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PDBsum entry 4c7t

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Transferase PDB id
4c7t
Contents
Protein chain
259 a.a.
Ligands
5RI
SO4
Waters ×44

References listed in PDB file
Key reference
Title Inhibition of both focal adhesion kinase and fibroblast growth factor receptor 2 pathways induces anti-Tumor and anti-Angiogenic activities.
Authors P.Dao, R.Jarray, N.Smith, Y.Lepelletier, J.Le coq, D.Lietha, R.Hadj-Slimane, J.P.Herbeuval, C.Garbay, F.Raynaud, H.Chen.
Ref. Cancer Lett, 2014, 348, 88-99. [DOI no: 10.1016/j.canlet.2014.03.007]
PubMed id 24657306
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.
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