4cfk: Difference between revisions
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==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH LY294002== | ==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH LY294002== | ||
<StructureSection load='4cfk' size='340' side='right' caption='[[4cfk]], [[Resolution|resolution]] 1.55Å' scene=''> | <StructureSection load='4cfk' size='340' side='right' caption='[[4cfk]], [[Resolution|resolution]] 1.55Å' scene=''> | ||
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=LY2:2-MORPHOLIN-4-YL-7-PHENYL-4H-CHROMEN-4-ONE'>LY2</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=LY2:2-MORPHOLIN-4-YL-7-PHENYL-4H-CHROMEN-4-ONE'>LY2</scene></td></tr> | ||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4cfl|4cfl]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4cfl|4cfl]]</td></tr> | ||
<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=4cfk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4cfk OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4cfk RCSB], [http://www.ebi.ac.uk/pdbsum/4cfk PDBsum]</span></td></tr> | <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=4cfk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4cfk OCA], [http://pdbe.org/4cfk PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4cfk RCSB], [http://www.ebi.ac.uk/pdbsum/4cfk PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4cfk ProSAT]</span></td></tr> | ||
</table> | </table> | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 4cfk" style="background-color:#fffaf0;"></div> | |||
==See Also== | |||
*[[Bromodomain-containing protein|Bromodomain-containing protein]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 19:05, 11 August 2016
N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH LY294002N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH LY294002
Structural highlights
Publication Abstract from PubMedA commonly used small-molecule probe in cell-signaling research is the phosphoinositide 3-kinase inhibitor LY294002. Quantitative chemoproteomic profiling shows that LY294002 and LY303511, a close analogue devoid of PI3K activity, inhibit the BET bromodomain proteins BRD2, BRD3, and BRD4 that comprise a family of targets structurally unrelated to PI3K. Both compounds competitively inhibit acetyl-lysine binding of the first but not the second bromodomain of BET proteins in cell extracts. X-ray crystallography shows that the chromen-4-one scaffold represents a new bromodomain pharmacophore and establishes LY294002 as a dual kinase and BET-bromodomain inhibitor, whereas LY303511 exhibits anti-inflammatory and antiproliferative effects similar to the recently discovered BET inhibitors. The Commonly Used PI3-Kinase Probe LY294002 Is an Inhibitor of BET Bromodomains.,Dittmann A, Werner T, Chung CW, Savitski MM, Falth Savitski M, Grandi P, Hopf C, Lindon M, Neubauer G, Prinjha RK, Bantscheff M, Drewes G ACS Chem Biol. 2014 Feb 21;9(2):495-502. doi: 10.1021/cb400789e. Epub 2013 Dec, 10. PMID:24533473[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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