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Article

Structure-guided identification and biological evaluation of reversible EGFR C797S inhibitors.

Scientific reports - 4 May 2026

Weiss Glen J, Loftus Joseph C, Mallery David W, Tran Nhan L

Abstract excerpt

Resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) remains a major therapeutic challenge in EGFR-mutant cancers. While third-generation covalent EGFR inhibitors successfully suppress the T790M-mediated resistance, acquisition of the C797S substitution abrogates irreversible drug binding and represents a dominant mechanism of therapeutic failure. To address this challenge, we...

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Source

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Identifiers

PMID: 42082576
DOI: 10.1038/s41598-026-51989-8
PMCID: PMC13333846

Genes

EGFR
F3

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026.

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Structure-guided identification and biological evaluation of reversible EGFR C797S inhibitors.PMID 42082576Read ↗

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Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer.Semantic proximity Read ↗

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Identification of a novel nitroflavone-based scaffold for designing mutant-selective EGFR tyrosine kinase inhibitors targeting T790M and C797S resistance in advanced NSCLC.Semantic proximity Read ↗

Discovery of a potent, selective, and orally available EGFR C797S mutant inhibitor (DS06652923) with in vivo antitumor activity.Semantic proximity Read ↗

Elucidating the role of the T790M mutation in BLU-945 selectivity for mutant EGFR: structural and energetic insights.Semantic proximity Read ↗

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