5y7w

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m (Protected "5y7w" [edit=sysop:move=sysop])
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'''Unreleased structure'''
 
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The entry 5y7w is ON HOLD until Paper Publication
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==Crystal structure of the Nco-A1 PAS-B domain with YL-2==
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<StructureSection load='5y7w' size='340' side='right' caption='[[5y7w]], [[Resolution|resolution]] 2.25&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5y7w]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5Y7W OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5Y7W FirstGlance]. <br>
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</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ALC:2-AMINO-3-CYCLOHEXYL-PROPIONIC+ACID'>ALC</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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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span></td></tr>
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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=5y7w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5y7w OCA], [http://pdbe.org/5y7w PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5y7w RCSB], [http://www.ebi.ac.uk/pdbsum/5y7w PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5y7w ProSAT]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/NCOA1_MOUSE NCOA1_MOUSE]] Nuclear receptor coactivator that directly binds nuclear receptors and stimulates the transcriptional activities in a hormone-dependent fashion. Involved in the coactivation of different nuclear receptors, such as for steroids (PGR, GR and ER), retinoids (RXRs), thyroid hormone (TRs) and prostanoids (PPARs). Also involved in coactivation mediated by STAT3, STAT5A, STAT5B and STAT6 transcription factors. Displays histone acetyltransferase activity toward H3 and H4; the relevance of such activity remains however unclear. Plays a central role in creating multisubunit coactivator complexes that act via remodeling of chromatin, and possibly acts by participating in both chromatin remodeling and recruitment of general transcription factors. Required with NCOA2 to control energy balance between white and brown adipose tissues. Required for mediating steroid hormone response. Isoform 2 has a higher thyroid hormone-dependent transactivation activity than isoform 1 and isoform 3.<ref>PMID:8616895</ref> <ref>PMID:9506940</ref> <ref>PMID:12507421</ref> <ref>PMID:16148126</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The complex formation between transcription factors (TFs) and coactivator proteins is required for transcriptional activity, and thus disruption of aberrantly activated TF/coactivator interactions could be an attractive therapeutic strategy. However, modulation of such protein-protein interactions (PPIs) has proven challenging. Here we report a cell-permeable, proteolytically stable, stapled helical peptide directly targeting nuclear receptor coactivator 1 (NCOA1), a coactivator required for the transcriptional activity of signal transducer and activator of transcription 6 (STAT6). We demonstrate that this stapled peptide disrupts the NCOA1/STAT6 complex, thereby repressing STAT6-mediated transcription. Furthermore, we solved the first crystal structure of a stapled peptide in complex with NCOA1. The stapled peptide therefore represents an invaluable chemical probe for understanding the precise role of the NCOA1/STAT6 interaction and an excellent starting point for the development of a novel class of therapeutic agents.
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Authors:
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Targeted Inhibition of the NCOA1/STAT6 Protein-Protein Interaction.,Lee Y, Yoon H, Hwang SM, Shin MK, Lee JH, Oh M, Im SH, Song J, Lim HS J Am Chem Soc. 2017 Nov 1. doi: 10.1021/jacs.7b08972. PMID:29090910<ref>PMID:29090910</ref>
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Description:
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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<div class="pdbe-citations 5y7w" style="background-color:#fffaf0;"></div>
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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: Histone acetyltransferase]]
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[[Category: Bae, J H]]
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[[Category: Lee, J H]]
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[[Category: Lee, Y J]]
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[[Category: Lim, H S]]
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[[Category: Song, J Y]]
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[[Category: Yoon, H S]]
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[[Category: Inflammatory allergic diseases and cancer]]
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[[Category: Nuclear receptor coactivator 1]]
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[[Category: Stapled peptide]]
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[[Category: Transcription-inihibitor complex]]

Revision as of 07:38, 15 November 2017

Crystal structure of the Nco-A1 PAS-B domain with YL-2

5y7w, resolution 2.25Å

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