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One hallmark of human cancers is their ability to evade apoptosis,or programmed cell death.Since apoptosis is a tightly regulated cellular process,targeting critical apoptosis regulators with the goal to restore apoptosis in tumor cells is a promising strategy for the development of new cancer therapeutics.In this presentation,I will summarize our research in the past decade to target three classes of key regulators of apoptosis:The inhibitor of apoptosis proteins(IAPs),the Bcl-2 family proteins and the MDM2 protein.IAP proteins regulate apoptosis by directly or indirectly blocking the activation of several caspases (caspase-8,-9,-3 and-7).Bcl-2 proteins control apoptosis by modulation of the outer membrane permeability of mitochondria.MDM2 regulates apoptosis by binding to and inhibition of tumor suppressor p53.One common feature of these apoptosis regulators is that they control apoptosis through protein-protein interactions.Targeting protein-protein interactions has been considered as a major challenge in modern medicinal chemistry.