Rapid and one-step radiofluorination of bioactive peptides: potential PET radiopharmaceuticals

Appl Radiat Isot. 2014 Sep:91:17-23. doi: 10.1016/j.apradiso.2014.05.001. Epub 2014 May 14.

Abstract

In an attempt to develop a new and rapid method for labeling peptides with (18)F, we have synthesized MUC1-[(18)F]SFB and BBN-[(18)F]SFB peptide conjugates using a convenient and one-step simple reactions. Radiochemical yields for MUC1-[(18)F]SFB and BBN-[(18)F]SFB peptide conjugates were greater than 70% in less than 30 min synthesis time, thus amenable for automation for the radiofluorination of peptides. in vitro tests on T47D breast cancer cells showed that the significant amounts of the radioconjugates were associated with cell fractions and held sufficient affinities and specificities toward T47D cell line. These radioconjugates may be useful as molecular probes for detecting and staging of breast cancer and monitoring tumor response to treatment.

Keywords: (18)F; (18)F-peptide; Bombesin; Breast cancer; Mucine; PET radiopharmaceuticals.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzoates / chemistry
  • Bombesin / analogs & derivatives*
  • Bombesin / chemistry
  • Breast Neoplasms / diagnostic imaging
  • Cell Line, Tumor
  • Female
  • Fluorine Radioisotopes / chemistry*
  • Humans
  • Isotope Labeling / methods
  • Mucin-1 / chemistry*
  • Positron-Emission Tomography / methods
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Succinimides / chemistry

Substances

  • Benzoates
  • Fluorine Radioisotopes
  • MUC1 protein, human
  • Mucin-1
  • Radiopharmaceuticals
  • Succinimides
  • N-succinimidyl-4-fluorobenzoate
  • Bombesin