In vivo NIRF imaging-guided delivery of a novel NGR-VEGI fusion protein for targeting tumor vasculature

Amino Acids. 2014 Dec;46(12):2721-32. doi: 10.1007/s00726-014-1828-6. Epub 2014 Sep 3.

Abstract

Pathological angiogenesis is crucial in tumor growth, invasion and metastasis. Previous studies demonstrated that the vascular endothelial growth inhibitor (VEGI), a member of the tumor necrosis factor superfamily, can be used as a potent endogenous inhibitor of tumor angiogenesis. Molecular probes containing the asparagine-glycine-arginine (NGR) sequence can specifically bind to CD13 receptor which is overexpressed on neovasculature and several tumor cells. Near-infrared fluorescence (NIRF) optical imaging for targeting tumor vasculature offers a noninvasive method for early detection of tumor angiogenesis and efficient monitoring of response to anti-tumor vasculature therapy. The aim of this study was to develop a new NIRF imaging probe on the basis of an NGR-VEGI protein for the visualization of tumor vasculature. The NGR-VEGI fusion protein was prepared from prokaryotic expression, and its function was characterized in vitro. The NGR-VEGI protein was then labeled with a Cy5.5 fluorophore to afford Cy5.5-NGR-VEGI probe. Using the NIRF imaging technique, we visualized and quantified the specific delivery of Cy5.5-NGR-VEGI protein to subcutaneous HT-1080 fibrosarcoma tumors in mouse xenografts. The Cy5.5-NGR-VEGI probe exhibited rapid HT-1080 tumor targeting, and highest tumor-to-background contrast at 8 h post-injection (pi). Tumor specificity of Cy5.5-NGR-VEGI was confirmed by effective blocking of tumor uptake in the presence of unlabeled NGR-VEGI (20 mg/kg). Ex vivo NIRF imaging further confirmed in vivo imaging findings, demonstrating that Cy5.5-NGR-VEGI displayed an excellent tumor-to-muscle ratio (18.93 ± 2.88) at 8 h pi for the non-blocking group and significantly reduced ratio (4.92 ± 0.75) for the blocking group. In conclusion, Cy5.5-NGR-VEGI provided highly sensitive, target-specific, and longitudinal imaging of HT-1080 tumors. As a novel theranostic protein, Cy5.5-NGR-VEGI has the potential to improve cancer treatment by targeting tumor vasculature.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis
  • Carbocyanines / chemistry
  • Drug Delivery Systems / instrumentation
  • Drug Delivery Systems / methods*
  • Female
  • Fluorescent Dyes / chemistry
  • Humans
  • Mice
  • Mice, Nude
  • Molecular Imaging
  • Molecular Probes / chemistry
  • Neoplasms / chemistry
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Neoplasms / physiopathology
  • Neovascularization, Pathologic / drug therapy*
  • Neovascularization, Pathologic / pathology
  • Neovascularization, Pathologic / physiopathology
  • Oligopeptides / administration & dosage*
  • Oligopeptides / chemistry
  • Oligopeptides / genetics
  • Oligopeptides / metabolism
  • Spectroscopy, Near-Infrared
  • Tumor Necrosis Factor Ligand Superfamily Member 15 / administration & dosage*
  • Tumor Necrosis Factor Ligand Superfamily Member 15 / chemistry
  • Tumor Necrosis Factor Ligand Superfamily Member 15 / genetics
  • Tumor Necrosis Factor Ligand Superfamily Member 15 / metabolism

Substances

  • CY5.5 cyanine dye
  • Carbocyanines
  • Fluorescent Dyes
  • Molecular Probes
  • NGR peptide
  • Oligopeptides
  • TNFSF15 protein, human
  • Tumor Necrosis Factor Ligand Superfamily Member 15