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Updated: Apr 14, 2026
Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
Published on: September 30, 2019
A peptide derivative serves as a fibroblast growth factor 2 antagonist in human gastric cancer
Lei Fan1,2, Wulan Li1,3, Shilong Ying1
1Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, 325035, China.
Abstract:
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.
Insights
A new peptide derivative, P32, effectively inhibits fibroblast growth factor 2 (FGF2) in gastric cancer cells. This stable compound shows therapeutic potential for treating FGF2-driven gastric tumors.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Fibroblast growth factor 2 (FGF2) is crucial in solid tumor development and progression.
- Elevated FGF2 levels in gastric carcinoma serum indicate its role as a potential therapeutic target.
- Inhibiting FGF2 bioactivity may offer a strategy for human gastric cancer therapy.
Purpose of the Study:
- To develop a stable FGF2-binding peptide derivative for gastric cancer therapy.
- To evaluate the efficacy and mechanism of the novel peptide P32 against FGF2-driven gastric cancer.
Main Methods:
- Isolation and characterization of a novel FGF2-binding peptide derivative (P32) from a less stable precursor (P7).
- Assessment of P32 stability in human plasma (half-life determination).
- In vitro evaluation of P32's inhibitory effects on FGF2-induced proliferation and invasion in gastric cancer cell lines.
- Investigation of P32's anti-proliferation mechanisms, including cell cycle arrest and signaling pathway modulation (AKT, Erk1/2).
Main Results:
- The novel peptide derivative P32 demonstrated enhanced stability with a half-life of up to 12 hours in human plasma.
- P32 significantly inhibited FGF2-induced cell proliferation and invasion in human gastric cancer cell lines.
- P32 induced G0/G1 phase arrest in FGF2-stimulated cells and reduced AKT and Erk1/2 activation.
Conclusions:
- The FGF2-binding peptide derivative P32 offers improved stability and safety compared to its precursor.
- P32 exhibits potent anti-cancer activity against FGF2-driven gastric cancer.
- P32 represents a promising therapeutic candidate for gastric cancer treatment targeting FGF2.
