2yja

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[[Image:2yja.jpg|left|200px]]
 
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==Stapled Peptides binding to Estrogen Receptor alpha.==
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The line below this paragraph, containing "STRUCTURE_2yja", creates the "Structure Box" on the page.
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<StructureSection load='2yja' size='340' side='right'caption='[[2yja]], [[Resolution|resolution]] 1.82&Aring;' scene=''>
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[2yja]] 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=2YJA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2YJA FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.82&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=EST:ESTRADIOL'>EST</scene>, <scene name='pdbligand=MK8:2-METHYL-L-NORLEUCINE'>MK8</scene>, <scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene></td></tr>
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{{STRUCTURE_2yja| PDB=2yja | SCENE= }}
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<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>
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</table>
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== Function ==
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[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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Synthetic peptides that specifically bind nuclear hormone receptors offer an alternative approach to small molecules for the modulation of receptor signaling and subsequent gene expression. Here we describe the design of a series of novel stapled peptides that bind the coactivator peptide site of estrogen receptors. Using a number of biophysical techniques, including crystal structure analysis of receptor-stapled peptide complexes, we describe in detail the molecular interactions and demonstrate that all-hydrocarbon staples modulate molecular recognition events. The findings have implications for the design of stapled peptides in general.
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===STAPLED PEPTIDES BINDING TO ESTROGEN RECEPTOR ALPHA.===
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Design and structure of stapled peptides binding to estrogen receptors.,Phillips C, Roberts LR, Schade M, Bazin R, Bent A, Davies NL, Moore R, Pannifer AD, Pickford AR, Prior SH, Read CM, Scott A, Brown DG, Xu B, Irving SL J Am Chem Soc. 2011 Jun 29;133(25):9696-9. Epub 2011 Jun 6. PMID:21612236<ref>PMID:21612236</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 2yja" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_21612236}}, adds the Publication Abstract to the page
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*[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 21612236 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_21612236}}
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__TOC__
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</StructureSection>
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==About this Structure==
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[[2yja]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2YJA OCA].
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==Reference==
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<ref group="xtra">PMID:021612236</ref><references group="xtra"/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Bazin, R.]]
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[[Category: Large Structures]]
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[[Category: Bent, A.]]
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[[Category: Bazin R]]
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[[Category: Brown, D G.]]
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[[Category: Bent A]]
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[[Category: Davies, N L.]]
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[[Category: Brown DG]]
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[[Category: Irving, S L.]]
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[[Category: Davies NL]]
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[[Category: Moore, R.]]
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[[Category: Irving SL]]
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[[Category: Pannifer, A D.]]
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[[Category: Moore R]]
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[[Category: Phillips, C.]]
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[[Category: Pannifer AD]]
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[[Category: Pickford, A R.]]
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[[Category: Phillips C]]
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[[Category: Roberts, L R.]]
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[[Category: Pickford AR]]
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[[Category: Schade, M.]]
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[[Category: Roberts LR]]
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[[Category: Scott, A.]]
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[[Category: Schade M]]
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[[Category: Xu, B.]]
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[[Category: Scott A]]
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[[Category: Hormone receptor-peptide complex]]
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[[Category: Xu B]]

Current revision

Stapled Peptides binding to Estrogen Receptor alpha.

PDB ID 2yja

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