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Updated: Jan 26, 2026

Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
07:32

Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library

Published on: September 30, 2019

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Identification of a peptide antagonist of the FGF1-FGFR1 signaling axis by phage display selection

Magdalena Lipok1,2, Anna Szlachcic1,2, Kinga Kindela1

  • 1Department of Protein Engineering, Faculty of Biotechnology, University of Wroclaw, Poland.

FEBS Open Bio
|April 11, 2019
PubMed

Insights

Researchers identified cyclic peptide F8 as a potent antagonist of fibroblast growth factor 1 (FGF1)-fibroblast growth factor receptor 1 (FGFR1) interaction. This peptide shows promise for developing new therapies against FGFR1-expressing cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Fibroblast growth factor receptor 1 (FGFR1) overexpression is prevalent in lung and breast cancers.
  • Current FGFR1-targeted drugs (small-molecule tyrosine kinase inhibitors) have limited specificity.
  • There is a need for novel therapeutics targeting the extracellular domain of FGFR1.

Purpose of the Study:

  • To identify novel molecules targeting the FGF1-FGFR1 interaction interface.
  • To evaluate the potential of cyclic peptides as FGFR1 antagonists for cancer therapy.

Main Methods:

  • Phage display technique was employed to select cyclic peptides.
  • Enzyme-linked immunosorbent assay (ELISA) and in vitro cell assays were utilized.
  • BA/F3 cells with and without FGFR1 expression were used for validation.

Main Results:

  • Cyclic peptides F8 and G10 were identified as binders of the FGF1-FGFR1 interface.
  • Cyclic peptide F8 demonstrated superior efficacy in blocking FGF1-FGFR1 interaction.
  • Peptide F8 significantly inhibited FGF1-induced proliferation of FGFR1-expressing cells by over 40%.

Conclusions:

  • Cyclic peptide F8 acts as a functional antagonist of the FGF1-FGFR1 interaction.
  • Peptide F8 holds potential for the development of targeted therapies against FGFR1-driven cancers.
Keywords:
FGF1FGFR1fibroblast growth factor receptor 1inhibitorpeptidephage display

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