2qa6

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[[Image:2qa6.png|left|200px]]
 
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{{STRUCTURE_2qa6| PDB=2qa6 | SCENE= }}
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==Crystal Structure of Estrogen Receptor Alpha mutant 537S Complexed with 4-(6-hydroxy-1H-indazol-3-yl)benzene-1,3-diol==
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<StructureSection load='2qa6' size='340' side='right'caption='[[2qa6]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
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===Crystal Structure of Estrogen Receptor Alpha mutant 537S Complexed with 4-(6-hydroxy-1H-indazol-3-yl)benzene-1,3-diol===
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2qa6]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2QA6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2QA6 FirstGlance]. <br>
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{{ABSTRACT_PUBMED_18344977}}
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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]] 2.6&#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=KN2:4-(6-HYDROXY-1H-INDAZOL-3-YL)BENZENE-1,3-DIOL'>KN2</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=2qa6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2qa6 OCA], [https://pdbe.org/2qa6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2qa6 RCSB], [https://www.ebi.ac.uk/pdbsum/2qa6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2qa6 ProSAT]</span></td></tr>
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[[2qa6]] is a 4 chain structure of [[Estrogen receptor]] 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=2QA6 OCA].
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/ESR1_HUMAN ESR1_HUMAN] Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full length receptor. Isoform 3 can bind to ERE and inhibit isoform 1.<ref>PMID:7651415</ref> <ref>PMID:10970861</ref> <ref>PMID:9328340</ref> <ref>PMID:10681512</ref> <ref>PMID:10816575</ref> <ref>PMID:11477071</ref> <ref>PMID:11682626</ref> <ref>PMID:15078875</ref> <ref>PMID:16043358</ref> <ref>PMID:15891768</ref> <ref>PMID:16684779</ref> <ref>PMID:18247370</ref> <ref>PMID:17932106</ref> <ref>PMID:19350539</ref> <ref>PMID:20705611</ref> <ref>PMID:21937726</ref> <ref>PMID:21330404</ref> <ref>PMID:22083956</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/qa/2qa6_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=2qa6 ConSurf].
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<div style="clear:both"></div>
==See Also==
==See Also==
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*[[Estrogen receptor|Estrogen receptor]]
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*[[Estrogen receptor 3D structures|Estrogen 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:018344977</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: Bruning, J B.]]
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[[Category: Large Structures]]
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[[Category: Greene, G L.]]
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[[Category: Mus musculus]]
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[[Category: Hahm, J B.]]
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[[Category: Bruning JB]]
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[[Category: Hochberg, R B.]]
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[[Category: Greene GL]]
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[[Category: Joachmiak, A.]]
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[[Category: Hahm JB]]
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[[Category: Katzenellenbogen, B S.]]
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[[Category: Hochberg RB]]
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[[Category: Katzenellenbogen, J A.]]
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[[Category: Joachmiak A]]
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[[Category: Kim, Y.]]
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[[Category: Katzenellenbogen BS]]
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[[Category: Kulp, K.]]
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[[Category: Katzenellenbogen JA]]
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[[Category: Nettles, K W.]]
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[[Category: Kim Y]]
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[[Category: Nowak, J.]]
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[[Category: Kulp K]]
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[[Category: Sharma, S K.]]
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[[Category: Nettles KW]]
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[[Category: Shi, Y.]]
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[[Category: Nowak J]]
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[[Category: Zhou, H.]]
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[[Category: Sharma SK]]
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[[Category: Protein-ligand complex]]
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[[Category: Shi Y]]
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[[Category: Transcription]]
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[[Category: Zhou H]]

Current revision

Crystal Structure of Estrogen Receptor Alpha mutant 537S Complexed with 4-(6-hydroxy-1H-indazol-3-yl)benzene-1,3-diol

PDB ID 2qa6

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