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Non-invasive PET Imaging of PARP1 Expression in Glioblastoma Models.


ABSTRACT: PURPOSE:The current study presents [(18)F]PARPi as imaging agent for PARP1 expression. PROCEDURES:[(18)F]PARPi was generated by conjugating a 2H-phthalazin-1-one scaffold to 4-[(18)F]fluorobenzoic acid. Biochemical assays, optical in vivo competition, biodistribution analysis, positron emission tomography (PET)/X-ray computed tomography, and PET/magnetic resonance imaging studies were performed in subcutaneous and orthotopic mouse models of glioblastoma. RESULTS:[(18)F]PARPi shows suitable pharmacokinetic properties for brain tumor imaging (IC50?=?2.8?±?1.1 nM; logPCHI?=?2.15?±?0.41; plasma-free fraction?=?63.9?±?12.6 %) and accumulates selectively in orthotopic brain tumor tissue. Tracer accumulation in subcutaneous brain tumors was 1.82?±?0.21 %ID/g, whereas in healthy brain, the uptake was only 0.04?±?0.01 %ID/g. CONCLUSIONS:[(18)F]PARPi is a selective PARP1 imaging agent that can be used to visualize glioblastoma in xenograft and orthotopic mouse models with high precision and good signal/noise ratios. It offers new opportunities to non-invasively image tumor growth and monitor interventions.

SUBMITTER: Carney B 

PROVIDER: S-EPMC4841747 | biostudies-literature | 2016 Jun

REPOSITORIES: biostudies-literature

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<h4>Purpose</h4>The current study presents [(18)F]PARPi as imaging agent for PARP1 expression.<h4>Procedures</h4>[(18)F]PARPi was generated by conjugating a 2H-phthalazin-1-one scaffold to 4-[(18)F]fluorobenzoic acid. Biochemical assays, optical in vivo competition, biodistribution analysis, positron emission tomography (PET)/X-ray computed tomography, and PET/magnetic resonance imaging studies were performed in subcutaneous and orthotopic mouse models of glioblastoma.<h4>Results</h4>[(18)F]PARP  ...[more]

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