9b2b

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Current revision (07:02, 27 August 2025) (edit) (undo)
 
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'''Unreleased structure'''
 
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The entry 9b2b is ON HOLD until Paper Publication
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==Estrogen Receptor Alpha Ligand Binding Domain in Complex with a Complete Estrogen Receptor Antagonists that Favors Tetramer Formation==
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<StructureSection load='9b2b' size='340' side='right'caption='[[9b2b]], [[Resolution|resolution]] 2.08&Aring;' scene=''>
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Authors: Fink, E.C., Chawla, R., Wells, K.S., Barratt, S., Myles, D.C., Pena, G., Robello, B.W., Ng, R., Fanning, S.W.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[9b2b]] 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=9B2B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=9B2B FirstGlance]. <br>
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Description: Estrogen Receptor Alpha Ligand Binding Domain in Complex with a Complete Estrogen Receptor Antagonists that Favors Tetramer Formation
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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]] 2.08&#8491;</td></tr>
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[[Category: Unreleased Structures]]
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A1AI0:2-chloro-3-{[{[1-(2-fluorophenyl)cyclopentyl]methyl}(4-{[1-(3-fluoropropyl)azetidin-3-yl]oxy}phenyl)amino]methyl}phenol'>A1AI0</scene></td></tr>
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[[Category: Myles, D.C]]
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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=9b2b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=9b2b OCA], [https://pdbe.org/9b2b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=9b2b RCSB], [https://www.ebi.ac.uk/pdbsum/9b2b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=9b2b ProSAT]</span></td></tr>
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[[Category: Chawla, R]]
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</table>
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[[Category: Fink, E.C]]
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== Function ==
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[[Category: Pena, G]]
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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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[[Category: Ng, R]]
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== References ==
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[[Category: Robello, B.W]]
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<references/>
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[[Category: Barratt, S]]
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__TOC__
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[[Category: Fanning, S.W]]
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</StructureSection>
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[[Category: Wells, K.S]]
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Barratt S]]
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[[Category: Chawla R]]
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[[Category: Fanning SW]]
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[[Category: Fink EC]]
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[[Category: Myles DC]]
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[[Category: Ng R]]
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[[Category: Pena G]]
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[[Category: Robello BW]]
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[[Category: Wells KS]]

Current revision

Estrogen Receptor Alpha Ligand Binding Domain in Complex with a Complete Estrogen Receptor Antagonists that Favors Tetramer Formation

PDB ID 9b2b

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