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Article

Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations.

Angewandte Chemie (International ed. in English) - 17 Aug 2020

Jang Jaebong, To Ciric, De Clercq Dries J H, Park Eunyoung, Ponthier Charles M, Shin Bo Hee, Mushajiang Mierzhati, Nowak Radosław P, Fischer Eric S, Eck Michael J, Jänne Pasi A, Gray Nathanael S

Abstract excerpt

Targeting epidermal growth factor receptor (EGFR) through an allosteric mechanism provides a potential therapeutic strategy to overcome drug-resistant EGFR mutations that emerge within the ATP binding site. Here, we develop an allosteric EGFR degrader, DDC-01-163, which can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells while leaving wildtype EGFR Ba/F3 cells unaffected. DDC-01-163...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 32510788
DOI: 10.1002/anie.202003500
PMCID: PMC7686272

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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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