A novel FGF2 antagonist peptide P8 with potent antiproliferation activity

作者：Fan, Lei; Xie, Hang; Chen, Lingzi; Ye, Hui; Ying, Shilong; Wang, Cong; Wu, Xiaoping; Li, Wulan^*; Wu, Jianzhang; Liang, Guang; Li, Xiaokun

来源：Tumor Biology, 2014, 35(10): 10571-10579.

DOI：10.1007/s13277-014-2356-4

• FGF2-binding peptide
• Cell proliferation
• Cell cycle
• Signaling pathway
• Multi-targets

Some fibroblast growth factors (FGFs) play a critical role in tumorigenesis and progression. Among them, FGF2 was highly expressed in some tumors, and antagonists binding to FGF2 can suppress the growth of tumor cells. Therefore, FGF2 has been considered as an important target in cancer therapy. In this study, we identified a novel FGF2-binding short peptide (P8, PLLQATAGGGS-NH2) using phage display technology and alanine scanning. The P8 peptide suppressed FGF2-induced proliferation with no cytotoxic effect on cells, arrested the cycle at the G0/G1 phase in B16-F10 cells, and downregulated the activation of fibroblast growth factor receptor substrate 2 alpha (FRS2 alpha)/ERK cascade in B16-F10, NIH-H460, and SGC-7901 cells. Besides, P8 peptide can also inhibit the phosphorylation of FRS2 alpha stimulated by FGF1 and KGF2. These implied that P8 peptide may develop as a multi-target antagonist peptide contributing to tumor treatment.

• 出版日期2014-10
• 单位暨南大学; 温州医科大学