Inhibition of endothelial cell migration and angiogenesis by a vascular endothelial growth factor receptor-1 derived peptide

Eur J Cancer. 2008 Sep;44(13):1914-21. doi: 10.1016/j.ejca.2008.06.032. Epub 2008 Aug 3.


Vascular endothelial growth factor receptor-1 (VEGFR-1) exists in two isoforms: a membrane-bound isoform (mVEGFR-1) and a soluble one (sVEGFR-1). mVEGFR-1 is involved in endothelial cell migration and survival supported by VEGF-A and placenta growth factor (PlGF), whereas the biologic function of sVEGFR-1 has not been fully elucidated. We previously reported that sVEGFR-1 induces endothelial cell motility and promotes endothelial cell adhesion. In this study, we tested a set of VEGFR-1-derived peptides for their ability to interfere with endothelial cell migration. Peptide B3 was found to specifically inhibit cell migration induced by sVEGFR-1 and by mVEGFR-1-specific ligands. Moreover, peptide B3 markedly hampered angiogenesis in vitro and in vivo and was found to interfere with VEGFR-1 homodimerisation. Altogether, these data demonstrate that peptide B3 might be a useful tool for the specific inhibition of VEGFR-1 function and might represent a basis for the development of new anti-angiogenic compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / pharmacology*
  • Cell Differentiation / drug effects
  • Cell Movement / drug effects*
  • Cell Proliferation / drug effects
  • Endothelial Cells / drug effects*
  • Endothelial Cells / physiology
  • Humans
  • Neovascularization, Pathologic / prevention & control
  • Peptide Fragments / pharmacology
  • Placenta Growth Factor
  • Pregnancy Proteins / metabolism
  • Umbilical Veins / blood supply*
  • Vascular Endothelial Growth Factor Receptor-1 / physiology*


  • Angiogenesis Inhibitors
  • PGF protein, human
  • Peptide Fragments
  • Pregnancy Proteins
  • Placenta Growth Factor
  • Vascular Endothelial Growth Factor Receptor-1