Anginex-conjugated liposomes for targeting of angiogenic endothelial cells

Bioconjug Chem. 2007 May-Jun;18(3):785-90. doi: 10.1021/bc060316h. Epub 2007 Mar 23.

Abstract

Identification of a tumor angiogenesis specific ligand would allow targeting of tumor vasculature. Lipidic vehicles can be used to deliver therapeutic agents for treatment of disease or contrast agents for molecular imaging. A targeting ligand would allow specific delivery of such formulations to angiogenic sites, thereby reducing side effects and gaining efficiency. Anginex, a synthetic 33-mer angiostatic peptide, has been described to home angiogenically activated endothelium, suggesting an ideal candidate as targeting ligand. To investigate this application of anginex, fluorescently labeled paramagnetic liposomes were conjugated with anginex. Using phase contrast and fluorescence microscopy as well as magnetic resonance imaging (MRI), we demonstrate that anginex-conjugated liposomes bind specifically to activated endothelial cells, suggesting application as an angiogenesis targeting agent for molecular targeting and molecular imaging of angiogenesis-dependent disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Cells, Cultured
  • Endothelial Cells / metabolism
  • Endothelium, Vascular / chemistry
  • Endothelium, Vascular / metabolism*
  • Humans
  • Liposomes / chemistry
  • Liposomes / metabolism
  • Magnetic Resonance Spectroscopy
  • Molecular Sequence Data
  • Peptides
  • Pharmaceutical Vehicles / analysis
  • Pharmaceutical Vehicles / chemistry
  • Pharmaceutical Vehicles / metabolism*
  • Proteins / analysis
  • Proteins / chemistry
  • Proteins / metabolism*

Substances

  • Liposomes
  • Peptides
  • Pharmaceutical Vehicles
  • Proteins
  • betapep-25 protein, synthetic