Research advances in M. Tuberculosis polyketide synthase 13 inhibitors
10.16438/j.0513-4870.2020-0213
- VernacularTitle:结核分枝杆菌聚酮合成酶13抑制剂的研究进展
- Author:
Wei DING
1
;
Wen-ting ZHAO
1
;
Dong-feng ZHANG
1
Author Information
1. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Chinese Academy of Medical Sciences Key Laboratory of Anti-DR TB Innovative Drug Research, Beijing 100050, China
- Publication Type:Research Article
- Keywords:
italic>M. tuberculosis;
mycolic acid;
polyketide synthase 13 inhibitor;
mechanism of action;
structure-activity relationship
- From:
Acta Pharmaceutica Sinica
2020;55(8):1768-1773
- CountryChina
- Language:Chinese
-
Abstract:
Polyketide synthase 13 (Pks13) performs a critical role in the final assembly step of mycolic acid synthesis in Mycobacterium tuberculosis. The inhibition of Pks13 can influence the biosynthesis of mycolic acid, which leads to Mycobacterium tuberculosis cell death. Researchers have discovered Pks13 inhibitors with five chemical scaffolds as antituberculosis agents. Herein, we summarize recent advances in the study of Pks13 inhibitors including the process of discovery, the mechanism of action and structure-activity relationships.
