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Updated: Sep 27, 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

Small-molecule inhibitors of fibroblast growth factor receptor (FGFR) tyrosine kinases (TK)

Fabrizio Manetti1, Maurizio Botta

  • 1Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via Aldo Moro, I-53100 Siena, Italy.

Current Pharmaceutical Design
|February 7, 2003
PubMed

Insights

This review explores synthetic chemical strategies targeting Fibroblast Growth Factor Receptors (FGFR) to inhibit cancer growth. It details structural properties and structure-activity relationships (SAR) for developing effective FGFR inhibitors.

Area of Science:

  • Molecular Biology
  • Medicinal Chemistry
  • Oncology

Background:

  • Fibroblast Growth Factor Receptors (FGFR) are key polypeptides in development and adult tissues.
  • FGFR signaling is crucial for cell differentiation, development, mitogenesis, and angiogenesis.
  • FGFR are implicated in both normal and malignant cellular processes.

Purpose of the Study:

  • To review synthetic chemical approaches targeting Fibroblast Growth Factor Receptors (FGFR).
  • To summarize structural properties required for FGFR affinity.
  • To define structure-activity relationships (SAR) for FGFR inhibitors.

Main Methods:

  • Literature survey of synthetic chemical inhibitors targeting FGFR.
  • Analysis of structural properties conferring FGFR affinity.
  • Examination of structure-activity relationships (SAR) for FGFR inhibitors.

Main Results:

  • FGFR inhibitors are designed to block signaling cascades via direct interaction with FGFR.
  • Inhibitors investigated for antiangiogenic and antitumor activities.
  • Key structural features for FGFR affinity are identified.

Conclusions:

  • Synthetic chemistry offers viable strategies for developing FGFR inhibitors.
  • Understanding SAR is critical for designing potent and selective FGFR-targeted therapies.
  • FGFR inhibitors hold promise for antiangiogenesis and antitumor applications.

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