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Int J Biol Sci 2018; 14(10):1389-1398. doi:10.7150/ijbs.24739

Research Paper

A novel FGFR1-binding peptide exhibits anti-tumor effect on lung cancer by inhibiting proliferation and angiogenesis

Qiaoyan Tan1#, Zuqiang Wang1#, Quan Wang1, Yuanqiang Wang2, Zhifeng Huang3, Nan Su1, Min Jin1, Liang Kuang1, Huabing Qi1, Zhenhong Ni1, Can Li1, Ying Zhu1, Wanling Jiang1, Hangang Chen1, Chuxia Deng4, Xiaolan Du1✉, Yangli Xie1✉, Lin Chen1✉

1. Department of Rehabilitation Medicine, Center of Bone Metabolism and Repair, State Key Laboratory of Trauma, Burns and Combined Injury, Trauma Center, Research Institute of Surgery, Daping Hospital, Third Military Medical University, Chongqing, China.
2. College of Bioengineering, Chongqing Institute of Technology, Chongqing, China.
3. School of Pharmacy, Wenzhou Medical University, Wenzhou, China.
4. Faculty of Health Sciences, University of Macau, Macau SAR, China.
# These authors contributed equally to this work.

Abstract

It has been reported that overactivation of fibroblast growth factor receptor 1 (FGFR1) is an important characteristic found in most non-small cell lung cancer (NSCLC) samples. Here, we identified a FGFR1 inhibitory peptide R1-P2 and investigated its effects on the lung cancer cells growth and angiogenesis in vitro and in vivo. Our results demonstrate that R1-P2 bound to human FGFR1 protein, and efficiently blocked the binding of FGF2 to FGFR1 in A549 and NCI-H460 cells. Moreover, this peptide significantly decreased the proliferation, migration and invasion, but promoted the apoptosis in both cell lines. In addition, R1-P2 treatment effectively inhibited the tumor growth and neovascularization in nude mice with xenografted A549 cells, and R1-P2 also significantly inhibited the FGF2-induced angiogenesis in tube formation experiment and CAM model. We further demonstrated that R1-P2 suppressed lung tumor growth through anti-angiogenic and anti-proliferative activity. Our data may provide a novle leading molecule with potential application in the treatment of FGFR1 activation related lung cancers.

Keywords: Phage display, FGFR1, Peptide, Cancer therapy, Lung cancer

This is an open access article distributed under the terms of the Creative Commons Attribution (CC BY-NC) license (https://creativecommons.org/licenses/by-nc/4.0/). See http://ivyspring.com/terms for full terms and conditions.
How to cite this article:
Tan Q, Wang Z, Wang Q, Wang Y, Huang Z, Su N, Jin M, Kuang L, Qi H, Ni Z, Li C, Zhu Y, Jiang W, Chen H, Deng C, Du X, Xie Y, Chen L. A novel FGFR1-binding peptide exhibits anti-tumor effect on lung cancer by inhibiting proliferation and angiogenesis. Int J Biol Sci 2018; 14(10):1389-1398. doi:10.7150/ijbs.24739. Available from http://www.ijbs.com/v14p1389.htm