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2qa6
From Proteopedia
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(New page: 200px {{Structure |PDB= 2qa6 |SIZE=350|CAPTION= <scene name='initialview01'>2qa6</scene>, resolution 2.600Å |SITE= <scene name='pdbsite=AC1:Kn2+Binding+Site...) |
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| - | [[Image:2qa6.jpg|left|200px]] | ||
| - | + | ==Crystal Structure of Estrogen Receptor Alpha mutant 537S Complexed with 4-(6-hydroxy-1H-indazol-3-yl)benzene-1,3-diol== | |
| - | + | <StructureSection load='2qa6' size='340' side='right'caption='[[2qa6]], [[Resolution|resolution]] 2.60Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | | | + | <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> |
| - | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.6Å</td></tr> | |
| - | + | <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> | |
| - | + | <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> | |
| + | </table> | ||
| + | == Function == | ||
| + | [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> | ||
| + | == 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/qa/2qa6_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/main_output.php?pdb_ID=2qa6 ConSurf]. | ||
| + | <div style="clear:both"></div> | ||
| - | + | ==See Also== | |
| - | + | *[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]] | |
| - | + | == References == | |
| - | == | + | <references/> |
| - | + | __TOC__ | |
| + | </StructureSection> | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: Bruning | + | [[Category: Mus musculus]] |
| - | [[Category: Greene | + | [[Category: Bruning JB]] |
| - | [[Category: Hahm | + | [[Category: Greene GL]] |
| - | [[Category: Hochberg | + | [[Category: Hahm JB]] |
| - | [[Category: Joachmiak | + | [[Category: Hochberg RB]] |
| - | [[Category: Katzenellenbogen | + | [[Category: Joachmiak A]] |
| - | [[Category: Katzenellenbogen | + | [[Category: Katzenellenbogen BS]] |
| - | [[Category: Kim | + | [[Category: Katzenellenbogen JA]] |
| - | [[Category: Kulp | + | [[Category: Kim Y]] |
| - | [[Category: Nettles | + | [[Category: Kulp K]] |
| - | [[Category: Nowak | + | [[Category: Nettles KW]] |
| - | [[Category: Sharma | + | [[Category: Nowak J]] |
| - | [[Category: Shi | + | [[Category: Sharma SK]] |
| - | [[Category: Zhou | + | [[Category: Shi Y]] |
| - | + | [[Category: Zhou H]] | |
| - | + | ||
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Current revision
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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Categories: Homo sapiens | Large Structures | Mus musculus | Bruning JB | Greene GL | Hahm JB | Hochberg RB | Joachmiak A | Katzenellenbogen BS | Katzenellenbogen JA | Kim Y | Kulp K | Nettles KW | Nowak J | Sharma SK | Shi Y | Zhou H

