BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen

Chemical inhibition of epigenetic regulatory proteins BrdT and Brd4 is emerging as a promising therapeutic strategy in contraception, cancer, and heart disease. We report an easily synthesized dihydropyridopyrimidine pan-BET inhibitor scaffold, which was uncovered via a virtual screen followed by te...

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Veröffentlicht in:	Journal of medicinal chemistry 2017-06, Vol.60 (12), p.4805-4817
Hauptverfasser:	Ayoub, Alex M, Hawk, Laura M. L, Herzig, Ryan J, Jiang, Jiewei, Wisniewski, Andrea J, Gee, Clifford T, Zhao, Peiliang, Zhu, Jin-Yi, Berndt, Norbert, Offei-Addo, Nana K, Scott, Thomas G, Qi, Jun, Bradner, James E, Ward, Timothy R, Schönbrunn, Ernst, Georg, Gunda I, Pomerantz, William C. K
Format:	Artikel
Sprache:	eng
Schlagworte:	BASIC BIOLOGICAL SCIENCES Binding Sites Cell Cycle Proteins Cell Line Crystallography, X-Ray Fluorescence Polarization Fluorometry - methods High-Throughput Screening Assays - methods Humans INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY Magnetic Resonance Spectroscopy Models, Molecular Nuclear Proteins - antagonists & inhibitors Nuclear Proteins - chemistry Nuclear Proteins - metabolism Protein Domains Pyrimidines - chemistry Structure-Activity Relationship Transcription Factors - antagonists & inhibitors Transcription Factors - chemistry Transcription Factors - metabolism User-Computer Interface
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