What is the Mechanism of Action of BET Inhibitors?
BET inhibitors function by competitively binding to the bromodomains of BET proteins, thereby preventing these proteins from attaching to acetylated lysine residues on histones. This inhibition disrupts the recruitment of BET proteins to chromatin, leading to alterations in the transcriptional machinery. As a result, the expression of genes critical for cancer cell proliferation and survival is downregulated, which can induce cell cycle arrest, apoptosis, and senescence in cancer cells.
