The Commonly Used PI3-Kinase Probe LY294002 Is an Inhibitor of BET Bromodomains
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https://figshare.com/articles/dataset/The_Commonly_Used_PI3_Kinase_Probe_LY294002_Is_an_Inhibitor_of_BET_Bromodomains/2321053
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资源简介：
A 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.
创建时间：
2014-02-21
