NCIt synonyms : BD2-selective BET Inhibitor ABBV-744;
NCIt related terms : ABBV-744;
NCIt definition : An orally bioavailable inhibitor of the Bromodomain and Extra-Terminal (BET) family
of proteins, with potential antineoplastic activity. Upon oral administration, the
BET inhibitor ABBV-744 preferentially binds to the second bromodomain (BD2) of BET
proteins, thereby preventing the interaction between the BET proteins and acetylated
histones. This disrupts chromatin remodeling and gene expression. Prevention of the
expression of certain growth-promoting genes may lead to an inhibition of proliferation
in BET-overexpressing tumor cells. BET proteins, comprised of BRD2, BRD3, BRD4 and
BRDT, are transcriptional regulators that contain two homologous bromodomains, the
BD1 and BD2 domains. They play an important role during development and cellular growth.;
UNII : 9MX546E2SF;
CAS number : 2138861-99-9; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2138861-99-9
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