6pet

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'''Unreleased structure'''
 
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The entry 6pet is ON HOLD until Paper Publication
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==Crystal structure of 8-hydroxychromene compound 30 bound to estrogen receptor alpha==
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<StructureSection load='6pet' size='340' side='right'caption='[[6pet]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
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Authors: Kiefer, J.R., Vinogradova, M., Liang, J., Wang, X., Zbieg, J., Labadie, S.S., Zhang, B., Li, J., Liang, W.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6pet]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6PET OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6PET FirstGlance]. <br>
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Description: Crystal structure of 8-hydroxychromene compound 30 bound to estrogen receptor alpha
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=G9J:(2S)-3-(3-hydroxyphenyl)-2-(4-iodophenyl)-4-methyl-2H-1-benzopyran-6-ol'>G9J</scene>, <scene name='pdbligand=ODY:(2S)-2-(4-{2-[3-(fluoromethyl)azetidin-1-yl]ethoxy}phenyl)-3-(3-hydroxyphenyl)-4-methyl-2H-1-benzopyran-8-ol'>ODY</scene></td></tr>
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[[Category: Unreleased Structures]]
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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=6pet FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6pet OCA], [http://pdbe.org/6pet PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6pet RCSB], [http://www.ebi.ac.uk/pdbsum/6pet PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6pet ProSAT]</span></td></tr>
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[[Category: Zhang, B]]
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</table>
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[[Category: Labadie, S.S]]
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== Function ==
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[[Category: Kiefer, J.R]]
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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>
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[[Category: Large Structures]]
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[[Category: Kiefer, J R]]
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[[Category: Labadie, S S]]
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[[Category: Li, J]]
[[Category: Liang, J]]
[[Category: Liang, J]]
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[[Category: Li, J]]
 
[[Category: Liang, W]]
[[Category: Liang, W]]
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[[Category: Vinogradova, M]]
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[[Category: Wang, X]]
[[Category: Zbieg, J]]
[[Category: Zbieg, J]]
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[[Category: Wang, X]]
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[[Category: Zhang, B]]
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[[Category: Vinogradova, M]]
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[[Category: Antagonist]]
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[[Category: Breast cancer]]
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[[Category: Drug]]
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[[Category: Hormone receptor]]
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[[Category: Ligand]]
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[[Category: Nuclear protein]]

Revision as of 10:49, 17 July 2019

Crystal structure of 8-hydroxychromene compound 30 bound to estrogen receptor alpha

PDB ID 6pet

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