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Simultaneous Covalent Modification of K-Ras(G12D) and K-Ras(G12C) with Tunable Oxirane Electrophiles.

Journal of the American Chemical Society - 20 Sept 2023

Yu Zhongtang, He Xiaoqiang, Wang Ruiliu, Xu Xinxin, Zhang Zhang, Ding Ke, Zhang Zhi-Min, Tan Yi, Li Zhengqiu

Abstract excerpt

Owing to their remarkable pharmaceutical properties compared to those of noncovalent inhibitors, the development of targeted covalent inhibitors (TCIs) has emerged as a powerful method for cancer treatment. The K-Ras mutant, which is prevalent in multiple cancers, has been confirmed to be a crucial drug target in the treatment of various malignancies. However, although the K-Ras(G12D) mutation is present in up to...

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PMID: 37534597
DOI: 10.1021/jacs.3c05899

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