Selective inhibition of BET bromodomains.
|Abstract||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 report a cell-permeable small molecule (JQ1) that binds competitively to acetyl-lysine recognition motifs, or bromodomains. High potency and specificity towards a subset of ... [truncated at 450 characters in length]|
|Author||Filippakopoulos, Panagis; Qi, Jun; Picaud, Sarah; et al|
|Subject||Amino Acid Sequence Animals Azirines Binding Sites Carcinoma, Squamous Cell Cell Differentiation Cell Line, Tumor Cell Proliferation Chromatin Dihydropyridines Female Humans Mice Mice, Nude Models, Molecular Molecular Sequence Data Nuclear Proteins Protein Binding Protein Structure, Tertiary Recombinant Proteins Sequence Alignment Skin Neoplasms Stereoisomerism Transcription Factors chemical synthesis chemistry pharmacology physiopathology drug effects drug effects metabolism chemical synthesis chemistry pharmacology antagonists and inhibitors metabolism drug effects metabolism physiopathology antagonists and inhibitors metabolism|