6z7m
From Proteopedia
(Difference between revisions)
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==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 (3R,4R)-N-cyclohexyl-4-((3-methyl-2-oxo-1,2-dihydro-1,7-naphthyridin-8-yl)amino)piperidine-3-carboxamide== | ==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 (3R,4R)-N-cyclohexyl-4-((3-methyl-2-oxo-1,2-dihydro-1,7-naphthyridin-8-yl)amino)piperidine-3-carboxamide== | ||
| - | <StructureSection load='6z7m' size='340' side='right'caption='[[6z7m]]' scene=''> | + | <StructureSection load='6z7m' size='340' side='right'caption='[[6z7m]], [[Resolution|resolution]] 1.26Å' 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=6Z7M OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6Z7M FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[6z7m]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6Z7M OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6Z7M FirstGlance]. <br> |
| - | </td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6z7m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6z7m OCA], [http://pdbe.org/6z7m PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6z7m RCSB], [http://www.ebi.ac.uk/pdbsum/6z7m PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6z7m ProSAT]</span></td></tr> | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=QAZ:(3R,4R)-N-cyclohexyl-4-((3-methyl-2-oxo-1,2-dihydro-1,7-naphthyridin-8-yl)amino)piperidine-3-carboxamide'>QAZ</scene></td></tr> |
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6z7l|6z7l]]</td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">BRD4, HUNK1 ([http://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'>[http://proteopedia.org/fgij/fg.htm?mol=6z7m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6z7m OCA], [http://pdbe.org/6z7m PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6z7m RCSB], [http://www.ebi.ac.uk/pdbsum/6z7m PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6z7m ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Disease == | ||
| + | [[http://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Note=A chromosomal aberration involving BRD4 is found in a rare, aggressive, and lethal carcinoma arising in midline organs of young people. Translocation t(15;19)(q14;p13) with NUT which produces a BRD4-NUT fusion protein.<ref>PMID:12543779</ref> <ref>PMID:11733348</ref> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity). | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Pan-BET inhibitors interact equipotently with all eight bromodomains of the BET family of proteins. They have shown profound efficacy in-vitro and in-vivo in oncology and immuno-modulatory models and a number are currently in clinical trials where significant safety signals have been reported. It is therefore important to understand the functional contribution of each bromodomain to assess the opportunity to tease apart efficacy and toxicity. This article discloses the in-vitro and cellular activity profile of GSK789, a potent, cell permeable and highly selective inhibitor of the first bromodomains of the BET family. | ||
| + | |||
| + | GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.,Watson RJ, Bamborough P, Barnett HA, Chung CW, Davis R, Gordon LJ, Grandi P, Petretich M, Phillipou A, Prinjha RK, Rioja I, Soden P, Werner T, Demont EH J Med Chem. 2020 Jul 21. doi: 10.1021/acs.jmedchem.0c00614. PMID:32691589<ref>PMID:32691589</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 6z7m" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Human]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Chung C]] | + | [[Category: Chung, C]] |
| + | [[Category: Antagonist]] | ||
| + | [[Category: Brd4]] | ||
| + | [[Category: Bromodomain]] | ||
| + | [[Category: Bromodomain containing protein 4]] | ||
| + | [[Category: Epigenetic reader]] | ||
| + | [[Category: Histone]] | ||
| + | [[Category: Inhibitor]] | ||
| + | [[Category: Transcription]] | ||
Revision as of 11:34, 23 September 2020
N-TERMINAL BROMODOMAIN OF HUMAN BRD4 (3R,4R)-N-cyclohexyl-4-((3-methyl-2-oxo-1,2-dihydro-1,7-naphthyridin-8-yl)amino)piperidine-3-carboxamide
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