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Updated: Jun 25, 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

FGFR2-related pathogenesis and FGFR2-targeted therapeutics (Review)

Yuriko Katoh1, Masaru Katoh

  • 1M&M Medical BioInformatics, Hongo 113-0033, Japan.

International Journal of Molecular Medicine
|February 13, 2009
PubMed

Insights

Fibroblast Growth Factor Receptor 2 (FGFR2) plays dual roles in cancer, with specific genetic alterations linked to tumor growth. FGFR2 inhibitors show promise for treatment but may hinder cancer prevention due to impaired cellular defense mechanisms.

Area of Science:

  • Genetics and Oncology
  • Molecular Biology
  • Cancer Research

Background:

  • The FGFR2 gene encodes crucial FGF receptors (FGFR2b/FGFR2c) with context-dependent oncogenic and anti-oncogenic functions.
  • Genetic alterations like SNPs, missense mutations, and copy number gains in FGFR2 are implicated in various cancers, including breast, gastric, prostate, and bladder cancers.
  • FGFR2 signaling dysregulation, driven by epigenetic and genetic factors, contributes to carcinogenesis, while loss of FGFR2b signaling can promote tumor progression and oxidative stress.

Purpose of the Study:

  • To elucidate the multifaceted roles of FGFR2 in cancer development and progression.
  • To explore the implications of FGFR2 genetic variations and signaling in different cancer types.
  • To evaluate the therapeutic potential and risks associated with FGFR2-targeted interventions.

Main Methods:

  • Analysis of FGFR2 gene structure, including single nucleotide polymorphisms (SNPs) and copy number variations.
  • Investigation of FGFR2 isoform switching (FGFR2b to FGFR2c) in cancer progression.
  • Assessment of FGFR2 signaling pathways, including Nrf2-mediated detoxification and epithelial-to-mesenchymal transition (EMT).
  • Review of existing and emerging FGFR2-targeted therapeutic strategies (small molecules, antibodies, RNA-based therapies).

Main Results:

  • FGFR2 SNPs are associated with breast cancer risk via allelic upregulation.
  • FGFR2 mutations and copy number gains activate oncogenic signaling in breast and gastric cancers.
  • Spliceosome dysregulation drives FGFR2 isoform switching in prostate and bladder cancers.
  • Loss of FGFR2b signaling in mice increases carcinogenesis sensitivity and promotes EMT and oxidative stress.
  • FGFR2 inhibitors are potential therapeutics for cancers with FGFR2 alterations.

Conclusions:

  • FGFR2 signaling is a critical determinant in cancer, with both oncogenic and protective roles.
  • Targeting FGFR2 offers therapeutic opportunities for specific cancer mutations and amplifications.
  • Caution is advised for using FGFR2 inhibitors in cancer prevention due to potential impairment of cytoprotective mechanisms against oxidative stress.

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