Abstract
An iodine-123 labeled bicyclic nucleoside analogue ([(123)I]-4) has been synthesized and evaluated as a potential single photon emission tomography (SPECT) reporter probe for the non-invasive imaging of expression of the varicella zoster virus thymidine kinase (VZV-tk) reporter gene. In vitro enzymatic assays revealed that the non-radioactive mono-iodo derivative 4 has good affinity for VZV-TK (IC(50): 4.2 microM). Biodistribution of [(123)I]-4 was examined in normal mice. Evaluation of [(123)I]-4 in HEK-293T cells showed 1.74-fold higher accumulation in VZV-TK-expressing cells compared to control cells.
Publication types
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Evaluation Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Antiviral Agents / chemical synthesis
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Antiviral Agents / pharmacology*
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Bridged Bicyclo Compounds / chemical synthesis
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Bridged Bicyclo Compounds / pharmacology*
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Cell Line / drug effects
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Genes, Reporter
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Herpesvirus 3, Human / drug effects*
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Herpesvirus 3, Human / genetics
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Humans
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Iodine Radioisotopes*
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Kidney / cytology
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Kidney / embryology
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Kidney / pathology
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Models, Chemical
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Nucleotides, Cyclic / chemical synthesis
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Nucleotides, Cyclic / pharmacology*
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Positron-Emission Tomography*
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Radiopharmaceuticals / chemical synthesis
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Radiopharmaceuticals / pharmacology*
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Thymidine Kinase / genetics
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Thymidine Kinase / metabolism
Substances
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Antiviral Agents
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Bridged Bicyclo Compounds
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Iodine Radioisotopes
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Nucleotides, Cyclic
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Radiopharmaceuticals
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Thymidine Kinase