期刊
ANTI-CANCER DRUGS
卷 27, 期 3, 页码 164-172出版社
LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/CAD.0000000000000312
关键词
FGF; FGFR; gastric cancer; invasion; proliferation; target therapy
资金
- ZheJiang Province Natural Science Funding of China [LY14H160044, Y4110029, LY13H160022]
- National Natural Science Foundation of China [81402839, 81102310]
- Technology Foundation for Medical Science of Zhejiang Province [2012KYB127]
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.
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