期刊
TUMOR BIOLOGY
卷 36, 期 9, 页码 7233-7241出版社
SAGE PUBLICATIONS LTD
DOI: 10.1007/s13277-015-3435-x
关键词
FGF2 binding; Peptide derivative; Half-life; Non-toxicity; Anti-proliferation
类别
资金
- National Natural Science Foundation of China [81102310, 81402839, 81272462]
- Zhejiang Province Natural Science Funding of China [Y4110029]
- Technology Foundation for Medical Science of Zhejiang Province [2012KYB127]
- Key Laboratory of Functional Protein Research of Guangdong Higher Education Institutes, Jinan University
- Fundamental Research Funds for the Central Universities
- Guangdong Provincial Thousand-Hundred-Ten Talent Project
Fibroblast growth factor 2 (FGF2) plays a critical role in tumorigenesis and progression of solid tumor and is upregulated in gastric carcinoma serum. Therefore, it is regarded as a potential therapeutic target of human gastric cancer. Suppression of bioactivities of FGF2 may contribute to human gastric cancer therapy. Herein, we obtained a novel FGF2-binding peptide derivative (named P32), which originated from a previously isolated P7 peptide with poor stability. We proved that P32, which had a half-life in human plasma up to 12 h, enhanced stability and exerted strong inhibitory effect on FGF2-induced cell proliferation and invasion in human gastric cancer cell lines. Further investigations revealed that the underlying anti-proliferation mechanisms of P32 in vitro included arresting FGF2-stimulated cells at the G0/G1 phase and reducing the activation of AKT and Erk1/2 cascades. The FGF2-binding peptide derivative P32 has improved stability, is relatively safe, and may have therapeutic potential in FGF2-driven gastric cancer.
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