A peptide encoded by exon 6 of VEGF (EG3306) inhibits VEGF-induced angiogenesis in vitro and ischaemic retinal neovascularisation in vivo

Biochem Biophys Res Commun. 2003 Mar 21;302(4):793-9. doi: 10.1016/s0006-291x(03)00222-5.

Abstract

VEGF is an important mediator of pathological angiogenesis in the eye and is a target for the development of novel anti-angiogenic molecules. In a previous study we identified 12-amino acid peptides derived from exon 6 of VEGF that inhibited VEGF binding to its receptors in HUVECs, endothelial cell functions, and in vitro angiogenesis. Screening of a series of truncated peptides corresponding to the inhibitory region of exon 6 identified a seven amino acid residue peptide, RKRKKSR, as the minimum exon 6-encoded sequence which retains the ability to inhibit VEGF receptor binding and angiogenesis in vitro. The effect of the seven-residue peptide was examined in a mouse model of ischaemic retinal neovascularisation. Administration of the peptide caused a 50% inhibition of retinal neovascularisation and was as effective in inhibiting ischaemic angiogenesis as soluble Flt-1 adenovirus. These results demonstrate that a seven amino acid VEGF exon 6-derived peptide is an effective inhibitor of ocular neovascularisation in vivo, and may have applications in the treatment of pathophysiological ocular neovascularisation in human disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Culture Media, Serum-Free
  • Disease Models, Animal
  • Endothelial Growth Factors / genetics*
  • Endothelial Growth Factors / metabolism*
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / metabolism
  • Exons
  • Female
  • Humans
  • Intercellular Signaling Peptides and Proteins / genetics*
  • Intercellular Signaling Peptides and Proteins / metabolism*
  • Ischemia / metabolism*
  • Lymphokines / genetics*
  • Lymphokines / metabolism*
  • Mice
  • Mice, Inbred C57BL
  • Peptides / genetics
  • Peptides / metabolism*
  • Pregnancy
  • Retina / cytology
  • Retina / pathology
  • Retinal Neovascularization / genetics
  • Retinal Neovascularization / metabolism*
  • Vascular Endothelial Growth Factor A
  • Vascular Endothelial Growth Factors

Substances

  • Culture Media, Serum-Free
  • Endothelial Growth Factors
  • Intercellular Signaling Peptides and Proteins
  • Lymphokines
  • Peptides
  • Vascular Endothelial Growth Factor A
  • Vascular Endothelial Growth Factors