4xi3

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'''Unreleased structure'''
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==Estrogen Receptor Alpha Ligand Binding Domain in Complex with Bazedoxifene==
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<StructureSection load='4xi3' size='340' side='right' caption='[[4xi3]], [[Resolution|resolution]] 2.49&Aring;' scene=''>
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The entry 4xi3 is ON HOLD until Jan 13 2017
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4xi3]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4XI3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4XI3 FirstGlance]. <br>
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Authors: Fanning, S.W., Mayne, C.G., Toy, W., Carlson, K., Greene, B., Nowak, J., Walter, R., Panchamukhi, S., Tajhorshid, E., Nettles, K.W., Chandarlapaty, S., Katzenellenbogen, J., Greene, G.L.
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=29S:BAZEDOXIFENE'>29S</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4xi3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xi3 OCA], [http://pdbe.org/4xi3 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4xi3 RCSB], [http://www.ebi.ac.uk/pdbsum/4xi3 PDBsum]</span></td></tr>
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Description: Estrogen Receptor Alpha Ligand Binding Domain in Complex with Bazedoxifene
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</table>
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[[Category: Unreleased Structures]]
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== Function ==
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[[http://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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== References ==
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<references/>
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__TOC__
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</StructureSection>
[[Category: Carlson, K]]
[[Category: Carlson, K]]
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[[Category: Katzenellenbogen, J]]
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[[Category: Chandarlapaty, S]]
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[[Category: Fanning, S W]]
[[Category: Greene, B]]
[[Category: Greene, B]]
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[[Category: Greene, G.L]]
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[[Category: Greene, G L]]
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[[Category: Fanning, S.W]]
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[[Category: Katzenellenbogen, J]]
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[[Category: Mayne, C.G]]
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[[Category: Mayne, C G]]
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[[Category: Tajhorshid, E]]
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[[Category: Nettles, K W]]
[[Category: Nowak, J]]
[[Category: Nowak, J]]
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[[Category: Nettles, K.W]]
 
[[Category: Panchamukhi, S]]
[[Category: Panchamukhi, S]]
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[[Category: Chandarlapaty, S]]
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[[Category: Tajhorshid, E]]
[[Category: Toy, W]]
[[Category: Toy, W]]
[[Category: Walter, R]]
[[Category: Walter, R]]
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[[Category: Bazedoxifene]]
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[[Category: Breast cancer]]
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[[Category: Estrogen receptor]]
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[[Category: Nuclear hormone receptor]]
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[[Category: Serm]]
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[[Category: Signaling protein]]

Revision as of 20:22, 13 January 2016

Estrogen Receptor Alpha Ligand Binding Domain in Complex with Bazedoxifene

4xi3, resolution 2.49Å

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