Solid-phase supported direct ¹⁸F-radiofluorination of peptides

Area of Science:

• Radiochemistry
• Peptide Synthesis
• Positron Emission Tomography (PET) Imaging

Background:

• Widespread use of peptides as molecular tracers in PET is hindered by a lack of universal and efficient labeling methods.
• Current labeling procedures often lack expediency and broad applicability for diverse peptide structures.

Purpose of the Study:

• To develop a proof-of-concept direct radiofluorination procedure for peptides.
• To enable efficient and versatile labeling of peptides for PET applications.
• To overcome existing limitations in peptide-based radiopharmaceutical development.

Main Methods:

• Utilized conventional solid-phase peptide synthesis (SPPS).
• Developed a direct radiofluorination technique compatible with standard amino acids.
• Applied the method to generate various peptide-based radiopharmaceuticals.

Main Results:

• Achieved radiochemical yields of up to 30%.
• Obtained radiochemical purities exceeding 95%.
• Demonstrated compatibility with all standard amino acids in SPPS.

Conclusions:

• The developed direct radiofluorination method is a viable approach for labeling peptides for PET.
• This technique facilitates the generation of high-purity peptide-based radiopharmaceuticals.
• The findings support broader application of peptides as molecular tracers in PET imaging.