Abstract
The current study presents [(18)F]PARPi-FL as a bimodal fluorescent/positron emission tomography (PET) agent for PARP1 imaging. [(18)F]PARPi-FL was obtained by (19)F/(18)F isotopic exchange and PET experiments, biodistribution studies, surface fluorescence imaging, and autoradiography carried out in a U87 MG glioblastoma mouse model. [(18)F]PARPi-FL showed high tumor uptake in vivo and ex vivo in small xenografts (< 2mm) with both PET and optical imaging technologies. Uptake of [(18)F]PARPi-FL in blocked U87 MG tumors was reduced by 84% (0.12 ± 0.02%injected dose/gram (%ID/g)), showing high specificity of the binding. PET imaging showed accumulation in the tumor (1h p.i.), which was confirmed by ex vivo phosphor autoradiography. The fluorescent component of [(18)F]PARPi-FL enables cellular resolution optical imaging, while the radiolabeled component of [(18)F]PARPi-FL allows whole-body deep-tissue imaging of malignant growth.
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