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Insight into the Therapeutic Selectivity of the Irreversible EGFR Tyrosine Kinase Inhibitor Osimertinib through Enzyme Kinetic Studies

Zhai X, Ward RA, Doig P, Argyrou A · Biochemistry 2020 · Biochemistry 59(14):1428-1441

EGFR (Tyr) wild-type & oncogenic mutants, Covalent Inhibitors Tyrosine kinase Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profilingMechanism & structural biology PhosphoSens

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Enozertinib Is a Selective, Brain-Penetrant EGFR Inhibitor for Treating Non-Small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations

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Structural Studies of Fourth-Generation EGFR Inhibitors Reveal Insights into Selective T790M and C797S Targeting

Damghani T, Song S, Lin KS, … Heppner DE · ACS Med Chem Lett 2026

TAS3351 is a brain penetrable EGFR-TKI that overcomes T790M and C797S resistant mutations

Kasuga H, Kataoka Y, Yamamoto F, … Mizuarai S · Commun Med (Lond) 2026

Covalent Alkynylpyridopyrimidinones Targeting Cysteine 775 of the Epidermal Growth Factor Receptor Overcome Resistance to Current Therapies

Stewart HL, Bordoni C, Jennings CE, … Waring MJ · J Med Chem 2025

Discovery of STX-721, a Covalent, Potent, and Highly Mutant-Selective EGFR/HER2 Exon20 Insertion Inhibitor for the Treatment of Non-Small Cell Lung Cancer

Milgram BC, Borrelli DR, Brooijmans N, … Guzman-Perez A · J Med Chem 2025

Factors affecting irreversible inhibition of EGFR and influence of chirality on covalent binding

Morese PA, Ahmad A, Martin MP, … Waring MJ · Commun Chem 2025

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