1. Data from Potent, Selective Inhibitors of Fibroblast Growth Factor Receptor Define Fibroblast Growth Factor Dependence in Preclinical Cancer Models
- Author
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Neil T. Thompson, David R. Newell, Christopher Murray, Julie Irving, John Lyons, Eddy Freyne, Edward J. Lewis, Jose Cosme, Andrew Pike, Brent L. Graham, Lindsay A. Devine, Susanne Bethell, Abarna Thiru, Ruth Feltell, Darcey Miller, Maria Carr, Sharna Rich, Michael A. Batey, Christopher Hamlett, Michael Reader, Martyn Frederickson, Alistair O'Brien, Emma Vickerstaffe, Rajdeep K. Benning, Andrew Madin, Charlotte Griffiths Jones, Douglas Ross, Lynsey Fazal, Tim Perera, Patrick Angibaud, Peter King, Anne Cleasby, Valerio Berdini, Gordan Saxty, George Ward, and Matthew Squires
- Abstract
We describe here the identification and characterization of 2 novel inhibitors of the fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases. The compounds exhibit selective inhibition of FGFR over the closely related VEGFR2 receptor in cell lines and in vivo. The pharmacologic profile of these inhibitors was defined using a panel of human tumor cell lines characterized for specific mutations, amplifications, or translocations known to activate one of the four FGFR receptor isoforms. This pharmacology defines a profile for inhibitors that are likely to be of use in clinical settings in disease types where FGFR is shown to play an important role. Mol Cancer Ther; 10(9); 1542–52. ©2011 AACR.
- Published
- 2023
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