8vv1

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Current revision (06:24, 19 March 2025) (edit) (undo)
 
Line 1: Line 1:
-
'''Unreleased structure'''
 
-
The entry 8vv1 is ON HOLD until Paper Publication
+
==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:(1~{R},3~{R})-2-(2-fluoranyl-2-methyl-propyl)-3-methyl-1-[4-(1-propylazetidin-3-yl)oxyphenyl]-1,3,4,9-tetrahydropyrido[3,4-b]indole'>A1AEA</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr>
-
[[Category: Hodges-Gallagher, L]]
+
<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: Parisian, A]]
+
</table>
-
[[Category: Chawla, R]]
+
== Function ==
-
[[Category: Yeghikyan, D]]
+
[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: Pena, G]]
+
== References ==
-
[[Category: Kushner, P.J]]
+
<references/>
-
[[Category: Hearn, B]]
+
__TOC__
-
[[Category: Robello, B]]
+
</StructureSection>
-
[[Category: Greene, G.L]]
+
[[Category: Homo sapiens]]
-
[[Category: Myles, D.C]]
+
[[Category: Large Structures]]
-
[[Category: Ng, R.A]]
+
[[Category: Andersen SE]]
-
[[Category: Rich, B]]
+
[[Category: Barratt S]]
-
[[Category: Sapugay, J]]
+
[[Category: Chawla R]]
-
[[Category: Barratt, S]]
+
[[Category: Duncan A]]
-
[[Category: Fanning, S.W]]
+
[[Category: Fanning SW]]
-
[[Category: Sun, R]]
+
[[Category: Greene GL]]
-
[[Category: Andersen, S.E]]
+
[[Category: Harmon C]]
-
[[Category: Harmon, C]]
+
[[Category: Hearn B]]
-
[[Category: Palanisamy, G]]
+
[[Category: Hodges-Gallagher L]]
-
[[Category: Duncan, A]]
+
[[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]]

Current revision

Estrogen receptor alpha ligand binding domain in complex with palazestrant

PDB ID 8vv1

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/8vv1"
Personal tools