Dysregulation of apoptosis plays a major role in cancer etiology. Cancer cells often contain genetic abnormalities which allow the cells to survive under conditions that normally would trigger their demise. The identification of these mutations has changed the models of cancer progression from a disease of excessive proliferation to one of unbalanced cell death and cell growth. During the last decade, fundamental knowledge delineating the molecular mechanisms of apoptosis has emerged and now can be exploited to identify novel apoptotic modulators for the treatment of cancer.