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6zn6
From Proteopedia
(Difference between revisions)
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==Protein polybromo-1 (PB1 BD2) Bound To MW278== | ==Protein polybromo-1 (PB1 BD2) Bound To MW278== | ||
| - | <StructureSection load='6zn6' size='340' side='right'caption='[[6zn6]]' scene=''> | + | <StructureSection load='6zn6' size='340' side='right'caption='[[6zn6]], [[Resolution|resolution]] 2.02Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6ZN6 OCA]. For a <b>guided tour on the structure components</b> use [ | + | <table><tr><td colspan='2'>[[6zn6]] 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=6ZN6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6ZN6 FirstGlance]. <br> |
| - | </td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | </td></tr><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=QMT:2-[6-azanyl-5-[(3~{R})-3-phenoxypiperidin-1-yl]pyridazin-3-yl]phenol'>QMT</scene></td></tr> |
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PBRM1, BAF180, PB1 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6zn6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6zn6 OCA], [https://pdbe.org/6zn6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6zn6 RCSB], [https://www.ebi.ac.uk/pdbsum/6zn6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6zn6 ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Disease == | ||
| + | [[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> | ||
| + | == Function == | ||
| + | [[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> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | 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. | ||
| + | |||
| + | 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> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 6zn6" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[Ribosome biogenesis protein|Ribosome biogenesis protein]] | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Human]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Chatterjee D]] | + | [[Category: Chatterjee, D]] |
| - | [[Category: Joerger | + | [[Category: Joerger, A C]] |
| - | [[Category: Knapp S]] | + | [[Category: Knapp, S]] |
| - | [[Category: Mathea S]] | + | [[Category: Mathea, S]] |
| - | [[Category: Preuss F]] | + | [[Category: Preuss, F]] |
| - | [[Category: Wanior M]] | + | [[Category: Wanior, M]] |
| + | [[Category: Bromodomain inhibitor epigenetic]] | ||
| + | [[Category: Protein binding]] | ||
Revision as of 17:53, 10 March 2021
Protein polybromo-1 (PB1 BD2) Bound To MW278
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