4C7T

Focal Adhesion Kinase catalytic domain in complex with a diarylamino- 1,3,5-triazine inhibitor

4C7T の概要

• エントリーDOI: 10.2210/pdb4c7t/pdb
• 分子名称: 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)
• 機能のキーワード: transferase, kinase inhibitor, atp-binding, integrin signaling
• 由来する生物種: GALLUS GALLUS (CHICKEN)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 32238.29

構造登録者

Le Coq, J.,Lietha, D. (登録日: 2013-09-25, 公開日: 2014-04-02, 最終更新日: 2023-12-20)

主引用文献

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

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: 24657306
DOI: 10.1016/J.CANLET.2014.03.007

実験手法

X-RAY DIFFRACTION (2.05 Å)