Article
Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib.
Cancer research - 15 Jan 2008
Gilmer Tona M, Cable Louann, Alligood Krystal, Rusnak David, Spehar Glenn, Gallagher Kathleen T, Woldu Ermias, Carter H Luke, Truesdale Anne T, Shewchuk Lisa, Wood Edgar R
Abstract excerpt
The goal of this study was to characterize the effects of non-small cell lung carcinoma (NSCLC)-associated mutations in epidermal growth factor receptor (EGFR/ErbB1) and HER2 (ErbB2) on interactions with the dual tyrosine kinase inhibitor lapatinib. Biochemical studies show that commonly observed variants of EGFR [G719C, G719S, L858R, L861Q, and Delta746-750 (del15)] are enzyme activating, increasing the tyrosine...
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