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Inhibitor of apoptosis (IAP) proteins are expressed at high levels in various cancers and block apoptosis at a key node. Therefore, there is currently much interest in IAP antagonists as cancer therapeutics. Structure-based development of selective IAP inhibitors now provides, for the first time, evidence that simultaneous inhibition of the c-IAP proteins and XIAP is necessary for efficient induction of cancer cell death by IAP antagonists.

Inhibitor of Apoptosis (IAP) Proteins: Novel Insights into the Cancer-Relevant Targets for Cell Death Induction