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6zs4

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'''Unreleased structure'''
 
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The entry 6zs4 is ON HOLD
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==Crystal structure of the fifth bromodomain of human protein polybromo-1 in complex with tert-butyl 4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperazine-1-carboxylate==
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<StructureSection load='6zs4' size='340' side='right'caption='[[6zs4]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6zs4]] is a 1 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=6ZS4 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6ZS4 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]] 2&#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=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=QP8:tert-butyl+4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperazine-1-carboxylate'>QP8</scene></td></tr>
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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=6zs4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6zs4 OCA], [https://pdbe.org/6zs4 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6zs4 RCSB], [https://www.ebi.ac.uk/pdbsum/6zs4 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6zs4 ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/PB1_HUMAN PB1_HUMAN] Defects in PBRM1 are a cause of renal cell carcinoma (RCC) [MIM:[https://omim.org/entry/144700 144700]. It is a heterogeneous group of sporadic or hereditary carcinoma derived from cells of the proximal renal tubular epithelium. It is subclassified into clear cell renal carcinoma (non-papillary carcinoma), papillary renal cell carcinoma, chromophobe renal cell carcinoma, collecting duct carcinoma with medullary carcinoma of the kidney, and unclassified renal cell carcinoma.<ref>PMID:21248752</ref>
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== Function ==
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[https://www.uniprot.org/uniprot/PB1_HUMAN PB1_HUMAN] Involved in transcriptional activation and repression of select genes by chromatin remodeling (alteration of DNA-nucleosome topology). Acts as a negative regulator of cell proliferation.<ref>PMID:21248752</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Accessibility of the human genome is modulated by the ATP-driven SWI/SNF chromatin remodeling multiprotein complexes BAF (BRG1/BRM-associated factor) and PBAF (polybromo-associated BAF factor), which involves reading of acetylated histone tails by the bromodomain-containing proteins SMARCA2 (BRM), SMARCA4 (BRG1), and polybromo-1. Dysregulation of chromatin remodeling leads to aberrant cell proliferation and differentiation. Here, we have characterized a set of potent and cell-active bromodomain inhibitors with pan-selectivity for canonical family VIII bromodomains. Targeted SWI/SNF bromodomain inhibition blocked the expression of key genes during adipogenesis, including the transcription factors PPARgamma and C/EBPalpha, and impaired the differentiation of 3T3-L1 murine fibroblasts into adipocytes. Our data highlight the role of SWI/SNF bromodomains in adipogenesis and provide a framework for the development of SWI/SNF bromodomain inhibitors for indirect targeting of key transcription factors regulating cell differentiation.
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Authors: Preuss, F., Joerger, A.C., Kraemer, A., Wanior, M., Knapp, S., Structural Genomics Consortium (SGC)
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Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis.,Wanior M, Preuss F, Ni X, Kramer A, Mathea S, Gobel T, Heidenreich D, Simonyi S, Kahnt AS, Joerger AC, Knapp S J Med Chem. 2020 Dec 10;63(23):14680-14699. doi: 10.1021/acs.jmedchem.0c01242., Epub 2020 Nov 20. PMID:33216538<ref>PMID:33216538</ref>
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Description: Crystal structure of the fifth bromodomain of human protein polybromo-1 in complex with tert-butyl 4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperazine-1-carboxylate
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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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[[Category: Joerger, A.C]]
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<div class="pdbe-citations 6zs4" style="background-color:#fffaf0;"></div>
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[[Category: Knapp, S]]
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== References ==
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[[Category: Wanior, M]]
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<references/>
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[[Category: Structural Genomics Consortium (Sgc)]]
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__TOC__
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[[Category: Preuss, F]]
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</StructureSection>
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[[Category: Kraemer, A]]
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Joerger AC]]
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[[Category: Knapp S]]
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[[Category: Kraemer A]]
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[[Category: Preuss F]]
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[[Category: Wanior M]]

Current revision

Crystal structure of the fifth bromodomain of human protein polybromo-1 in complex with tert-butyl 4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperazine-1-carboxylate

PDB ID 6zs4

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