A novel non-ATP competitive FGFR1 inhibitor with therapeutic potential on gastric cancer through inhibition of cell proliferation, survival and migration

作者：Wu, Jianzhang; Du, Xiaojing; Li, Wulan; Zhou, Yangyang; Bai, Encheng; Kang, Yanting; Chen, Qiuxiang; Fu, Weitao; Yun, Di; Xu, Qing; Qiu, Peihong^*; Jin, Rong^*; Cai, Yuepiao^*; Liang, Guang

来源：Apoptosis, 2017, 22(6): 852-864.

DOI：10.1007/s10495-017-1361-7

• Gastric cancer
• Non-ATP competitive FGFR1 inhibitor
• Proliferation
• Survival
• Migration

Fibroblast growth factor receptor 1 (FGFR1), belonging to receptor tyrosine kinases (RTKs), possesses various biological functions. Over-expression of FGFR1 has been observed in multiple human malignancies. Hence, targeting FGFR1 is an attractive prospect for the advancement of cancer treatment options. Here, we present a novel small molecular FGFR1 inhibitor L16H50, which can inhibit FGFR1 kinase in an ATP-independent manner. It potently inhibits FGFR1-mediated signaling in a gastric cancer cell line, resulting in inhibition of cell growth, survival and migration. It also displays an outstanding anti-tumor activity in a gastric cancer xenograft tumor model by targeting FGFR1 signaling. These results show that L16H50 is a potent non-ATP-competitive FGFR1 inhibitor and may provide strong rationale for its evaluation in gastric cancer patients.

• 出版日期2017-6
• 单位温州医科大学; 温州大学