NCIt definition : A second mitochondrial activator of caspases (Smac) mimetic inhibitor of IAPs (Inhibitor
of Apoptosis Proteins) with potential antineoplastic activity. Smac mimetic GDC-0152
binds to the Smac binding groove on IAPs, including the direct caspase inhibitor X
chromosome-linked IAP (XIAP) and the cellular IAPs 1 and 2, which may inhibit their
activities and promote the induction of apoptosis through apoptotic signaling pathways.
IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding
to and inhibiting active caspases-3, -7 and -9 via their baculoviral lAP repeat (BIR)
domains. Smac, the endogenous IAP antagonist, relies on its N-terminal four amino-acid
motif for binding to IAPs.;
Semantic type(s)