title: Peptidomimetic suppresses proliferation and invasion of gastric cancer cells by fibroblast growth factor 2 signaling cascade blockage.
abstract: Fibroblast growth factor 2 (FGF2) is closely involved in a variety of tumors, including gastric cancer (GC). FGF2 inhibitors exert good antitumor activity, but no FGF2 inhibitor has been employed for clinical use. To obtain a low-toxicity, stable peptidomimetic (called P29) target to FGF2, the affinity between P29 and FGF2 was detected by surface plasmon resonance. The stability of P29 was measured by high performance liquid chromatography. MTT assay and transwell assay were used to access the proliferative and invasive ability of GC cells, respectively. Western blot assay and flow cytometric analysis were applied to study the mechanism of P29. P29 possessed high affinity with FGF2 and a longer half-life in vitro. P29 suppressed the FGF2-induced proliferation of GC cells. It also inhibited the phosphorylation of FRS2, ERK1/2, and AKT triggered by FGF2 in GC. In addition, P29 blocked GC cell transformation from the G1/G0 phase to the S phase and weakened the invasive capability of GC cells. In this paper, we present a novel FGF2 inhibitor that could exert improved anticancer effect in GC in vitro.
authors.affiliation: aChemical Biology Research Center, College of Pharmaceutical Sciences bCollege of Information Science and Computer Engineering cSchool of Basic Medical Sciences, Wenzhou Medical University Departments of dDigestive Diseases eEpidemiology, the First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang, China.
authors.forename: Wulan
authors.initials: W
authors.lastname: Li
authors.forename: Xiaojing
authors.initials: X
authors.lastname: Du
authors.forename: Qiuxiang
authors.initials: Q
authors.lastname: Chen
authors.forename: Yanting
authors.initials: Y
authors.lastname: Kang
authors.forename: Chaochao
authors.initials: C
authors.lastname: Xu
authors.forename: Lei
authors.initials: L
authors.lastname: Fan
authors.forename: Hui
authors.initials: H
authors.lastname: Ye
authors.forename: Shilong
authors.initials: S
authors.lastname: Ying
authors.forename: Lingyi
authors.initials: L
authors.lastname: Shi
authors.forename: Rong
authors.initials: R
authors.lastname: Jin
authors.forename: Jianzhang
authors.initials: J
authors.lastname: Wu
authors.forename: Guang
authors.initials: G
authors.lastname: Liang
authors.forename: Xiaokun
authors.initials: X
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor / Q000187:drug effects; D002465:Cell Movement / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D016222:Fibroblast Growth Factor 2 / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D006801:Humans; D009842:Oligopeptides / Q000494:pharmacology*; D057786:Peptidomimetics / Q000494:pharmacology*; D017468:Receptors, Fibroblast Growth Factor / Q000037:antagonists & inhibitors; D015398:Signal Transduction; D013274:Stomach Neoplasms / Q000188:drug therapy*
chemical_list: D000970:Antineoplastic Agents; D009842:Oligopeptides; D057786:Peptidomimetics; D017468:Receptors, Fibroblast Growth Factor; D016222:Fibroblast Growth Factor 2