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 heal

SUBMITTER: Carney B 

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

REPOSITORIES: biostudies-literature