NCIt definition : A small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing
proteins with potential antineoplastic activity. Upon administration, molibresib 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 bromodomain at the N-terminus, BET proteins, comprising
of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important
role during development and cellular growth.;
UNII : 5QIO6SRZ2R;
InChIKey : AAAQFGUYHFJNHI-SFHVURJKSA-N;
CAS number : 1260907-17-2;
Molecule name : GSK525762; I-BET 762; GSK-525762A;