Abstract
[(18)F]-FBAU and [(18)F]-FCAU have been synthesized and evaluated in vivo as markers for HSV1-tk gene expression. At 2 hours, uptake of [(18)F]-FBAU and [(18)F]-FCAU in HSV1-tk-positive tumors was 7.9-fold and 6.0-fold higher than the control tumors, respectively. Micro-PET images also showed very high uptake in HSV-tk tumors. Compared to [(14)C]-FMAU, total uptake of [(18)F]-FBAU and [(18)F]-FCAU was similar in tk-positive cells, but the uptake ratio (tk+/wild) was higher. [(18)F]-FBAU and [(18)F]-FCAU appear to be potential PET imaging agents for gene expression.
Publication types
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Comparative Study
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Evaluation Study
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Research Support, U.S. Gov't, P.H.S.
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Validation Study
MeSH terms
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Animals
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Arabinofuranosyluracil / analogs & derivatives
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Arabinofuranosyluracil / chemistry
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Arabinofuranosyluracil / pharmacokinetics*
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Biomarkers, Tumor / metabolism*
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Bromouracil / analogs & derivatives
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Bromouracil / pharmacokinetics*
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Colonic Neoplasms / diagnostic imaging*
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Colonic Neoplasms / genetics
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Colonic Neoplasms / metabolism*
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Fluorouracil / analogs & derivatives
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Fluorouracil / chemistry
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Fluorouracil / pharmacokinetics*
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Gene Expression Profiling / methods
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Gene Expression Regulation, Neoplastic
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Genetic Markers / genetics
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Humans
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Isotope Labeling / methods
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Metabolic Clearance Rate
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Mice
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Mice, Nude
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Organ Specificity
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Radioisotope Dilution Technique
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Radiopharmaceuticals / chemical synthesis
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Radiopharmaceuticals / pharmacokinetics
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Reproducibility of Results
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Sensitivity and Specificity
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Thymidine Kinase / metabolism*
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Tissue Distribution
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Tomography, Emission-Computed / methods
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Viral Proteins / metabolism*
Substances
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1-(2-fluoro-2-deoxyarabinofuranosyl)-5-bromouracil
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2'-deoxy-2'-fluoro-5-chloro-1-arabinofuranosyluracil
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Biomarkers, Tumor
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Genetic Markers
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Radiopharmaceuticals
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Viral Proteins
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Arabinofuranosyluracil
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Bromouracil
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thymidine kinase, Canid herpesvirus 1
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Thymidine Kinase
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Fluorouracil