6dfn

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(New page: '''Unreleased structure''' The entry 6dfn is ON HOLD Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Zhang, B., Ortwine, D.F., Nettles, K.W., Nwachukwu, J.C. Description: Crystal st...)
Current revision (14:33, 13 March 2024) (edit) (undo)
 
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'''Unreleased structure'''
 
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The entry 6dfn is ON HOLD
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==Crystal structure of estrogen receptor alpha in complex with receptor degrader 16aa==
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<StructureSection load='6dfn' size='340' side='right'caption='[[6dfn]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6dfn]] 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=6DFN OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6DFN 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]] 2.1&#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=G91:(8S)-8-(4-{2-[3-(fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-1,8-dihydro-2H-[1]benzopyrano[4,3-d][1]benzoxepine-5,11-diol'>G91</scene>, <scene name='pdbligand=G9J:(2S)-3-(3-hydroxyphenyl)-2-(4-iodophenyl)-4-methyl-2H-1-benzopyran-6-ol'>G9J</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</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=6dfn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dfn OCA], [https://pdbe.org/6dfn PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6dfn RCSB], [https://www.ebi.ac.uk/pdbsum/6dfn PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6dfn ProSAT]</span></td></tr>
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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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Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Zhang, B., Ortwine, D.F., Nettles, K.W., Nwachukwu, J.C.
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==See Also==
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*[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]]
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Description: Crystal structure of estrogen receptor alpha in complex with receptor degrader 16ab
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== References ==
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[[Category: Unreleased Structures]]
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<references/>
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[[Category: Zhang, B]]
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__TOC__
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[[Category: Nwachukwu, J.C]]
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</StructureSection>
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[[Category: Ortwine, D.F]]
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[[Category: Homo sapiens]]
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[[Category: Kiefer, J.R]]
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[[Category: Large Structures]]
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[[Category: Liang, J]]
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[[Category: Kiefer JR]]
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[[Category: Nettles, K.W]]
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[[Category: Liang J]]
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[[Category: Vinogradova, M]]
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[[Category: Nettles KW]]
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[[Category: Nwachukwu JC]]
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[[Category: Ortwine DF]]
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[[Category: Vinogradova M]]
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[[Category: Zhang B]]

Current revision

Crystal structure of estrogen receptor alpha in complex with receptor degrader 16aa

PDB ID 6dfn

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