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

Yun CH, Boggon TJ, Li Y, Woo MS, Greulich H, Meyerson M, Eck MJ
Cancer Cell 11 217-27 (2007)
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Cited: 539 times
EuropePMC logo PMID: 17349580

Abstract

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 accelerate catalysis as much as 50-fold in vitro. Structures of inhibitors in complex with both wild-type and mutant kinases reveal similar binding modes for gefitinib and AEE788, but a marked rotation of the staurosporine in the G719S mutant. Strikingly, direct binding measurements show that gefitinib binds 20-fold more tightly to the L858R mutant than to the wild-type enzyme.

Reviews - 2itu mentioned but not cited (1)

  1. Structure and clinical relevance of the epidermal growth factor receptor in human cancer. Kumar A, Petri ET, Halmos B, Boggon TJ. J Clin Oncol 26 1742-1751 (2008)

Articles - 2itu mentioned but not cited (9)

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