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Updated: Sep 25, 2025

Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
Published on: September 30, 2019
Signaling Pathway and Small-Molecule Drug Discovery of FGFR: A Comprehensive Review
Jia Zheng1, Wei Zhang1, Linfeng Li1
1Center for Novel Target and Therapeutic Intervention, Institute of Life Sciences, Chongqing Medical University, Chongqing, China.
Abstract:
Targeted therapy is a groundbreaking innovation for cancer treatment. Among the receptor tyrosine kinases, the fibroblast growth factor receptors (FGFRs) garnered substantial attention as promising therapeutic targets due to their fundamental biological functions and frequently observed abnormality in tumors. In the past 2 decades, several generations of FGFR kinase inhibitors have been developed. This review starts by introducing the biological basis of FGF/FGFR signaling. It then gives a detailed description of different types of small-molecule FGFR inhibitors according to modes of action, followed by a systematic overview of small-molecule-based therapies of different modalities. It ends with our perspectives for the development of novel FGFR inhibitors.
Insights
Targeted cancer therapy innovations include fibroblast growth factor receptor (FGFR) inhibitors. This review details FGFR signaling, inhibitor types, and future perspectives for novel targeted therapies.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Fibroblast growth factor receptors (FGFRs) are key targets in cancer therapy.
- FGFRs are receptor tyrosine kinases with critical biological roles.
- Aberrant FGFR signaling is common in various tumors.
Purpose of the Study:
- To review the biological basis of FGF/FGFR signaling.
- To categorize small-molecule FGFR inhibitors by mechanism of action.
- To provide an overview of small-molecule-based FGFR therapies and future directions.
Main Methods:
- Literature review of FGF/FGFR signaling pathways.
- Classification of FGFR inhibitors based on their modes of action.
- Systematic analysis of small-molecule therapies targeting FGFR.
Main Results:
- Detailed explanation of FGF/FGFR signaling pathways.
- Categorization of multiple generations of FGFR kinase inhibitors.
- Overview of diverse small-molecule-based therapeutic modalities.
Conclusions:
- FGFRs represent a significant target for innovative cancer treatments.
- Small-molecule inhibitors offer a promising avenue for targeted therapy.
- Further development of novel FGFR inhibitors is essential for advancing cancer care.
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