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Article

Development of SOS1 Inhibitor-Based Degraders to Target KRAS-Mutant Colorectal Cancer.

Journal of medicinal chemistry - 22 Dec 2022

Bian Yujia, Alem Diego, Beato Francisca, Hogenson Tara L, Yang Xinrui, Jiang Kun, Cai Jianfeng, Ma Wen Wee, Fernandez-Zapico Martin, Tan Aik Choon, Lawrence Nicholas J, Fleming Jason B, Yuan Yu, Xie Hao

Abstract excerpt

Direct blockade of KRAS driver mutations in colorectal cancer (CRC) has been challenging. Targeting SOS1, a guanine nucleotide exchange factor, has arisen as an attractive approach for KRAS-mutant CRC. Here, we describe the development of novel SOS1 degraders and their activity in patient-derived CRC organoids (PDO). The design of these degraders as proteolysis-targeting chimera was based on the crystal...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 36459180
DOI: 10.1021/acs.jmedchem.2c01300
PMCID: PMC10113742

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