4cfl: Difference between revisions
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==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH LY303511== | ==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH LY303511== | ||
<StructureSection load='4cfl' size='340' side='right' caption='[[4cfl]], [[Resolution|resolution]] 1.32Å' scene=''> | <StructureSection load='4cfl' size='340' side='right'caption='[[4cfl]], [[Resolution|resolution]] 1.32Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4cfl]] 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=4CFL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4CFL FirstGlance]. <br> | <table><tr><td colspan='2'>[[4cfl]] 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=4CFL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4CFL FirstGlance]. <br> | ||
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</StructureSection> | </StructureSection> | ||
[[Category: Human]] | [[Category: Human]] | ||
[[Category: Large Structures]] | |||
[[Category: Chung, C]] | [[Category: Chung, C]] | ||
[[Category: Dittmann, A]] | [[Category: Dittmann, A]] | ||
Revision as of 12:16, 20 March 2019
N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH LY303511N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH LY303511
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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