Direct electrophilic radiofluorination of a cyclic RGD peptide for in vivo alpha(v)beta3 integrin related tumor imaging

Nucl Med Biol. 2003 Jan;30(1):1-9. doi: 10.1016/s0969-8051(02)00387-6.

Abstract

The association of the alpha(v)beta(3) integrin with tumor metastasis and tumor related angiogenesis has been suggested. Therefore, by imaging the alpha(v)beta(3) receptor with PET, information concerning the tumor status could be obtained. Cyclic peptides including the RGD sequence, were radiolabeled by direct electrophilic fluorination with [(18)F]AcOF. In tumor-bearing mice, the labeled peptides accumulated at the tumor with a high tumor to blood ratio. These findings suggest that an assessment of tumor characteristics may be obtained by using these (18)F-labeled peptides.

Publication types

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

MeSH terms

  • Acetates / administration & dosage
  • Acetates / chemical synthesis
  • Acetates / pharmacokinetics
  • Adenocarcinoma / diagnostic imaging*
  • Adenocarcinoma / metabolism*
  • Animals
  • Back / diagnostic imaging
  • Colonic Neoplasms / diagnostic imaging
  • Colonic Neoplasms / metabolism
  • Esters / administration & dosage
  • Esters / chemical synthesis
  • Esters / pharmacokinetics
  • Fluorine Radioisotopes / administration & dosage
  • Fluorine Radioisotopes / chemistry
  • Fluorine Radioisotopes / pharmacokinetics*
  • Humans
  • Injections, Intravenous
  • Integrin alphaVbeta3 / administration & dosage
  • Integrin alphaVbeta3 / chemistry
  • Integrin alphaVbeta3 / metabolism*
  • Isotope Labeling / methods
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Neoplasm Transplantation
  • Organ Specificity
  • Oxidation-Reduction
  • Radiopharmaceuticals / administration & dosage
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics
  • Sensitivity and Specificity
  • Tissue Distribution
  • Tomography, Emission-Computed / methods

Substances

  • Acetates
  • Esters
  • Fluorine Radioisotopes
  • Integrin alphaVbeta3
  • Radiopharmaceuticals
  • acetyl hypofluorite