Targeting of gelatinase activity with a radiolabeled cyclic HWGF peptide

Nucl Med Biol. 2004 Apr;31(3):337-44. doi: 10.1016/j.nucmedbio.2003.10.011.

Abstract

Matrix metalloproteinases (MMPs) are a family of proteinases that play an important role in cancer as well as in numerous diseases. In this article, we describe the labeling of a phage display selected cyclic decapeptide containing the HWGF (histidine-tryptophane-glycine-phenylalanine) sequence to target MMP-2 and MMP-9. To evaluate the ability of this labeled peptide to monitor non invasively MMP-2 and MMP-9 activity, in vitro studies, biodistribution, competition studies and plasma metabolites analyses in Lewis Lung cancer tumor bearing mice were performed.

Publication types

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

MeSH terms

  • Animals
  • Biomarkers, Tumor / metabolism*
  • Drug Delivery Systems / methods
  • Enzyme Activation
  • Female
  • Gelatinases / metabolism
  • Iodine Radioisotopes / chemistry
  • Iodine Radioisotopes / pharmacokinetics
  • Isotope Labeling / methods
  • Lung Neoplasms / diagnostic imaging*
  • Lung Neoplasms / metabolism*
  • Matrix Metalloproteinase 2 / metabolism*
  • Matrix Metalloproteinase 9 / metabolism*
  • Metabolic Clearance Rate
  • Mice
  • Mice, Inbred BALB C
  • Organ Specificity
  • Peptides, Cyclic / chemical synthesis
  • Peptides, Cyclic / pharmacokinetics*
  • Radionuclide Imaging
  • Radiopharmaceuticals / pharmacokinetics
  • Tissue Distribution

Substances

  • Biomarkers, Tumor
  • Iodine Radioisotopes
  • Peptides, Cyclic
  • Radiopharmaceuticals
  • Gelatinases
  • Matrix Metalloproteinase 2
  • Matrix Metalloproteinase 9