Definition

An orally bioavailable inhibitor of the bromodomain and extra-terminal (BET) family of proteins, with potential antineoplastic activity. Upon oral administration, BET inhibitor TQB3617 targets and binds to the acetyl-lysine binding site in the bromodomains (BRDs), thereby preventing the interaction between BET proteins and acetylated histones. This disrupts chromatin remodeling and suppresses the expression of certain oncogenes, resulting in the inhibition of tumor cell growth. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role in the modulation of gene expression during cellular growth and development.