Giuseppe Carlucci1, Brandon Carney1,2,3, Christian Brand1, Susanne Kossatz1, Christopher P Irwin1, Sean D Carlin1, Edmund J Keliher4, Wolfgang Weber1,5, Thomas Reiner6,7. 1. Department of Radiology, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, NY, 10065, USA. 2. Department of Chemistry and Biochemistry, Hunter College of the City University of New York, New York, NY, 10065, USA. 3. Ph.D. Program in Chemistry, The Graduate Center of the City University of New York, New York, 10018, USA. 4. Center for Systems Biology, Massachusetts General Hospital, Boston, MA, 02114, USA. 5. Weill Cornell Medical College, New York, NY, 10065, USA. 6. Department of Radiology, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, NY, 10065, USA. reinert@mskcc.org. 7. Weill Cornell Medical College, New York, NY, 10065, USA. reinert@mskcc.org.
Abstract
PURPOSE: The current study presents [(18)F]PARPi-FL as a bimodal fluorescent/positron emission tomography (PET) agent for PARP1 imaging. PROCEDURES: [(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. RESULTS: [(18)F]PARPi-FL showed high tumor uptake in vivo and ex vivo in small xenografts (< 2 mm) 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 (1 h p.i.), which was confirmed by ex vivo phosphor autoradiography. CONCLUSIONS: 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.
PURPOSE: The current study presents [(18)F]PARPi-FL as a bimodal fluorescent/positron emission tomography (PET) agent for PARP1 imaging. PROCEDURES: [(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 glioblastomamouse model. RESULTS: [(18)F]PARPi-FL showed high tumor uptake in vivo and ex vivo in small xenografts (< 2 mm) 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 (1 h p.i.), which was confirmed by ex vivo phosphor autoradiography. CONCLUSIONS: 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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