1k74

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[[Image:1k74.png|left|200px]]
 
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{{STRUCTURE_1k74| PDB=1k74 | SCENE= }}
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==The 2.3 Angstrom resolution crystal structure of the heterodimer of the human PPARgamma and RXRalpha ligand binding domains respectively bound with GW409544 and 9-cis retinoic acid and co-activator peptides.==
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<StructureSection load='1k74' size='340' side='right'caption='[[1k74]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
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===The 2.3 Angstrom resolution crystal structure of the heterodimer of the human PPARgamma and RXRalpha ligand binding domains respectively bound with GW409544 and 9-cis retinoic acid and co-activator peptides.===
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== Structural highlights ==
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<table><tr><td colspan='2'>[[1k74]] 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=1K74 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1K74 FirstGlance]. <br>
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{{ABSTRACT_PUBMED_11698662}}
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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]] 2.3&#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=544:2-(1-METHYL-3-OXO-3-PHENYL-PROPYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC+ACID'>544</scene>, <scene name='pdbligand=9CR:(9CIS)-RETINOIC+ACID'>9CR</scene></td></tr>
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==About this Structure==
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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=1k74 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1k74 OCA], [https://pdbe.org/1k74 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1k74 RCSB], [https://www.ebi.ac.uk/pdbsum/1k74 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1k74 ProSAT]</span></td></tr>
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[[1k74]] 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=1K74 OCA].
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</table>
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== Function ==
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[https://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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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/k7/1k74_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</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/main_output.php?pdb_ID=1k74 ConSurf].
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<div style="clear:both"></div>
==See Also==
==See Also==
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*[[Peroxisome Proliferator-Activated Receptors|Peroxisome Proliferator-Activated Receptors]]
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*[[Peroxisome proliferator-activated receptor 3D structures|Peroxisome proliferator-activated receptor 3D structures]]
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*[[Retinoid X receptor|Retinoid X receptor]]
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*[[Retinoid X receptor 3D structures|Retinoid X receptor 3D structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:011698662</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Collins, J L.]]
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[[Category: Large Structures]]
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[[Category: Gampe, R T.]]
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[[Category: Collins JL]]
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[[Category: Kliewer, S A.]]
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[[Category: Gampe Jr RT]]
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[[Category: Lambert, M H.]]
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[[Category: Kliewer SA]]
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[[Category: McKee, D D.]]
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[[Category: Lambert MH]]
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[[Category: Montana, V G.]]
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[[Category: McKee DD]]
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[[Category: Moore, J T.]]
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[[Category: Montana VG]]
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[[Category: Moore, L B.]]
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[[Category: Moore JT]]
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[[Category: Oplinger, J A.]]
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[[Category: Moore LB]]
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[[Category: Willson, T M.]]
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[[Category: Oplinger JA]]
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[[Category: Xu, H E.]]
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[[Category: Willson TM]]
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[[Category: The heterodimer of the nuclear receptor ligand binding domains of rxralpha and ppargamma bound respectively with 9-cis retinoic acid and gw409544 and coactivator peptide]]
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[[Category: Xu HE]]
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[[Category: Transcription]]
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Current revision

The 2.3 Angstrom resolution crystal structure of the heterodimer of the human PPARgamma and RXRalpha ligand binding domains respectively bound with GW409544 and 9-cis retinoic acid and co-activator peptides.

PDB ID 1k74

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Proteopedia Page Contributors and Editors (what is this?)

OCA

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