title: A novel FGF2 antagonist peptide P8 with potent antiproliferation activity.
abstract: 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 2α (FRS2α)/ERK cascade in B16-F10, NIH-H460, and SGC-7901 cells. Besides, P8 peptide can also inhibit the phosphorylation of FRS2α stimulated by FGF1 and KGF2. These implied that P8 peptide may develop as a multi-target antagonist peptide contributing to tumor treatment.
authors: Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical University, 325035, Wenzhou, China.
authors: Lei
authors: L
authors: Fan
authors: Hang
authors: H
authors: Xie
authors: Lingzi
authors: L
authors: Chen
authors: Hui
authors: H
authors: Ye
authors: Shilong
authors: S
authors: Ying
authors: Cong
authors: C
authors: Wang
authors: Xiaoping
authors: X
authors: Wu
authors: Wulan
authors: W
authors: Li
authors: Jianzhang
authors: J
authors: Wu
authors: Guang
authors: G
authors: Liang
authors: Xiaokun
authors: X
authors: Li
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D015153:Blotting, Western; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D016222:Fibroblast Growth Factor 2 / Q000037:antagonists & inhibitors*; D006801:Humans; D010455:Peptides / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; C541129:P8 peptide; D010455:Peptides; D016222:Fibroblast Growth Factor 2