Bcl-2 Inhibitors as Sensitizing Agents for Cancer Chemotherapy

Abstract This chapter reviewed B-cell lymphoma 2 (known as Bcl-2) family proteins in the cancer chemotherapy as sensitizing agents. Escaping apoptosis plays a key role in survival of the tumor. Bcl-2 family members could regulate cell apoptosis or survival through interactions between pro- and antiapoptotic proteins. Targeting Bcl-2 antiapoptotic proteins has gradually become one of the most important therapeutic strategies in cancer therapy. This chapter reviewed the discovery history of Bcl-2 molecules, the Bcl-2 family members, and their structures. The mechanisms of apoptosis regulated by Bcl-2 family and effects of Bcl-2 on the development and prognosis of cancer were also discussed. In addition, this review summarized the therapeutic agents targeting Bcl-2 in cancer chemotherapy including the mechanisms of actions, the clinical and preclinical effects, adverse effects, and future applications.