2yja
From Proteopedia
(Difference between revisions)
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<StructureSection load='2yja' size='340' side='right'caption='[[2yja]], [[Resolution|resolution]] 1.82Å' scene=''> | <StructureSection load='2yja' size='340' side='right'caption='[[2yja]], [[Resolution|resolution]] 1.82Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[2yja]] is a 2 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[2yja]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2YJA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2YJA FirstGlance]. <br> |
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EST:ESTRADIOL'>EST</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EST:ESTRADIOL'>EST</scene></td></tr> | ||
<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=MK8:2-METHYL-L-NORLEUCINE'>MK8</scene>, <scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene></td></tr> | <tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=MK8:2-METHYL-L-NORLEUCINE'>MK8</scene>, <scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene></td></tr> | ||
| - | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2yat|2yat]], [[1xp1|1xp1]], [[1qkt|1qkt]], [[1r5k|1r5k]], [[1zky|1zky]], [[2bj4|2bj4]], [[1akf|1akf]], [[1hcp|1hcp]], [[1hcq|1hcq]], [[1a52|1a52]], [[1qku|1qku]], [[1g50|1g50]], [[1xp6|1xp6]], [[1pcg|1pcg]], [[2b1v|2b1v]], [[2jf9|2jf9]], [[1uom|1uom]], [[1yim|1yim]], [[2ayr|2ayr]], [[3ert|3ert]], [[1yin|1yin]], [[1err|1err]], [[1x7r|1x7r]], [[3erd|3erd]], [[1l2i|1l2i]], [[1xp9|1xp9]], [[2fai|2fai]], [[1gwr|1gwr]], [[1sj0|1sj0]], [[2jfa|2jfa]], [[1gwq|1gwq]], [[1xpc|1xpc]], [[1x7e|1x7e]], [[1xqc|1xqc]], [[1ere|1ere]], [[2yjd|2yjd]], [[2ldd|2ldd]], [[2lda|2lda]], [[2ldc|2ldc]]</td></tr> | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[2yat|2yat]], [[1xp1|1xp1]], [[1qkt|1qkt]], [[1r5k|1r5k]], [[1zky|1zky]], [[2bj4|2bj4]], [[1akf|1akf]], [[1hcp|1hcp]], [[1hcq|1hcq]], [[1a52|1a52]], [[1qku|1qku]], [[1g50|1g50]], [[1xp6|1xp6]], [[1pcg|1pcg]], [[2b1v|2b1v]], [[2jf9|2jf9]], [[1uom|1uom]], [[1yim|1yim]], [[2ayr|2ayr]], [[3ert|3ert]], [[1yin|1yin]], [[1err|1err]], [[1x7r|1x7r]], [[3erd|3erd]], [[1l2i|1l2i]], [[1xp9|1xp9]], [[2fai|2fai]], [[1gwr|1gwr]], [[1sj0|1sj0]], [[2jfa|2jfa]], [[1gwq|1gwq]], [[1xpc|1xpc]], [[1x7e|1x7e]], [[1xqc|1xqc]], [[1ere|1ere]], [[2yjd|2yjd]], [[2ldd|2ldd]], [[2lda|2lda]], [[2ldc|2ldc]]</div></td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2yja FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2yja OCA], [https://pdbe.org/2yja PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2yja RCSB], [https://www.ebi.ac.uk/pdbsum/2yja PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2yja ProSAT]</span></td></tr> |
</table> | </table> | ||
== Function == | == Function == | ||
| - | [[ | + | [[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> |
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
Revision as of 12:31, 27 April 2022
Stapled Peptides binding to Estrogen Receptor alpha.
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