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Updated: May 9, 2026
07:32
Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
Published on: September 30, 2019
[Developing FGFR inhibitors as potential anti-cancer agents]
Lilian Zsákai1, Gábor Németh, Csaba Szántai-Kis
1Orvosi Vegytani, Molekuláris Biológiai és Patobiokémiai Intézet, Semmelweis Egyetem.
Acta Pharmaceutica Hungarica
|August 10, 2013
Summary
Fibroblast Growth Factor Receptor (FGFR) inhibitors show promise for cancer treatment. Researchers developed novel benzotiophene and oxindole compounds targeting FGFR signaling pathways for therapeutic applications.
Area of Science:
- Molecular Biology
- Oncology
- Medicinal Chemistry
Background:
- The Fibroblast Growth Factor Receptor (FGFR) family comprises four tyrosine kinases (FGFR1-4) crucial for physiological processes like cell proliferation and tissue repair.
- Aberrant FGFR signaling, through overexpression or mutation, drives various cancers, including breast, pancreas, gastric tumors, and multiple myeloma.
Purpose of the Study:
- To identify and develop novel small molecule FGFR inhibitors for targeted cancer therapy.
- To explore benzotiophene and oxindole derivatives as potential lead compounds for FGFR-targeted signal transduction therapies.
Main Methods:
- In silico modeling for lead compound design.
- In vitro biochemical assays to assess inhibitory activity.
- Cell line testing, including cytotoxicity assays, to evaluate efficacy on relevant cancer models.
Main Results:
- Development of two distinct lead molecule series based on benzotiophene and oxindole scaffolds.
- Validation of these compounds through a comprehensive range of in silico, in vitro, and cell-based assays.
Conclusions:
- Novel benzotiophene and oxindole compounds demonstrate potential as FGFR inhibitors.
- These findings support the development of FGFR-targeted therapies for cancers driven by aberrant FGFR signaling.
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