4j5w

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{{STRUCTURE_4j5w| PDB=4j5w | SCENE= }}
 
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===Crystal Structure of the apo-PXR/RXRalpha LBD Heterotetramer Complex===
 
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{{ABSTRACT_PUBMED_23602807}}
 
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==Function==
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==Crystal Structure of the apo-PXR/RXRalpha LBD Heterotetramer Complex==
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[[http://www.uniprot.org/uniprot/NR1I2_HUMAN NR1I2_HUMAN]] Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and isoflavones. Response to specific ligands is species-specific. Activated by naturally occurring steroids, such as pregnenolone and progesterone. Binds to a response element in the promoters of the CYP3A4 and ABCB1/MDR1 genes.<ref>PMID:9727070</ref> <ref>PMID:11668216</ref> <ref>PMID:11297522</ref> <ref>PMID:19297428</ref> <ref>PMID:12578355</ref> <ref>PMID:18768384</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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<StructureSection load='4j5w' size='340' side='right'caption='[[4j5w]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4j5w]] 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=4J5W OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4J5W FirstGlance]. <br>
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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]] 2.8&#8491;</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=MG:MAGNESIUM+ION'>MG</scene></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=4j5w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4j5w OCA], [https://pdbe.org/4j5w PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4j5w RCSB], [https://www.ebi.ac.uk/pdbsum/4j5w PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4j5w ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/NR1I2_HUMAN NR1I2_HUMAN] Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and isoflavones. Response to specific ligands is species-specific. Activated by naturally occurring steroids, such as pregnenolone and progesterone. Binds to a response element in the promoters of the CYP3A4 and ABCB1/MDR1 genes.<ref>PMID:9727070</ref> <ref>PMID:11668216</ref> <ref>PMID:11297522</ref> <ref>PMID:19297428</ref> <ref>PMID:12578355</ref> <ref>PMID:18768384</ref>
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==About this Structure==
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==See Also==
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[[4j5w]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Gekko_coi Gekko coi] and [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4J5W OCA].
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*[[Pregnane X receptor 3D structures|Pregnane X receptor 3D structures]]
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*[[Retinoid X receptor 3D structures|Retinoid X receptor 3D structures]]
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==Reference==
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== References ==
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<ref group="xtra">PMID:023602807</ref><references group="xtra"/><references/>
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<references/>
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[[Category: Gekko coi]]
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__TOC__
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[[Category: Histone acetyltransferase]]
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Betts, L.]]
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[[Category: Large Structures]]
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[[Category: Redinbo, M R.]]
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[[Category: Betts L]]
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[[Category: Wallace, B D.]]
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[[Category: Redinbo MR]]
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[[Category: Alpha helical sandwich]]
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[[Category: Wallace BD]]
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[[Category: Ligand binding domain]]
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[[Category: Nuclear receptor]]
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[[Category: Pregnane x receptor]]
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[[Category: Retinoic acid-binding protein]]
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[[Category: Retinoid x receptor alpha]]
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[[Category: Unique intermolecular beta-sheet dimerization]]
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[[Category: Upregulation of drug metabolism enzyme]]
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[[Category: Xenobiotic sensing]]
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Current revision

Crystal Structure of the apo-PXR/RXRalpha LBD Heterotetramer Complex

PDB ID 4j5w

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