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CycloSal-dRFIB, a Thymidine Mimetic, Thymidine Kinase by-Pass Nucleoside Prodrug: Radioiodination, in vitro Cellular Uptake and Biodistribution in Murine Models

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Cyclo-(3-methylsaligenyl)-5-O-[1-(2,4-difluoro-5-[125I]iodophenyl)-2-deoxy-β-D-ribofuranosyl]phosphate (cycloSal- dRF[125I]IB) was radioiodinated with sodium [125I]iodide via copper-catalyzed isotope exchange in 48% radiochemical yield. cycloSal-dRF[125I]IB was found to be incorporated into the cytoplasmic nucleic acid and mitochondrial fractions of murine KBALB and K-STK (engineered to express HSV-1 thymidine kinase) cells in cell culture. Uptake was greater than that for either the corresponding nucleoside dRF[125I]IB or [125I]IUdR. These in vitro studies support a mechanism of metabolic activation to the free nucleotide, thereby effecting TK-bypass. Pharmacokinetic studies in rats reflect a complex interplay of tissue depot effects, hepatobiliary recycling, and metabolism. Biodistribution studies in tumor- bearing mice provide further evidence for lipophilic depot effects and hepatobiliary recirculation, with no evidence for active (metabolic) accumulation in any tissue.





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Keywords: (CO asphyxiation); BSA; Cell Culture; Coomassie blue G250 reagent; CycloSal-dRFIB; ELISA; EMT6 tumour cells; HSV-1 thymidine kinase; Iododeoxyuridine; Murine Models; Thymidine; Thymidine Kinase by-Pass; Tris-acetate-EDTA buffer; Xenopus oocytes; [I]IUdR; biodistribution; bovine plasma albumin; cycloSal-dRFIB; cycloSal-dRF[I]IB; cyclosaligenyl phosphodiester pronucleotides; dRF[I]IB; difluorophenyldeoxyribosides; fluorodeoxyuridine; gamma scintillation counter; mitochondrial uptake; monophosphate; nucleoside kinases; nucleotides; pharmacokinetics; phosphorylation; prodrugs; pyrimidine nucleosides; radioassay; thymidine kinase (TK) by-pass

Document Type: Research Article

Publication date: October 1, 2010

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  • Current Radiopharmaceuticals publishes original research articles, letters, reviews, drug clinical trial studies and guest edited issues on all aspects of research and development of radiolabelled compound preparations. The scope of the journal covers the following areas: radio imaging techniques, therapies; preparation and application of radionuclide compounds including the incorporation of tracer methods used in scientific research and applications.
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