Proteins of B-cell lymphoma (Bcl-2) family are key regulators of apoptosis and are involved
in the pathogenesis of various cancers. Disrupting the interactions between the antiapoptotic
and proapoptotic Bcl-2 members is an attractive strategy to reactivate the apoptosis of cancer cells.
Structure-based drug design (SBDD) has been successfully applied to the discovery of small molecule
inhibitors targeting Bcl-2 proteins in past decades. Up to now, many Bcl-2 inhibitors with different
paralogue selectivity profiles have been developed and some were used in clinical trials. This
review focused on the recent applications of SBDD strategies in the development of small molecule
inhibitors targeting Bcl-2 family proteins.
Keywords: Bcl-2 family proteins, apoptosis, cancer, structure-based drug design strategy, co-crystal structure, small molecule
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