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Updated: Feb 1, 2026

Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
Published on: September 30, 2019
Structure, activation and dysregulation of fibroblast growth factor receptor kinases: perspectives for clinical
Brendan Farrell1, Alexander L Breeze2
1Astbury Centre for Structural Molecular Biology, Faculty of Biological Sciences, University of Leeds, Leeds LS2 9JT, U.K.
Abstract:
The receptor tyrosine kinase family of fibroblast growth factor receptors (FGFRs) play crucial roles in embryonic development, metabolism, tissue homeostasis and wound repair via stimulation of intracellular signalling cascades. As a consequence of FGFRs' influence on cell growth, proliferation and differentiation, FGFR signalling is frequently dysregulated in a host of human cancers, variously by means of overexpression, somatic point mutations and gene fusion events. Dysregulation of FGFRs is also the underlying cause of many developmental dysplasias such as hypochondroplasia and achondroplasia. Accordingly, FGFRs are attractive pharmaceutical targets, and multiple clinical trials are in progress for the treatment of various FGFR aberrations. To effectively target dysregulated receptors, a structural and mechanistic understanding of FGFR activation and regulation is required. Here, we review some of the key research findings from the last couple of decades and summarise the strategies being explored for therapeutic intervention.
Insights
Fibroblast growth factor receptors (FGFRs) are vital for development and tissue repair. Dysregulated FGFR signaling drives cancers and developmental disorders, making them key pharmaceutical targets for new therapies.
Area of Science:
- Molecular Biology
- Cell Signaling
- Oncology
Background:
- Fibroblast growth factor receptors (FGFRs) are receptor tyrosine kinases crucial for embryonic development, metabolism, tissue homeostasis, and wound repair.
- FGFR signaling pathways regulate cell growth, proliferation, and differentiation.
- Dysregulation of FGFRs, through overexpression, mutations, or gene fusions, is implicated in various human cancers and developmental disorders like hypochondroplasia and achondroplasia.
Purpose of the Study:
- To review key research findings on fibroblast growth factor receptor (FGFR) activation and regulation over the past two decades.
- To summarize current therapeutic intervention strategies targeting FGFR aberrations.
- To highlight the importance of understanding FGFR structure and mechanism for effective drug development.
Main Methods:
- Literature review of research findings from the last 20 years.
- Synthesis of information on FGFR signaling pathways.
- Analysis of therapeutic strategies for FGFR-related diseases.
Main Results:
- FGFRs play critical roles in multiple biological processes.
- Aberrant FGFR signaling is a common driver in oncogenesis and developmental dysplasias.
- Multiple FGFR-targeting drugs are currently in clinical trials.
Conclusions:
- FGFRs are significant pharmaceutical targets due to their roles in cancer and developmental disorders.
- A comprehensive understanding of FGFR activation and regulation is essential for developing effective therapies.
- Ongoing research and clinical trials show promise for treating FGFR-driven diseases.
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