Progress in small-molecule inhibitors of Bcl-2 family proteins

• Published in: Yao hsüeh hsüeh pao Vol. 43; no. 7; p. 669
• Main Authors: Tang, Yong, Zhang, Da-yong, Wu, Xiao-ming
• Format: Journal Article
• Language: Chinese
• Published: China 01.07.2008
• Subjects: Antimycin A - chemistry; Antimycin A - pharmacology; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Apoptosis - drug effects; bcl-X Protein - antagonists & inhibitors; bcl-X Protein - pharmacology; Benzopyrans - chemistry; Benzopyrans - pharmacology; Biphenyl Compounds - chemistry; Biphenyl Compounds - pharmacology; Cell Line, Tumor; Drug Design; Drugs, Chinese Herbal - chemistry; Drugs, Chinese Herbal - pharmacology; Gossypol - chemistry; Gossypol - pharmacology; Humans; Nitriles - chemistry; Nitriles - pharmacology; Nitrophenols - chemistry; Nitrophenols - pharmacology; Piperazines - chemistry; Piperazines - pharmacology; Proto-Oncogene Proteins c-bcl-2 - antagonists & inhibitors; Proto-Oncogene Proteins c-bcl-2 - pharmacology; Structure-Activity Relationship; Sulfonamides - chemistry; Sulfonamides - pharmacology; Thiazoles - chemistry; Thiazoles - pharmacology
• ISSN: 0513-4870

Apoptosis is an essential factor in keeping homeostasis of the organism. Apoptosis is regulated by a series of cytokines. Bcl-2 family proteins are key regulators of apoptosis. The Bcl-2 family includes both anti- and pro-apoptotic proteins with opposing biological functions. Their interaction regulates the transmission of the apoptosis signal. High expression of anti-apoptotic members such as Bcl-2 and Bcl-xL are commonly found in human cancers. In recent years, following the disclosing of the crystal structures of Bcl-2 family proteins, researchers have paid attention to the development of the small molecule inhibitors of Bcl-2 family proteins. This article reviews the progress in this field from the view of drug design.