Progress in small-molecule inhibitors of Bcl-2 family proteins.
- Author:
Yong TANG
1
;
Da-yong ZHANG
;
Xiao-ming WU
Author Information
1. School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
- Publication Type:Journal Article
- MeSH:
Antimycin A;
chemistry;
pharmacology;
Antineoplastic Agents;
chemistry;
pharmacology;
Apoptosis;
drug effects;
Benzopyrans;
chemistry;
pharmacology;
Biphenyl Compounds;
chemistry;
pharmacology;
Cell Line, Tumor;
Drug Design;
Drugs, Chinese Herbal;
chemistry;
pharmacology;
Gossypol;
chemistry;
pharmacology;
Humans;
Nitriles;
chemistry;
pharmacology;
Nitrophenols;
chemistry;
pharmacology;
Piperazines;
chemistry;
pharmacology;
Proto-Oncogene Proteins c-bcl-2;
antagonists & inhibitors;
pharmacology;
Structure-Activity Relationship;
Sulfonamides;
chemistry;
pharmacology;
Thiazoles;
chemistry;
pharmacology;
bcl-X Protein;
antagonists & inhibitors;
pharmacology
- From:
Acta Pharmaceutica Sinica
2008;43(7):669-677
- CountryChina
- Language:Chinese
-
Abstract:
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.
