Preferred Label : Smac Mimetic BGB-24714;
NCIt synonyms : Second Mitochondrial-derived Activator of Caspases Mimetic BGB-24714;
NCIt definition : An orally bioavailable mimetic of the natural second mitochondrial-derived activator
of caspases (Smac), with potential apoptotic-inducing, chemo-radio-sensitizing and
antineoplastic activities. Upon oral administration, Smac mimetic BGB-24714 targets
and binds to the Smac binding groove on inhibitor of apoptosis proteins (IAPs), including
the direct caspase inhibitor X chromosome-linked IAP (XIAP), and the cellular IAPs
1 (c-IAP1) and 2 (c-IAP2). This inhibits the activities of these IAPs and promotes
the induction of apoptosis through apoptotic signaling pathways. IAPs are overexpressed
by many cancer cell types and suppress both intrinsic and extrinsic apoptosis by binding
to and inhibiting active caspases via their baculoviral lAP repeat (BIR) domains.
They contribute to chemo-radio-resistance of cancer cells to certain cytotoxic agents
and radiation, promote tumor cell survival and are associated with poor prognosis
in certain types of cancer. Smac, a pro-apoptotic mitochondrial protein, is an endogenous
inhibitor of the IAPs family of cellular proteins.;
Molecule name : BGB-24714; BGB 24714;
NCI Metathesaurus CUI : CL1792826;
Origin ID : C188052;
UMLS CUI : C5706446;
Semantic type(s)
- concept_is_in_subset
- has_target
