NCIt definition : An inhibitor of the Bromodomain (BRD) and Extra-Terminal (BET) family of BRD-containing
proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor
INCB057643 binds to the acetylated lysine recognition motifs found in the BRD of BET
proteins, thereby preventing the interaction between the BET proteins and acetylated
lysines on histones. This disrupts chromatin remodeling and gene expression. Prevention
of the expression of certain growth-promoting genes, such as c-Myc-dependent target
genes, may lead to an inhibition of tumor cell growth. BET proteins are transcriptional
regulators that are overexpressed in certain tumor cells and play an important role
in cellular growth.;