Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib.

@article{Gilmer2008ImpactOC,
  title={Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib.},
  author={Tona M. Gilmer and Louann Cable and Krystal J Alligood and David Rusnak and Glenn M Spehar and Kathleen T Gallagher and Ermias Woldu and Henrietta Carter and Anne T Truesdale and Lisa M. Shewchuk and Edgar R. Wood},
  journal={Cancer research},
  year={2008},
  volume={68 2},
  pages={
          571-9
        }
}
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 kinase V(max) and increasing the K(m)((app)) for ATP. The point mutations G719C… CONTINUE READING
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