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

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

doi:10.1021/jacs.3c05899

journal article Aug 03, 2023

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

Zhongtang Yu

Xiaoqiang He

Ruiliu Wang Xinxin Xu

Journal of the American Chemical Society Vol. 145 No. 37 pp. 20403-20411 · American Chemical Society (ACS)

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Details

Published: Aug 03, 2023
Vol/Issue: 145(37)
Pages: 20403-20411
License: View

Authors

Z

Zhongtang Yu

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development (MOE), Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; Guangzhou City Key Laboratory of Precision Chemical Drug Development, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China

X

Xiaoqiang He

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development (MOE), Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; Guangzhou City Key Laboratory of Precision Chemical Drug Development, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China

R

Ruiliu Wang

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development (MOE), Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; Guangzhou City Key Laboratory of Precision Chemical Drug Development, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China

X

Xinxin Xu

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development (MOE), Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; Guangzhou City Key Laboratory of Precision Chemical Drug Development, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China

Z

Zhang Zhang

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development (MOE), Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; Guangzhou City Key Laboratory of Precision Chemical Drug Development, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China

K

Ke Ding

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development (MOE), Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; Guangzhou City Key Laboratory of Precision Chemical Drug Development, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China

Z

Zhi-Min Zhang

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development (MOE), Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; Guangzhou City Key Laboratory of Precision Chemical Drug Development, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China

Y

Yi Tan

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development (MOE), Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; Guangzhou City Key Laboratory of Precision Chemical Drug Development, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China

Z

Zhengqiu Li

International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development (MOE), Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; MOE Key Laboratory of Tumor Molecular Biology, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; Guangzhou City Key Laboratory of Precision Chemical Drug Development, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China

Funding

National Natural Science Foundation of China Award: 22077051

Science and Technology Planning Project of Guangdong Province Award: 2019B151502025

Guangzhou Municipal Science and Technology Project Award: 202102070001

Guangdong Provincial Pearl River Talents Program Award: 2017BT01Y036

Cite This Article

Zhongtang Yu, Xiaoqiang He, Ruiliu Wang, et al. (2023). Simultaneous Covalent Modification of K-Ras(G12D) and K-Ras(G12C) with Tunable Oxirane Electrophiles. Journal of the American Chemical Society, 145(37), 20403-20411. https://doi.org/10.1021/jacs.3c05899

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

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