NCIt definition : An inhibitor of the bromodomain-containing protein 4 (BRD4), with potential antineoplastic
activity. Upon administration, the BRD4 inhibitor PLX51107 binds to the acetylated
lysine recognition motifs in the bromodomains of the BRD4 protein, thereby preventing
the binding of BRD4 to acetylated lysines on histones. This disrupts chromatin remodeling
and gene expression. Prevention of the expression of certain growth-promoting genes
may lead to an induction of apoptosis and an inhibition of proliferation in BRD4-overexpressing
tumor cells. BRD4, a member of the human bromodomain and extra-terminal (BET) family
of proteins, is a transcriptional regulator that is overexpressed in certain tumor
cells and plays an important role in cellular proliferation.;