Rise of the Selective Inhibitors of Anti-Apoptotic Bcl-2 Family Proteins

Authors

  • Dr. Li Han,

    1. State Key Laboratory of Bioorganic & Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032 (China)
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  • Prof. Renxiao Wang

    Corresponding author
    1. State Key Laboratory of Bioorganic & Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032 (China)
    2. State Key Laboratory of Quality Research in Chinese Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Avenida Wai Long, Taipa, Macau (China)
    • State Key Laboratory of Bioorganic & Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032 (China)

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Abstract

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No trivial pursuit! It is not trivial to develop effective small-molecule regulators of protein–protein interactions (PPIs). Moreover, anti-apoptotic Bcl-2 family proteins share similar binding grooves, making it particularly difficult to target them selectively. Despite these challenges, potent and selective inhibitors of individual members of the Bcl-2 family have been successfully developed.

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