| Literature DB >> 21764904 |
Matthew Squires1, George Ward, Gordan Saxty, Valerio Berdini, Anne Cleasby, Peter King, Patrick Angibaud, Tim Perera, Lynsey Fazal, Douglas Ross, Charlotte Griffiths Jones, Andrew Madin, Rajdeep K Benning, Emma Vickerstaffe, Alistair O'Brien, Martyn Frederickson, Michael Reader, Christopher Hamlett, Michael A Batey, Sharna Rich, Maria Carr, Darcey Miller, Ruth Feltell, Abarna Thiru, Susanne Bethell, Lindsay A Devine, Brent L Graham, Andrew Pike, Jose Cosme, Edward J Lewis, Eddy Freyne, John Lyons, Julie Irving, Christopher Murray, David R Newell, Neil T Thompson.
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.Entities:
Mesh：
Substances：
Year: 2011 PMID： 21764904 DOI： 10.1158/1535-7163.MCT-11-0426
Source DB: PubMed Journal: Mol Cancer Ther ISSN： 1535-7163 Impact factor: 6.261