Apoptosis is a programmed cell death process, critical for normal cellular development and tissue homeostasis. B-cell lymphocyte/leukemia 2 (Bcl-2) family proteins are important regulators of apoptosis. Numerous studies have demonstrated that over-expressing anti-apoptotic Bcl-2 proteins is one mechanism for cancer cells to acquire resistance against cancer chemotherapies, suggesting antagonizing these proteins would be a potential approach to overcoming such drug resistance. This review briefly discusses the principle and the recent advances in the development of such antagonists, with some highlights about several promising antagonists.
Keywords: Bcl-2 antagonists, drug resistance, apoptosis, cancer
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