NCIt definition : An orally bioavailable second mitochondrial-derived activator of caspases (SMAC) mimetic
and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins, with potential
antineoplastic activity. SMAC mimetic LCL161 binds to IAPs, such as X chromosome-linked
IAP (XIAP) and cellular IAPs 1 and 2. Since IAPs shield cancer cells from the apoptosis
process, this agent may restore and promote the induction of apoptosis through apoptotic
signaling pathways in cancer cells. IAPs are overexpressed by many cancer cell types
and suppress apoptosis by binding and inhibiting active caspases-3, -7 and -9, which
play essential roles in apoptosis (programmed cell death), necrosis and inflammation.;
Semantic type(s)