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. 2014 Jun 28;348(1-2):88-99.
doi: 10.1016/j.canlet.2014.03.007. Epub 2014 Mar 19.

Inhibition of both focal adhesion kinase and fibroblast growth factor receptor 2 pathways induces anti-tumor and anti-angiogenic activities

Pascal Dao  1 , Rafika Jarray  1 , Nikaia Smith  1 , Yves Lepelletier  2 , Johanne Le Coq  3 , Daniel Lietha  3 , Réda Hadj-Slimane  4 , Jean-Philippe Herbeuval  1 , Christiane Garbay  1 , Françoise Raynaud  1 , Huixiong Chen  5
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Inhibition of both focal adhesion kinase and fibroblast growth factor receptor 2 pathways induces anti-tumor and anti-angiogenic activities

Pascal Dao et al. Cancer Lett. .

Abstract

FAK and FGFR2 signaling pathways play important roles in cancer development, progression and tumor angiogenesis. PHM16 is a novel ATP competitive inhibitor of FAK and FGFR2. To evaluate the therapeutic efficacy of this agent, we examined its anti-angiogenic effect in HUVEC and its anti-tumor effect in different cancer cell lines. We showed PHM16 inhibited endothelial cell viability, adherence and tube formation along with the added ability to induce endothelial cell apoptosis. This compound significantly delayed tumor cell growth. Together, these data showed that inhibition of both FAK and FGFR2 signaling pathways can enhance anti-tumor and anti-angiogenic activities.

Keywords: Angiogenesis; Cancer; FAK; FGFR2; Inhibitor.

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