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Article

Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.

Cancer cell - 1 Mar 2007

Yun Cai-Hong, Boggon Titus J, Li Yiqun, Woo Michele S, Greulich Heidi, Meyerson Matthew, Eck Michael J

Abstract excerpt

Mutations in the EGFR kinase are a cause of non-small-cell lung cancer. To understand their mechanism of activation and effects on drug binding, we studied the kinetics of the L858R and G719S mutants and determined their crystal structures with inhibitors including gefitinib, AEE788, and a staurosporine. We find that the mutations activate the kinase by disrupting autoinhibitory interactions, and that they...

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Identifiers

PMID: 17349580
DOI: 10.1016/j.ccr.2006.12.017
PMCID: PMC1939942

Genes

EGFR

Provenance

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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