We report a straight-forward route to the generation of 18F-labeled biomolecules such as peptides, proteins, antibodies and antibody-derived fragments for PET imaging. We combine a sortase-mediated installation of an aminooxy-functionalized short peptide, labeled with 18F-2-deoxyfluoroglucose (FDG) in a phenylenediamine-catalyzed oxime ligation. The method is rapid, site-specific, shows excellent yields and requires only minimal and facile modification of the protein of interest.  The ready availability of 18F-2-deoxyfluoroglucose in radiopharmaceutical facilities equipped for PET imaging avoids the far more complicated chemistries employed to date. We demonstrate utility of the method by performing PET scans of human Class II MHC-positive tumors in a mouse xenograft model.

Site-specific 18F-labeling of proteins for immuno-PET imaging using sortase

248th National Meeting (2014)

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