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Article

Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations.

Journal of medicinal chemistry - 10 Mar 2022

Zhou Chuan, Fan Zisheng, Zhou Zehui, Li Yupeng, Cui Rongrong, Liu Chaoyi, Zhou Guizhen, Diao Xingxing, Jiang Hualiang, Zheng Mingyue, Zhang Sulin, Xu Tianfeng

Abstract excerpt

Regulating SOS1 functions may result in targeted pan-KRAS therapies. Small-molecule SOS1 inhibitors showed promising anticancer potential, and the most advanced inhibitor BI 1701963 is currently under phase I clinical studies. SOS1 agonists provide new opportunities to treat cancer; however, the underlying mechanisms still warrant investigation. We here report the discovery of the first SOS1 PROTACs designed...

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Identifiers

PMID: 35230841
DOI: 10.1021/acs.jmedchem.1c01774

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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