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Updated: Aug 16, 2026

A Simple Bioassay for the Evaluation of Vascular Endothelial Growth Factors
09:04

A Simple Bioassay for the Evaluation of Vascular Endothelial Growth Factors

Published on: March 15, 2016

Design, synthesis, and evaluation of original carriers for targeting vascular endothelial growth factor receptor

Mario Gonçalves1, Karine Estieu-Gionnet, Thomas Berthelot

  • 1CEA Saclay, DSM/DRECAM/LSI/LPI, 91191, Gif-sur-Yvette Cedex, France.

Pharmaceutical Research
|August 4, 2005
PubMed
Abstract

Insights

Modified cyclo-VEGI peptides show potent antitumor properties and cellular accumulation. These novel molecules are promising for developing targeted delivery systems for cancer and angiogenesis-related diseases.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Angiogenesis, driven by vascular endothelial growth factor (VEGF), is crucial for tumor growth and diseases.
  • VEGF and its receptors are key targets for cancer therapy and imaging.
  • A novel cyclopeptide, cyclo-VEGI, was developed with significant antitumor activity.

Purpose of the Study:

  • To design novel molecules derived from cyclo-VEGI for targeting cancer and angiogenesis-related diseases.
  • To create potential targeting agents based on structural studies of VEGF.

Main Methods:

  • Selective chemical modification of the cyclo-VEGI cyclopeptide.
  • Synthesis and coupling of hydrophilic linkers to create nanocarriers.
  • Evaluation of VEGF binding inhibition using competition assays and fluorescent labeling for cellular uptake studies.

Main Results:

  • Chemical modifications of cyclo-VEGI retained or enhanced its biological activity.
  • Fluorescently labeled cyclo-VEGI demonstrated strong cellular accumulation.
  • The synthesized conjugates show potential as leads for targeted delivery systems.

Conclusions:

  • Modified cyclo-VEGIs are valuable tools for therapeutic targeting and imaging.
  • These compounds offer a versatile platform for developing delivery systems in oncology and other angiogenesis-related conditions.

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