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Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
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Targeting Drugs Against Fibroblast Growth Factor(s)-Induced Cell Signaling

Shilpi Agrawal1, Sanhita Maity1, Zeina AlRaawi1

  • 1Department of Chemistry and Biochemistry, University of Arkansas, Fayetteville, Arkansas, United States.

Current Drug Targets
|October 13, 2020
PubMed
Abstract

Insights

Fibroblast growth factor (FGF) and fibroblast growth factor receptor (FGFR) signaling pathways are crucial in development and disease. Aberrant signaling drives cancer, necessitating novel therapeutic strategies beyond current FGFR inhibitors.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • The fibroblast growth factor (FGF) family comprises 23 proteins regulating development, tissue repair, and angiogenesis.
  • FGF binding to fibroblast growth factor receptors (FGFRs), tyrosine kinase receptors, is heparin-dependent, activating downstream pathways like RAS-MAPK and PI3K-AKT.
  • Dysregulation of FGF/FGFR signaling via gene amplification, mutations, or rearrangements is common in cancer and affects development and homeostasis.

Purpose of the Study:

  • To review the biology, chemistry, and functions of FGFs and their therapeutic applications.
  • To discuss FGFR signaling aberrations and targeted therapies for disorders including cancer, diabetes, and fatty liver disease.
  • To highlight the development of novel drugs targeting FGF/FGFR signaling.

Main Methods:

  • Comprehensive literature review of FGF/FGFR signaling.
  • Analysis of current therapeutic strategies and drug development for FGF/FGFR-related disorders.
  • Discussion of preclinical and clinical studies on novel FGFR inhibitors.

Main Results:

  • FGF/FGFR signaling plays a vital role in various physiological and pathological processes.
  • Aberrant FGFR signaling is implicated in cancer development and progression.
  • Current FGFR inhibitors face challenges due to resistance mechanisms, driving research into new therapeutic approaches.

Conclusions:

  • Targeting FGF/FGFR signaling offers therapeutic potential for cancers and other diseases.
  • Development of novel FGFR-targeting drugs with different mechanisms of action is crucial.
  • Overcoming drug resistance is key to realizing the full clinical benefit of FGF/FGFR therapies.
Keywords:
FGF/FGFR signalingFibroblast growth factoraberrant FGFR signalingcancerfibroblast growth factor receptor

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