Post-translational modification of KRAS: potential targets for cancer therapy  

作　　者：Wei-hua Wang Tao Yuan Mei-jia Qian Fang-jie Yan Liu Yang Qiao-jun He Bo Yang Jin-jian Lu Hong Zhu 

机构地区：[1]Zhejiang Province Key Laboratory of Anti-cancer Drug Research,Institute of Pharmacology and Toxicology,College of Pharmaceutical Sciences,Zhejiang University,Hangzhou 310058,China [2]Key Laboratory of Tumor Molecular Diagnosis and Individualized Medicine of Zhejiang Province,Zhejiang Provincial People’s Hospital,People’s Hospital of Hangzhou Medical College,Hangzhou 310014,China [3]State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macao,Macao,China

出　　处：《Acta Pharmacologica Sinica》2021年第8期1201-1211,共11页中国药理学报（英文版）

摘　　要：Aberrant activation of the RAS superfamily is one of the critical factors in carcinogenesis.Among them,KRAS is the most frequently mutated one which has inspired extensive studies for developing approaches to intervention.Although the cognition toward KRAS remains far from complete,mounting evidence suggests that a variety of post-translational modifications regulate its activation and localization.In this review,we summarize the regulatory mode of post-translational modifications on KRAS including prenylation,post-prenylation,palmitoylation,ubiquitination,phosphorylation,SUMOylation,acetylation,nitrosylation,etc.We also highlight the recent studies targeting these modifications having exhibited potent anti-tumor activities.

关 键 词：ONCOGENE KRAS post-translational modification PRENYLATION postprenylation PALMITOYLATION ubiquitination phosphorylation SUMOYLATION acetylation NITROSYLATION cancer therapy 

分 类 号：R730.5[医药卫生—肿瘤]