NCIt definition : The hydrated form of pelabresib, a small molecule inhibitor of the Bromodomain and
Extra-Terminal (BET) family of proteins, with potential antineoplastic activity. Upon
administration, pelabresib binds to the acetylated lysine recognition motifs on the
bromodomain of BET proteins, thereby preventing the interaction between the BET proteins
and acetylated histone peptides. This disrupts chromatin remodeling and gene expression.
Prevention of the expression of certain growth-promoting genes may lead to an inhibition
of tumor cell growth. Characterized by a tandem repeat of two bromodomains at the
N-terminus, the BET proteins (BRD2, BRD3, BRD4 and BRDT) are transcriptional regulators
that play an important role during development and cellular growth.;