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

• Rapid method for labeling peptides with fluorine-18.
• Preparation of MUC1-[18F]SFB and BBN-[18F]SFB peptide conjugates.
• High binding affinity of radioconjugates for breast cancer cell line.

In an attempt to develop a new and rapid method for labeling peptides with 18F, we have synthesized MUC1-[18F]SFB and BBN-[18F]SFB peptide conjugates using a convenient and one-step simple reactions. Radiochemical yields for MUC1-[18F]SFB and BBN-[18F]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.