2p1v - Revision history

OCA at 07:13, 11 September 2015

2015-09-11T07:13:33Z

←Older revision		Revision as of 07:13, 11 September 2015
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	<StructureSection load='2p1v' size='340' side='right' caption='[[2p1v]], [[Resolution\|resolution]] 2.20Å' scene=''>		<StructureSection load='2p1v' size='340' side='right' caption='[[2p1v]], [[Resolution\|resolution]] 2.20Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2p1v]] 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=2P1V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2P1V FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2p1v]] 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=2P1V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2P1V FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5TN:(2E)-3-[4-HYDROXY-3-(5,5,8,8-TETRAMETHYL-3-PROPOXY-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)PHENYL]ACRYLIC+ACID'>5TN</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5TN:(2E)-3-[4-HYDROXY-3-(5,5,8,8-TETRAMETHYL-3-PROPOXY-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)PHENYL]ACRYLIC+ACID'>5TN</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lbd\|1lbd]], [[1fby\|1fby]], [[1mvc\|1mvc]], [[1xdk\|1xdk]], [[2p1t\|2p1t]], [[2p1u\|2p1u]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lbd\|1lbd]], [[1fby\|1fby]], [[1mvc\|1mvc]], [[1xdk\|1xdk]], [[2p1t\|2p1t]], [[2p1u\|2p1u]]</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">RXRA, NR2B1 ([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">RXRA, NR2B1 ([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=2p1v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p1v OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2p1v RCSB], [http://www.ebi.ac.uk/pdbsum/2p1v 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=2p1v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p1v OCA], [http://pdbe.org/2p1v PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2p1v RCSB], [http://www.ebi.ac.uk/pdbsum/2p1v PDBsum]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
Line 30:		Line 30:
	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 2p1v" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 37:		Line 38:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Bourguet, W]]		[[Category: Bourguet, W]]
	[[Category: Nahoum, V]]		[[Category: Nahoum, V]]
	[[Category: Hormone receptor]]		[[Category: Hormone receptor]]
	[[Category: Protein-ligand complex]]		[[Category: Protein-ligand complex]]

OCA at 18:32, 19 January 2015

2015-01-19T18:32:02Z

←Older revision		Revision as of 18:32, 19 January 2015
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2p1v]] 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=2P1V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2P1V FirstGlance]. <br>		<table><tr><td colspan='2'>[[2p1v]] 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=2P1V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2P1V FirstGlance]. <br>
-	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5TN:(2E)-3-[4-HYDROXY-3-(5,5,8,8-TETRAMETHYL-3-PROPOXY-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)PHENYL]ACRYLIC+ACID'>5TN</scene><br>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5TN:(2E)-3-[4-HYDROXY-3-(5,5,8,8-TETRAMETHYL-3-PROPOXY-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)PHENYL]ACRYLIC+ACID'>5TN</scene></td></tr>
-	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lbd\|1lbd]], [[1fby\|1fby]], [[1mvc\|1mvc]], [[1xdk\|1xdk]], [[2p1t\|2p1t]], [[2p1u\|2p1u]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lbd\|1lbd]], [[1fby\|1fby]], [[1mvc\|1mvc]], [[1xdk\|1xdk]], [[2p1t\|2p1t]], [[2p1u\|2p1u]]</td></tr>
-	<tr><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">RXRA, NR2B1 ([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">RXRA, NR2B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
-	<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2p1v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p1v OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2p1v RCSB], [http://www.ebi.ac.uk/pdbsum/2p1v 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=2p1v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p1v OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2p1v RCSB], [http://www.ebi.ac.uk/pdbsum/2p1v PDBsum]</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.		[[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.
Line 38:		Line 38:
	</StructureSection>		</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
-	[[Category: Bourguet, W.]]	+	[[Category: Bourguet, W]]
-	[[Category: Nahoum, V.]]	+	[[Category: Nahoum, V]]
	[[Category: Hormone receptor]]		[[Category: Hormone receptor]]
	[[Category: Protein-ligand complex]]		[[Category: Protein-ligand complex]]

OCA at 20:16, 30 September 2014

2014-09-30T20:16:17Z

←Older revision		Revision as of 20:16, 30 September 2014
Line 1:		Line 1:
-	~~{{STRUCTURE_2p1v\| PDB=2p1v \| SCENE= }}~~	+	==Crystal structure of the ligand binding domain of the retinoid X receptor alpha in complex with 3-(2'-propoxy)-tetrahydronaphtyl cinnamic acid and a fragment of the coactivator TIF-2==
-	===Crystal structure of the ligand binding domain of the retinoid X receptor alpha in complex with 3-(2'-propoxy)-tetrahydronaphtyl cinnamic acid and a fragment of the coactivator TIF-2===	+	<StructureSection load='2p1v' size='340' side='right' caption='[[2p1v]], [[Resolution\|resolution]] 2.20Å' scene=''>
-	~~{{ABSTRACT_PUBMED_17947383}}~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[2p1v]] 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=2P1V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2P1V FirstGlance]. <br>
-	==Disease==	+	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5TN:(2E)-3-[4-HYDROXY-3-(5,5,8,8-TETRAMETHYL-3-PROPOXY-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)PHENYL]ACRYLIC+ACID'>5TN</scene><br>
		+	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1lbd\|1lbd]], [[1fby\|1fby]], [[1mvc\|1mvc]], [[1xdk\|1xdk]], [[2p1t\|2p1t]], [[2p1u\|2p1u]]</td></tr>
		+	<tr><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">RXRA, NR2B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
		+	<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2p1v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p1v OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2p1v RCSB], [http://www.ebi.ac.uk/pdbsum/2p1v 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/RXRA_HUMAN RXRA_HUMAN]] Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. The high affinity ligand for RXRs is 9-cis retinoic acid. RXRA serves as a common heterodimeric partner for a number of nuclear receptors. The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone acetylation, chromatin condensation and transcriptional suppression. On ligand binding, the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation. The RXRA/PPARA heterodimer is required for PPARA transcriptional activity on fatty acid oxidation genes such as ACOX1 and the P450 system genes.<ref>PMID:10195690</ref> <ref>PMID:11162439</ref> <ref>PMID:11915042</ref> <ref>PMID:20215566</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>
		+	== Evolutionary Conservation ==
		+	[[Image:Consurf_key_small.gif\|200px\|right]]
		+	Check<jmol>
		+	<jmolCheckbox>
		+	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/p1/2p1v_consurf.spt"</scriptWhenChecked>
		+	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
		+	<text>to colour the structure by Evolutionary Conservation</text>
		+	</jmolCheckbox>
		+	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/chain_selection.php?pdb_ID=2ata ConSurf].
		+	<div style="clear:both"></div>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Retinoid X receptors (RXRalpha, -beta, and -gamma) occupy a central position in the nuclear receptor superfamily, because they form heterodimers with many other family members and hence are involved in the control of a variety of (patho)physiologic processes. Selective RXR ligands, referred to as rexinoids, are already used or are being developed for cancer therapy and have promise for the treatment of metabolic diseases. However, important side effects remain associated with existing rexinoids. Here we describe the rational design and functional characterization of a spectrum of RXR modulators ranging from partial to pure antagonists and demonstrate their utility as tools to probe the implication of RXRs in cell biological phenomena. One of these ligands renders RXR activity particularly sensitive to coactivator levels and has the potential to act as a cell-specific RXR modulator. A combination of crystallographic and fluorescence anisotropy studies reveals the molecular details accounting for the agonist-to-antagonist transition and provides direct experimental evidence for a correlation between the pharmacological activity of a ligand and its impact on the structural dynamics of the activation helix H12. Using RXR and its cognate ligands as a model system, our correlative analysis of 3D structures and dynamic data provides an original view on ligand actions and enables the establishment of mechanistic concepts, which will aid in the development of selective nuclear receptor modulators.

-	~~==Function==~~	+	Modulators of the structural dynamics of the retinoid X receptor to reveal receptor function.,Nahoum V, Perez E, Germain P, Rodriguez-Barrios F, Manzo F, Kammerer S, Lemaire G, Hirsch O, Royer CA, Gronemeyer H, de Lera AR, Bourguet W Proc Natl Acad Sci U S A. 2007 Oct 30;104(44):17323-8. Epub 2007 Oct 18. PMID:17947383<ref>PMID:17947383</ref>
-	[[http://www.uniprot.org/uniprot/RXRA_HUMAN RXRA_HUMAN]] Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the ~~retinoic acid response elements (RARE) composed~~ of tandem 5'-AGGTCA-3' sites known as DR1-DR5. The high affinity ligand for RXRs is 9-cis retinoic acid. RXRA serves as a common heterodimeric partner for a number of nuclear receptors. The RXR/RAR heterodimers bind to ~~the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5~~. ~~In the absence of ligand~~, ~~the RXR~~-~~RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone acetylation~~, ~~chromatin condensation and transcriptional suppression. On ligand binding~~, ~~the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation~~. The RXRA/PPARA heterodimer is required for PPARA transcriptional activity on fatty acid oxidation genes such as ACOX1 and the P450 system genes.<ref>PMID:10195690</ref><ref>PMID:11162439</ref><ref>PMID:11915042</ref><ref>PMID:20215566</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==~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[2p1v]] 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=2P1V OCA].~~	+	</div>

	==See Also==		==See Also==
	*[[Retinoid X receptor\|Retinoid X receptor]]		*[[Retinoid X receptor\|Retinoid X receptor]]
-		+	== References ==
-	==~~Reference~~==	+	<references/>
-	~~<ref group="xtra">PMID:017947383</ref>~~<references ~~group="xtra"~~/><~~references~~/>	+	__TOC__
		+	</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Bourguet, W.]]		[[Category: Bourguet, W.]]

OCA at 02:53, 25 March 2013

2013-03-25T02:53:09Z

←Older revision		Revision as of 02:53, 25 March 2013
Line 1:		Line 1:
-	[[Image:2p1v.png\|left\|200px]]
-
	{{STRUCTURE_2p1v\| PDB=2p1v \| SCENE= }}		{{STRUCTURE_2p1v\| PDB=2p1v \| SCENE= }}
-
	===Crystal structure of the ligand binding domain of the retinoid X receptor alpha in complex with 3-(2'-propoxy)-tetrahydronaphtyl cinnamic acid and a fragment of the coactivator TIF-2===		===Crystal structure of the ligand binding domain of the retinoid X receptor alpha in complex with 3-(2'-propoxy)-tetrahydronaphtyl cinnamic acid and a fragment of the coactivator TIF-2===
		+	{{ABSTRACT_PUBMED_17947383}}

-	~~{{ABSTRACT_PUBMED_17947383}}~~	+	==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==
		+	[[http://www.uniprot.org/uniprot/RXRA_HUMAN RXRA_HUMAN]] Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. The high affinity ligand for RXRs is 9-cis retinoic acid. RXRA serves as a common heterodimeric partner for a number of nuclear receptors. The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone acetylation, chromatin condensation and transcriptional suppression. On ligand binding, the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation. The RXRA/PPARA heterodimer is required for PPARA transcriptional activity on fatty acid oxidation genes such as ACOX1 and the P450 system genes.<ref>PMID:10195690</ref><ref>PMID:11162439</ref><ref>PMID:11915042</ref><ref>PMID:20215566</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==		==About this Structure==
Line 14:		Line 16:

	==Reference==		==Reference==
-	<ref group="xtra">PMID:017947383</ref><references group="xtra"/>	+	<ref group="xtra">PMID:017947383</ref><references group="xtra"/><references/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Bourguet, W.]]		[[Category: Bourguet, W.]]

OCA: Protected "2p1v" [edit=sysop:move=sysop]

2012-10-20T17:01:16Z

Protected "2p1v" [edit=sysop:move=sysop]

←Older revision

Revision as of 17:01, 20 October 2012

OCA at 17:01, 20 October 2012

2012-10-20T17:01:14Z

←Older revision		Revision as of 17:01, 20 October 2012
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-	{{Seed}}
	[[Image:2p1v.png\|left\|200px]]		[[Image:2p1v.png\|left\|200px]]

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	{{STRUCTURE_2p1v\| PDB=2p1v \| SCENE= }}		{{STRUCTURE_2p1v\| PDB=2p1v \| SCENE= }}

	===Crystal structure of the ligand binding domain of the retinoid X receptor alpha in complex with 3-(2'-propoxy)-tetrahydronaphtyl cinnamic acid and a fragment of the coactivator TIF-2===		===Crystal structure of the ligand binding domain of the retinoid X receptor alpha in complex with 3-(2'-propoxy)-tetrahydronaphtyl cinnamic acid and a fragment of the coactivator TIF-2===

-
-	<!--
-	The line below this paragraph, {{ABSTRACT_PUBMED_17947383}}, adds the Publication Abstract to the page
-	(as it appears on PubMed at http://www.pubmed.gov), where 17947383 is the PubMed ID number.
-	-->
	{{ABSTRACT_PUBMED_17947383}}		{{ABSTRACT_PUBMED_17947383}}

	==About this Structure==		==About this Structure==
-	~~2P1V~~ is a 2 ~~chains~~ structure ~~of sequences~~ 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=2P1V OCA].	+	[[2p1v]] 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=2P1V OCA].
		+
		+	==See Also==
		+	*[[Retinoid X receptor\|Retinoid X receptor]]

	==Reference==		==Reference==
-	<ref group="xtra">PMID:~~17947383~~</ref><references group="xtra"/>	+	<ref group="xtra">PMID:017947383</ref><references group="xtra"/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Bourguet, W.]]		[[Category: Bourguet, W.]]
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	[[Category: Hormone receptor]]		[[Category: Hormone receptor]]
	[[Category: Protein-ligand complex]]		[[Category: Protein-ligand complex]]
-
-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Feb 17 16:56:13 2009''

OCA at 14:56, 17 February 2009

2009-02-17T14:56:13Z

←Older revision		Revision as of 14:56, 17 February 2009
Line 20:		Line 20:

	==About this Structure==		==About this Structure==
-	2P1V is a ~~[[Protein complex]]~~ structure of sequences 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=2P1V OCA].	+	2P1V is a 2 chains structure of sequences 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=2P1V OCA].

	==Reference==		==Reference==
-	Modulators of the structural dynamics of the retinoid X receptor to reveal receptor function., Nahoum V, Perez E, Germain P, Rodriguez-Barrios F, Manzo F, Kammerer S, Lemaire G, Hirsch O, Royer CA, Gronemeyer H, de Lera AR, Bourguet W, Proc Natl Acad Sci U S A. 2007 Oct 30;104(44):17323-8. Epub 2007 Oct 18. PMID:~~[http:~~//~~www.ncbi.nlm.nih.gov/pubmed/17947383 17947383]~~	+	<ref group="xtra">PMID:17947383</ref><references group="xtra"/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
-	[[Category: Protein complex]]
	[[Category: Bourguet, W.]]		[[Category: Bourguet, W.]]
	[[Category: Nahoum, V.]]		[[Category: Nahoum, V.]]
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	[[Category: Protein-ligand complex]]		[[Category: Protein-ligand complex]]

-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Mon Jul 28 23~~:45:~~14 2008~~''	+	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Feb 17 16:56:13 2009''

OCA at 20:45, 28 July 2008

2008-07-28T20:45:18Z

←Older revision		Revision as of 20:45, 28 July 2008
Line 1:		Line 1:
-	[[Image:2p1v.~~jpg~~\|left\|200px]]	+	{{Seed}}
		+	[[Image:2p1v.png\|left\|200px]]

	<!--		<!--
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	{{STRUCTURE_2p1v\| PDB=2p1v \| SCENE= }}		{{STRUCTURE_2p1v\| PDB=2p1v \| SCENE= }}

-	~~'''~~Crystal structure of the ligand binding domain of the retinoid X receptor alpha in complex with 3-(2'-propoxy)-tetrahydronaphtyl cinnamic acid and a fragment of the coactivator TIF-2~~'''~~	+	===Crystal structure of the ligand binding domain of the retinoid X receptor alpha in complex with 3-(2'-propoxy)-tetrahydronaphtyl cinnamic acid and a fragment of the coactivator TIF-2===


-	~~==Overview==~~	+	<!--
-	~~Retinoid X receptors (RXRalpha~~, ~~-beta~~, ~~and -gamma) occupy a central position in~~ the ~~nuclear receptor superfamily, because they form heterodimers with many other family members and hence are involved in~~ the ~~control of a variety of~~ (~~patho)physiologic processes. Selective RXR ligands, referred to~~ as ~~rexinoids, are already used or are being developed for cancer therapy and have promise for the treatment of metabolic diseases~~. ~~However~~, ~~important side effects remain associated with existing rexinoids. Here we describe~~ the rational design and functional characterization of a spectrum of RXR modulators ranging from partial to pure antagonists and demonstrate their utility as tools to probe the implication of RXRs in cell biological phenomena. ~~One of these ligands renders RXR activity particularly sensitive to coactivator levels and has the potential to act as a cell~~-~~specific RXR modulator. A combination of crystallographic and fluorescence anisotropy studies reveals the molecular details accounting for the agonist~~-to-antagonist transition and provides direct experimental evidence for a correlation between the pharmacological activity of a ligand and its impact on the structural dynamics of the activation helix H12. Using RXR and its cognate ligands as a model system, our correlative analysis of 3D structures and dynamic data provides an original view on ligand actions and enables the establishment of mechanistic concepts, which will aid in the development of selective nuclear receptor modulators.	+	The line below this paragraph, {{ABSTRACT_PUBMED_17947383}}, adds the Publication Abstract to the page
		+	(as it appears on PubMed at http://www.pubmed.gov), where 17947383 is the PubMed ID number.
		+	-->
		+	{{ABSTRACT_PUBMED_17947383}}

	==About this Structure==		==About this Structure==
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	[[Category: Hormone receptor]]		[[Category: Hormone receptor]]
	[[Category: Protein-ligand complex]]		[[Category: Protein-ligand complex]]
-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sun May 4 12~~:10:02 2008''	+
		+	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 23:45:14 2008''

OCA at 09:10, 4 May 2008

2008-05-04T09:10:04Z

←Older revision		Revision as of 09:10, 4 May 2008
Line 1:		Line 1:
	[[Image:2p1v.jpg\|left\|200px]]		[[Image:2p1v.jpg\|left\|200px]]

-	~~{{Structure~~	+	<!--
-	~~\|PDB= 2p1v \|SIZE=350\|CAPTION= <scene name='initialview01'>2p1v</scene>~~, ~~resolution 2~~.~~200Å~~	+	The line below this paragraph, containing "STRUCTURE_2p1v", creates the "Structure Box" on the page.
-	~~\|SITE=~~	+	You may change the PDB parameter (which sets the PDB file loaded into the applet)
-	~~\|LIGAND= <scene name='pdbligand=5TN:~~(2E)~~-3-[4-HYDROXY-3-~~(~~5,5,8,8-TETRAMETHYL-3-PROPOXY-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)PHENYL]ACRYLIC+ACID'>5TN</~~scene>	+	or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-	~~\|ACTIVITY=~~	+	or leave the SCENE parameter empty for the default display.
-	~~\|GENE= RXRA, NR2B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]~~)	+	-->
-	~~\|DOMAIN=~~	+	{{STRUCTURE_2p1v\| PDB=2p1v \| SCENE= }}
-	~~\|RELATEDENTRY=[[1lbd\|1LBD]]~~, ~~[[1fby\|1FBY]], [[1mvc\|1MVC]], [[1xdk\|1XDK]]~~	+
-	~~\|RESOURCES=<span class='plainlinks'>[http://oca~~.~~weizmann.ac.il/oca~~-~~docs/fgij/fg.htm?mol=2p1v FirstGlance], [http://oca.weizmann.ac.il/oca~~-~~bin/ocaids?id~~=2p1v ~~OCA], [http://www.ebi.ac.uk/pdbsum/2p1v PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId~~=~~2p1v RCSB]</span>~~	+
-	}}	+

	'''Crystal structure of the ligand binding domain of the retinoid X receptor alpha in complex with 3-(2'-propoxy)-tetrahydronaphtyl cinnamic acid and a fragment of the coactivator TIF-2'''		'''Crystal structure of the ligand binding domain of the retinoid X receptor alpha in complex with 3-(2'-propoxy)-tetrahydronaphtyl cinnamic acid and a fragment of the coactivator TIF-2'''
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	[[Category: Bourguet, W.]]		[[Category: Bourguet, W.]]
	[[Category: Nahoum, V.]]		[[Category: Nahoum, V.]]
-	[[Category: ~~hormone~~ receptor]]	+	[[Category: Hormone receptor]]
-	[[Category: ~~protein~~-ligand complex]]	+	[[Category: Protein-ligand complex]]
-		+	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 12:10:02 2008''
-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Mon Mar 31 04~~:27:22 2008''	+

OCA at 01:27, 31 March 2008

2008-03-31T01:27:23Z

←Older revision		Revision as of 01:27, 31 March 2008
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	\|PDB= 2p1v \|SIZE=350\|CAPTION= <scene name='initialview01'>2p1v</scene>, resolution 2.200Å		\|PDB= 2p1v \|SIZE=350\|CAPTION= <scene name='initialview01'>2p1v</scene>, resolution 2.200Å
	\|SITE=		\|SITE=
-	\|LIGAND= <scene name='pdbligand=5TN:(2E)-3-[4-HYDROXY-3-(5,5,8,8-TETRAMETHYL-3-PROPOXY-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)PHENYL]ACRYLIC ACID'>5TN</scene>	+	\|LIGAND= <scene name='pdbligand=5TN:(2E)-3-[4-HYDROXY-3-(5,5,8,8-TETRAMETHYL-3-PROPOXY-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)PHENYL]ACRYLIC+ACID'>5TN</scene>
	\|ACTIVITY=		\|ACTIVITY=
	\|GENE= RXRA, NR2B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])		\|GENE= RXRA, NR2B1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
		+	\|DOMAIN=
		+	\|RELATEDENTRY=[[1lbd\|1LBD]], [[1fby\|1FBY]], [[1mvc\|1MVC]], [[1xdk\|1XDK]]
		+	\|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2p1v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p1v OCA], [http://www.ebi.ac.uk/pdbsum/2p1v PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2p1v RCSB]</span>
	}}		}}

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	[[Category: Bourguet, W.]]		[[Category: Bourguet, W.]]
	[[Category: Nahoum, V.]]		[[Category: Nahoum, V.]]
-	[[Category: 5TN]]
	[[Category: hormone receptor]]		[[Category: hormone receptor]]
	[[Category: protein-ligand complex]]		[[Category: protein-ligand complex]]

-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Thu~~ Mar ~~20 18~~:07:28 2008''	+	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:27:22 2008''