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Article

Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation.

Journal of medicinal chemistry - 9 May 2024

Zhu Yasheng, Ye Xiuquan, Wu Yuxing, Shen Hao, Cai Zeyu, Xia Fei, Min Wenjian, Hou Yi, Wang Liping, Wang Xiao, Xiao Yibei, Yang Peng

Abstract excerpt

The epidermal growth factor receptor (EGFR) tertiary C797S mutation is an important cause of resistance to Osimertinib, which seriously hinders the clinical application of Osimertinib. Developing proteolysis-targeting chimeras (PROTACs) targeting EGFR mutants can offer a promising strategy to overcome drug resistance. In this study, some novel PROTACs targeting C797S mutation were designed and synthesized based...

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Identifiers

PMID: 38676656
DOI: 10.1021/acs.jmedchem.4c00107

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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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