摘要
在结核分枝杆菌分枝菌酸的生物合成通路中,聚酮合成酶13(polyketide synthase 13,Pks13)起到最后一步的组装作用。通过抑制Pks13可以抑制分枝菌酸的合成,进而起到杀灭结核分枝杆菌的作用。目前已发现五类化学骨架不同的Pks13抑制剂,本文将简要介绍这几类Pks13抑制剂的发现过程、作用机制以及不同抑制剂的构效关系。
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.
作者
丁威
赵文婷
张东峰
DING Wei;ZHAO Wen-ting;ZHANG Dong-feng(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)
出处
《药学学报》
CAS
CSCD
北大核心
2020年第8期1768-1773,共6页
Acta Pharmaceutica Sinica
基金
中国医学科学院医学与健康科技创新工程(2016-I2M-1-013)。
关键词
结核分枝杆菌
分枝菌酸
聚酮合成酶13抑制剂
作用机制
构效关系
M.tuberculosis
mycolic acid
polyketide synthase 13 inhibitor
mechanism of action
structureactivity relationship
