68Ga-labeled cyclic NGR peptide for microPET imaging of CD13 receptor expression

Molecules. 2014 Aug 5;19(8):11600-12. doi: 10.3390/molecules190811600.

Abstract

Peptides containing the asparagines-glycine-arginine (NGR) motif have been identified as specific ligands binding to CD13/aminopeptidase N (APN) receptor, a tumor neovascular biomarker. In this study, we synthesized a novel NGR-containing peptide (NOTA-G3-NGR), and labeled NOTA-G3-NGR with (68)Ga (t1/2 = 67.7 min). The resulting (68)Ga-NOTA-G3-NGR peptide was subject to in vitro and in vivo characterization. The microPET imaging results revealed that the (68)Ga-NOTA-G3-NGR peptide exhibits rapid and specific tumor uptake, and high tumor-to-background contrast in a subcutaneous HT-1080 fibrosarcoma mouse model. We concluded that the (68)Ga-NOTA-G3-NGR peptide has potential in the diagnosis of CD13-targeted tumor angiogenesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminopeptidases / genetics
  • Aminopeptidases / metabolism*
  • Animals
  • CD13 Antigens / genetics
  • CD13 Antigens / metabolism*
  • Cell Line, Tumor
  • Female
  • Gallium Radioisotopes* / chemistry
  • Gene Expression
  • Heterografts
  • Humans
  • Mice
  • Molecular Imaging*
  • Oligopeptides* / chemistry
  • Oligopeptides* / metabolism
  • Positron-Emission Tomography*
  • Protein Binding
  • Signal-To-Noise Ratio
  • Tissue Distribution

Substances

  • Gallium Radioisotopes
  • NGR peptide
  • Oligopeptides
  • Aminopeptidases
  • CD13 Antigens