Background:

BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins.

BMS-986158 is an inhibitor of the bromodomain (BRD) and extra-terminal domain (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor BMS-986158 binds to the acetyl-lysine binding site in the BRD of BET proteins, thereby preventing the interaction between BET proteins and acetylated histones. This disrupts chromatin remodeling and prevents the expression of certain growth-promoting genes, resulting in an inhibition of tumor cell growth[2].

[1]. von Schaper E. Roche bets on bromodomains. Nat Biotechnol. 2016 Apr;34(4):361-2. [2]. BET Inhibitor BMS-986158.