Tyrosine kinase inhibitors of overexpressed FGFR1 Tyrosine kinase inhibitors bind and inhibit overexpressed FGFR1 dimers Authored: Rothfels, K, 2012-02-09 Edited: Rothfels, K, 2012-05-16 Pubmed17121884 Pubmed20094046 Pubmed20179196 Pubmed21160078 Pubmed21666749 Pubmed21711248 Reactome Database ID Release 432023462 Reactome, http://www.reactome.org ReactomeREACT_121386 Reviewed: Ezzat, S, 2012-05-15 Treatment of FGFR1-amplified lung and breast cancer cell lines with the in vitro reagents PD173704, SU5402 and FIIN-1 inhibits proliferation, while cells expressing wild-type levels of FGFR1 are insensitive to inhibitors, suggesting that amplified FGFR1 may be a suitable therapeutic target in some cancer lines (Weiss, 2010; Reis-Filho, 2006; Dutt, 2011; Turner, 2010). In fact, a number of other small molecule inhibitors, including Dovitinib and AZD4547, are currently in clinical trials for treatment of FGFR1-amplified cancers (reviewed in Turner and Grose, 2010; Wesche, 2011; http://ClinicalTrials.gov) has a Stoichiometric coefficient of 2 Overexpressed FGFR1:TKIs Overexpressed FGFR1 homodimers