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'''Unreleased structure'''


The entry 6pfm is ON HOLD
==Crystal structure of GDC-0927 bound to estrogen receptor alpha==
 
<StructureSection load='6pfm' size='340' side='right'caption='[[6pfm]], [[Resolution|resolution]] 2.84&Aring;' scene=''>
Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Zhang, B., Wang, X., Zbieg, J.R., Labadie, S.S., Li, J., Ray, N.C., Ortwine, D.
== Structural highlights ==
 
<table><tr><td colspan='2'>[[6pfm]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6PFM OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6PFM FirstGlance]. <br>
Description: Crystal structure of GDC-0927 bound to estrogen receptor alpha
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=OGJ:(2S)-2-(4-{2-[3-(fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-3-(3-hydroxyphenyl)-4-methyl-2H-1-benzopyran-6-ol'>OGJ</scene></td></tr>
[[Category: Unreleased Structures]]
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6pet|6pet]]</td></tr>
[[Category: Zhang, B]]
<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=6pfm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6pfm OCA], [http://pdbe.org/6pfm PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6pfm RCSB], [http://www.ebi.ac.uk/pdbsum/6pfm PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6pfm ProSAT]</span></td></tr>
[[Category: Labadie, S.S]]
</table>
== Function ==
[[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> 
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Large Structures]]
[[Category: Kiefer, J R]]
[[Category: Labadie, S S]]
[[Category: Li, J]]
[[Category: Liang, J]]
[[Category: Ortwine, D]]
[[Category: Ortwine, D]]
[[Category: Zbieg, J.R]]
[[Category: Ray, N C]]
[[Category: Kiefer, J.R]]
[[Category: Vinogradova, M]]
[[Category: Liang, J]]
[[Category: Ray, N.C]]
[[Category: Li, J]]
[[Category: Wang, X]]
[[Category: Wang, X]]
[[Category: Vinogradova, M]]
[[Category: Zbieg, J R]]
[[Category: Zhang, B]]
[[Category: Antagonist]]
[[Category: Breast cancer]]
[[Category: Ligand]]
[[Category: Nuclear protein]]
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