Selective inhibition of BET bromodomains.

Epigenetic proteins are intently pursued targets in ligand discovery. So far, successful efforts have been limited to chromatin modifying enzymes, or so-called epigenetic 'writers' and 'erasers'. Potent inhibitors of histone binding modules have not yet been described. Here we re...

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Bibliographic Details
Main Authors:	Filippakopoulos, P, Qi, J, Picaud, S, Shen, Y, Smith, W, Fedorov, O, Morse, E, Keates, T, Hickman, T, Felletar, I, Philpott, M, Munro, S, McKeown, M, Wang, Y, Christie, A, West, N, Cameron, M, Schwartz, B, Heightman, T, La Thangue, N, French, C, Wiest, O, Kung, A, Knapp, S, Bradner, J
Format:	Journal article
Language:	English
Published:	2010
Subjects:	Amino Acid Sequence chemical synthesis Mice, Nude Protein Structure, Tertiary Binding Sites Skin Neoplasms Stereoisomerism Molecular Sequence Data physiopathology Recombinant Proteins pharmacology Transcription Factors Chromatin antagonists and inhibitors Cell Line, Tumor metabolism Mice Humans Protein Binding Azirines Sequence Alignment chemistry Nuclear Proteins Carcinoma, Squamous Cell Female Cell Proliferation drug effects Models, Molecular Animals Cell Differentiation Dihydropyridines

Selective inhibition of BET bromodomains.

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