Development of a kit-like radiofluorinated biomolecule leading to a controlled self-assembly of F nanoparticles for a smart PET imaging application.

A kit-like F-fluorination method has been successfully applied to prepare an activatable probe 1 with good radiochemical yield and high specific activity. The probe has good in vitro stability and favorable cell membrane permeability. A controlled condensation reaction was initiated, and self-assembly into nanoparticles occurred when the probe was in a reducing environment. Positron emission tomography (PET) imaging of the biothiol level in living subjects was conveniently and precisely realized using this probe. The present study may provide a new platform for the development of "smart" PET tracers for tumor imaging.