., Xu, R., Zuercher, W.J.~~	+	===Human LRH1 LBD bound to GR470===

-	Description: Human LRH1 LBD bound to GR470

-	~~''Page seeded by~~ [http://oca.weizmann.ac.il/oca OCA ] ~~on Wed Dec 15 08~~:24:~~14 2010''~~	+	<!--
		+	The line below this paragraph, {{ABSTRACT_PUBMED_21391689}}, adds the Publication Abstract to the page
		+	(as it appears on PubMed at http://www.pubmed.gov), where 21391689 is the PubMed ID number.
		+	-->
		+	{{ABSTRACT_PUBMED_21391689}}
		+
		+	==About this Structure==
		+	[[3plz]] is a 4 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=3PLZ OCA].
		+
		+	==Reference==
		+	<ref group="xtra">PMID:21391689</ref><references group="xtra"/>
		+	[[Category: Homo sapiens]]
		+	[[Category: Williams, S P.]]
		+	[[Category: Xu, R.]]
		+	[[Category: Zuercher, W J.]]

OCA at 05:11, 15 December 2010

OCA — Wed, 15 Dec 2010 05:11:54 GMT

←Older revision		Revision as of 05:11, 15 December 2010
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

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

	Authors: Williams, S.P., Xu, R., Zuercher, W.J.		Authors: Williams, S.P., Xu, R., Zuercher, W.J.
Line 7:		Line 7:
	Description: Human LRH1 LBD bound to GR470		Description: Human LRH1 LBD bound to GR470

-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed ~~Nov 24 13~~:58:47 2010''	+	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Dec 15 08:24:14 2010''

OCA: New page: '''Unreleased structure''' The entry 3plz is ON HOLD Authors: Williams, S.P., Xu, R., Zuercher, W.J. Description: Human LRH1 LBD bound to GR470 ''Page seeded by [http://oca.weizmann.a...

OCA — Wed, 24 Nov 2010 10:47:16 GMT

New page: '''Unreleased structure''' The entry 3plz is ON HOLD Authors: Williams, S.P., Xu, R., Zuercher, W.J. Description: Human LRH1 LBD bound to GR470 ''Page seeded by [http://oca.weizmann.a...

New page

'''Unreleased structure'''

The entry 3plz is ON HOLD

Authors: Williams, S.P., Xu, R., Zuercher, W.J.

Description: Human LRH1 LBD bound to GR470

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Nov 24 13:58:47 2010''