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6a60

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==Crystal structure of human FXR/RXR-LBD heterodimer bound to GW4064 and 9cRA and SRC1==
==Crystal structure of human FXR/RXR-LBD heterodimer bound to GW4064 and 9cRA and SRC1==
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<StructureSection load='6a60' size='340' side='right' caption='[[6a60]], [[Resolution|resolution]] 3.05&Aring;' scene=''>
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<StructureSection load='6a60' size='340' side='right'caption='[[6a60]], [[Resolution|resolution]] 3.05&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[6a60]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6A60 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6A60 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[6a60]] 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=6A60 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6A60 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=064:3-[(E)-2-(2-CHLORO-4-{[3-(2,6-DICHLOROPHENYL)-5-(1-METHYLETHYL)ISOXAZOL-4-YL]METHOXY}PHENYL)ETHENYL]BENZOIC+ACID'>064</scene>, <scene name='pdbligand=9CR:(9CIS)-RETINOIC+ACID'>9CR</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.05&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6a5w|6a5w]], [[6a5x|6a5x]], [[6a5y|6a5y]], [[6a5z|6a5z]]</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=064:3-[(E)-2-(2-CHLORO-4-{[3-(2,6-DICHLOROPHENYL)-5-(1-METHYLETHYL)ISOXAZOL-4-YL]METHOXY}PHENYL)ETHENYL]BENZOIC+ACID'>064</scene>, <scene name='pdbligand=9CR:(9CIS)-RETINOIC+ACID'>9CR</scene></td></tr>
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<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=6a60 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6a60 OCA], [http://pdbe.org/6a60 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6a60 RCSB], [http://www.ebi.ac.uk/pdbsum/6a60 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6a60 ProSAT]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6a60 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6a60 OCA], [https://pdbe.org/6a60 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6a60 RCSB], [https://www.ebi.ac.uk/pdbsum/6a60 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6a60 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[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/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>
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[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>
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==See Also==
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*[[Bile acid receptor 3D structures|Bile acid receptor 3D structures]]
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*[[Retinoid X receptor 3D structures|Retinoid X receptor 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Liu, J]]
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[[Category: Homo sapiens]]
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[[Category: Wang, N]]
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[[Category: Large Structures]]
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[[Category: Nuclear receptor heterodimer]]
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[[Category: Liu J]]
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[[Category: Transcription]]
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[[Category: Wang N]]

Current revision

Crystal structure of human FXR/RXR-LBD heterodimer bound to GW4064 and 9cRA and SRC1

PDB ID 6a60

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