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|