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

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 evid...

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Bibliographic Details
Published in:Acta pharmacologica Sinica 2021-08, Vol.42 (8), p.1201-1211
Main Authors: Wang, Wei-hua, Yuan, Tao, Qian, Mei-jia, Yan, Fang-jie, Yang, Liu, He, Qiao-jun, Yang, Bo, Lu, Jin-jian, Zhu, Hong
Format: Article
Language:English
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Summary: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.
ISSN:1671-4083
1745-7254
DOI:10.1038/s41401-020-00542-y