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Article

Discovery of highly potent and selective KRASG12C degraders by VHL-recruiting PROTACs for the treatment of tumors with KRASG12C-Mutation.

European journal of medicinal chemistry - 5 Dec 2023

Yang Ning, Fan Zhiya, Sun Shiyang, Hu Xiaotong, Mao Yaqiu, Jia Changkai, Cai Xu, Xu Tingting, Li Bingkun, Li Yi, Han Luobing, Wei Ting, Qian Xiaohong, Qin Weijie, Li Pengyun, Zheng Zhibing, Li Song

Abstract excerpt

Although several covalent KRASG12C inhibitors have made great progress in the treatment of KRASG12C-mutant cancer, their clinical applications are limited by adaptive resistance, motivating novel therapeutic strategies. Through drug design and structure optimization, a series of highly potent and selective KRASG12C Proteolysis Targeting Chimeras (PROTACs) were developed by incorporating AMG510 and VHL ligand...

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Identifiers

PMID: 37852032
DOI: 10.1016/j.ejmech.2023.115857

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