The Commonly Used PI3-Kinase Probe LY294002 Is an Inhibitor of BET Bromodomains

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 compri...

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Veröffentlicht in:	ACS chemical biology 2014-02, Vol.9 (2), p.495-502
Hauptverfasser:	Dittmann, Antje, Werner, Thilo, Chung, Chun-Wa, Savitski, Mikhail M, Fälth Savitski, Maria, Grandi, Paola, Hopf, Carsten, Lindon, Matthew, Neubauer, Gitte, Prinjha, Rabinder K, Bantscheff, Marcus, Drewes, Gerard
Format:	Artikel
Sprache:	eng
Schlagworte:	Cell Line Chromones - chemistry Chromones - pharmacology Crystallography, X-Ray Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology HEK293 Cells Humans Models, Molecular Morpholines - chemistry Morpholines - pharmacology Nuclear Proteins - antagonists & inhibitors Nuclear Proteins - metabolism Phosphatidylinositol 3-Kinases - antagonists & inhibitors Piperazines - chemistry Piperazines - pharmacology Protein-Serine-Threonine Kinases - antagonists & inhibitors Protein-Serine-Threonine Kinases - metabolism RNA-Binding Proteins - antagonists & inhibitors RNA-Binding Proteins - metabolism Transcription Factors - antagonists & inhibitors Transcription Factors - metabolism
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