Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor.

@article{Fry1998SpecificII,
  title={Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor.},
  author={David W. Fry and Alex J. Bridges and William A. Denny and Ann O' Doherty and Kenneth D. Greis and Jessica L. Hicks and Kenneth E. Hook and Paul R Keller and Wilbur R. Leopold and Joseph A Loo and Dennis J McNamara and James M. Nelson and Veronica Sherwood and Jeff Bruce Smaill and Susanne Trumpp-Kallmeyer and Ellen M Dobrusin},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={1998},
  volume={95 20},
  pages={12022-7}
}
A class of high-affinity inhibitors is disclosed that selectively target and irreversibly inactivate the epidermal growth factor receptor tyrosine kinase through specific, covalent modification of a cysteine residue present in the ATP binding pocket. A series of experiments employing MS, molecular modeling, site-directed mutagenesis, and 14C-labeling studies in viable cells unequivocally demonstrate that these compounds selectively bind to the catalytic domain of the epidermal growth factor… CONTINUE READING
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Fry et al

  • D. J. II Riese, D. F. BioEssays 20 41–48. FIG. 6. Comparative antitum Stern, +10 authors phosphotyrosine content was determined by ELISA . 12026 Pharmacology
  • Proc. Natl. Acad. Sci. USA 95
  • 1998

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