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Article

Design and synthesis of selective degraders of EGFRL858R/T790M mutant.

European journal of medicinal chemistry - 15 Apr 2020

Zhang Xin, Xu Fang, Tong Linjiang, Zhang Tao, Xie Hua, Lu Xiaoyun, Ren Xiaomei, Ding Ke

Abstract excerpt

A series of PROTAC (proteolysis targeting chimera) based selective EGFRL858R/T790M (leucine 858 to arginine 858 mutation and threonine 790 to methionine 790) mutant degraders were designed and synthesized. One of the most potent compounds, 14o, effectively and selectively degraded EGFRL858R/T790M with an DC50 value of 5.9 nM, while did not show obvious effect on the wild-type protein. Further mechanism...

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Identifiers

PMID: 32171162
DOI: 10.1016/j.ejmech.2020.112199

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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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