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Article

Design, Synthesis, and Biological Evaluation of Potent and Selective PROTAC Degraders of Oncogenic KRASG12D.

Journal of medicinal chemistry - 25 Jan 2024

Zhou Chuan, Fan Zisheng, Gu Yuejiao, Ge Zhiming, Tao Zhaofan, Cui Rongrong, Li Yupeng, Zhou Guizhen, Huo Ruifeng, Gao Mingshan, Wang Dan, He Wei, Zheng Mingyue, Zhang Sulin, Xu Tianfeng

Abstract excerpt

KRASG12D, the most frequent KRAS oncogenic mutation, is a promising target for cancer therapy. Herein, we report the design, synthesis, and biological evaluation of a series of KRASG12D PROTACs by connecting the analogues of MRTX1133 and the VHL ligand. Structural modifications of the linker moiety and KRAS inhibitor part suggested a critical role of membrane permeability in the degradation activity of the...

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PMID: 38197882
DOI: 10.1021/acs.jmedchem.3c01622

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