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Updated: Jan 17, 2026

Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
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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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Small-molecule FGFR-targeted medicinal chemistry: Advances since 2020 and future perspectives

Hao Yue1, Yu Wang1, Na Zhang1

  • 1School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, PR China.

European Journal of Medicinal Chemistry
|September 13, 2025
PubMed

Insights

Fibroblast Growth Factor Receptor (FGFR) inhibitors show promise in cancer treatment but face challenges like toxicity and resistance. Next-generation FGFR therapeutics aim to improve selectivity and overcome resistance for better patient outcomes.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Fibroblast Growth Factor Receptors (FGFRs) are implicated in various cancers due to alterations like mutations and amplifications.
  • FGFR inhibitors offer therapeutic potential but are limited by off-target toxicities and acquired resistance.

Purpose of the Study:

  • To review recent advances (2020-present) in FGFR inhibitors and degraders.
  • To discuss strategies for enhancing isoform selectivity and overcoming resistance mutations.
  • To provide insights for developing improved FGFR-targeted therapies.

Main Methods:

  • Literature review of FGFR inhibitors and degraders published from 2020 to the present.
  • Analysis of structure-activity relationships (SARs), binding modes, and biological evaluations.
  • Discussion of resistance mechanisms and subtype selectivity.

Main Results:

  • Significant progress has been made in designing selective FGFR inhibitors and degraders.
  • Understanding resistance mechanisms is crucial for developing next-generation agents.
  • Enhanced isoform selectivity is a key strategy for improving therapeutic efficacy.

Conclusions:

  • Next-generation FGFR therapeutics are essential to address limitations of current treatments.
  • Targeting FGFRs with improved selectivity and resistance-overcoming strategies holds promise for oncology.
  • Further research into FGFR biology and drug development is warranted.
Keywords:
Acquired resistanceFGFRInhibitorsPROTACsSubtype selectivity

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