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Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
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A time-resolved live cell imaging assay to identify small molecule inhibitors of FGF2 signaling

Mennatallah Ahmed1, Cyril Legrand1, Ana Yagüe Relimpio1

  • 1Heidelberg University Biochemistry Center, Germany.

FEBS Letters
|May 29, 2019
PubMed

Insights

We developed a new live imaging assay to screen for inhibitors of Fibroblast Growth Factor 2 (FGF2) signaling. This method identifies compounds blocking FGF2-dependent tumor cell survival, crucial for cancer therapy.

Area of Science:

  • Oncology
  • Cell Biology
  • Pharmacology

Background:

  • Fibroblast Growth Factor 2 (FGF2) is a key factor in cell survival and tumor angiogenesis.
  • Targeting FGF2 signaling is a promising strategy for cancer treatment.

Purpose of the Study:

  • To develop and validate a novel time-resolved assay for screening FGF2 signaling inhibitors.
  • To identify small molecules that inhibit FGF2-dependent tumor cell survival.

Main Methods:

  • Live cell imaging of neuroblastoma cells to monitor FGF2 signaling dynamics.
  • High-throughput screening of 8960 small molecules for FGF2 signaling inhibition.
  • Validation of hit compounds using dose-response assays, receptor antagonism, ERK phosphorylation, and chemoresistance models.

Main Results:

  • A novel kinetic FGF2 signaling assay was established and validated.
  • The assay successfully identified compounds inhibiting FGF2 signaling with kinetic resolution.
  • The screening pipeline deselects compounds with pleiotropic effects, enhancing specificity.

Conclusions:

  • The developed assay and experimental pipeline offer a powerful tool for discovering novel FGF2 signaling inhibitors.
  • This approach has significant potential for identifying therapeutics that block FGF2-dependent tumor cell survival and angiogenesis.
Keywords:
FGF2 signalingfibroblast growth factor 2live cell imagingsmall molecule inhibitorstumor cell survivaltumor-induced angiogenesis

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