4C7T
Focal Adhesion Kinase catalytic domain in complex with a diarylamino- 1,3,5-triazine inhibitor
Summary for 4C7T
| Entry DOI | 10.2210/pdb4c7t/pdb |
| Descriptor | FOCAL ADHESION KINASE 1, N-methyl-2-[[4-[(3,4,5-trimethoxyphenyl)amino]-1,3,5-triazin-2-yl]amino]benzamide, SULFATE ION, ... (4 entities in total) |
| Functional Keywords | transferase, kinase inhibitor, atp-binding, integrin signaling |
| Biological source | GALLUS GALLUS (CHICKEN) |
| Total number of polymer chains | 1 |
| Total formula weight | 32238.29 |
| Authors | Le Coq, J.,Lietha, D. (deposition date: 2013-09-25, release date: 2014-04-02, Last modification date: 2023-12-20) |
| Primary citation | Dao, P.,Jarray, R.,Smith, N.,Lepelletier, Y.,Le Coq, J.,Lietha, D.,Hadj-Slimane, R.,Herbeuval, J.P.,Garbay, C.,Raynaud, F.,Chen, H. Inhibition of Both Focal Adhesion Kinase and Fibroblast Growth Factor Receptor 2 Pathways Induces Anti-Tumor and Anti-Angiogenic Activities. Cancer Lett., 348:88-, 2014 Cited by PubMed 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. PubMed: 24657306DOI: 10.1016/J.CANLET.2014.03.007 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (2.05 Å) |
Structure validation
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