8vv1: Difference between revisions

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New page: '''Unreleased structure''' The entry 8vv1 is ON HOLD Authors: Ng, R.A., Barratt, S., Parisian, A., Palanisamy, G., Sun, R., Robello, B., Pena, G., Sapugay, J., Yeghikyan, D., Duncan, A....
 
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'''Unreleased structure'''


The entry 8vv1 is ON HOLD
==Estrogen receptor alpha ligand binding domain in complex with palazestrant==
 
<StructureSection load='8vv1' size='340' side='right'caption='[[8vv1]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
Authors: Ng, R.A., Barratt, S., Parisian, A., Palanisamy, G., Sun, R., Robello, B., Pena, G., Sapugay, J., Yeghikyan, D., Duncan, A., Andersen, S.E., Chawla, R., Rich, B., Hearn, B., Harmon, C., Hodges-Gallagher, L., Kushner, P.J., Greene, G.L., Myles, D.C., Fanning, S.W.
== Structural highlights ==
 
<table><tr><td colspan='2'>[[8vv1]] is a 2 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=8VV1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8VV1 FirstGlance]. <br>
Description: Estrogen receptor alpha ligand binding domain in complex with palazestrant
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.196&#8491;</td></tr>
[[Category: Unreleased Structures]]
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A1AEA:(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1-{4-[(1-propylazetidin-3-yl)oxy]phenyl}-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole'>A1AEA</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr>
[[Category: Kushner, P.J]]
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8vv1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8vv1 OCA], [https://pdbe.org/8vv1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8vv1 RCSB], [https://www.ebi.ac.uk/pdbsum/8vv1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8vv1 ProSAT]</span></td></tr>
[[Category: Yeghikyan, D]]
</table>
[[Category: Andersen, S.E]]
== Function ==
[[Category: Pena, G]]
[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>
[[Category: Palanisamy, G]]
== References ==
[[Category: Greene, G.L]]
<references/>
[[Category: Sapugay, J]]
__TOC__
[[Category: Fanning, S.W]]
</StructureSection>
[[Category: Hodges-Gallagher, L]]
[[Category: Homo sapiens]]
[[Category: Chawla, R]]
[[Category: Large Structures]]
[[Category: Harmon, C]]
[[Category: Andersen SE]]
[[Category: Duncan, A]]
[[Category: Barratt S]]
[[Category: Parisian, A]]
[[Category: Chawla R]]
[[Category: Ng, R.A]]
[[Category: Duncan A]]
[[Category: Hearn, B]]
[[Category: Fanning SW]]
[[Category: Rich, B]]
[[Category: Greene GL]]
[[Category: Barratt, S]]
[[Category: Harmon C]]
[[Category: Myles, D.C]]
[[Category: Hearn B]]
[[Category: Robello, B]]
[[Category: Hodges-Gallagher L]]
[[Category: Sun, R]]
[[Category: Kushner PJ]]
[[Category: Myles DC]]
[[Category: Ng RA]]
[[Category: Palanisamy G]]
[[Category: Parisian A]]
[[Category: Pena G]]
[[Category: Rich B]]
[[Category: Robello B]]
[[Category: Sapugay J]]
[[Category: Sun R]]
[[Category: Yeghikyan D]]
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