NCIt definition : An inhibitor of the Bromodomain (BRD) and Extra-Terminal domain (BET) family of proteins,
with potential antineoplastic activity. Upon administration, the BET inhibitor BAY1238097
binds to the acetylated lysine recognition motifs on the BRD of BET proteins, thereby
preventing the interaction between BET proteins and histones. This disrupts chromatin
remodeling and prevents the expression of certain growth-promoting genes. This leads
to an inhibition of tumor cell growth. BET proteins (BRD2, BRD3, BRD4 and BRDT) are
transcriptional regulators that bind to acetylated lysines on the tails of histones
H3 and H4, and regulate chromatin structure and function; they play an important role
in the modulation of gene expression during development and cellular growth.;