Source:http://linkedlifedata.com/resource/pubmed/id/18047266
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
26
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| pubmed:dateCreated |
2007-12-20
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| pubmed:abstractText |
We recently reported a new positron emission tomography (PET) reporter gene, namely, varicella-zoster virus thymidine kinase (VZV-tk) in combination, with carbon-11 or fluorine-18 labeled m-alkoxyphenyl bicyclic nucleoside analogues (BCNAs) as PET reporter probes. We now report the synthesis and evaluation of p-alkoxyphenyl-BCNA tracers ([11C]-4 and [18F]-5), which are found to be superior to the m-alkoxyphenyl-BCNA tracers. In particular, the fluorine-18 labeled tracer ([18F]-5, IC50 of 5 is 4.2 microM) shows a higher accumulation in VZV-tk expressing cells than the previously reported m-methoxyphenyl BCNA. [11C]-4 and [18F]-5 were synthesized by heating the phenol precursor 3 with 11CH 3I and 18FCH 2CH 2Br, respectively, as alkylating agents. In vitro evaluation of [11C]-4 and [18F]-5 in 293T cells showed about 14- and 54-fold higher uptake, respectively, into VZV-tk gene-transduced cells compared to control cells. LC-MS analysis confirmed the formation of monophosphate derivative of 5 upon catalysis by VZV TK. In vivo studies of this new reporter gene/probe system are in progress.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds, Heterocyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Carbon Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidine Nucleosides,
http://linkedlifedata.com/resource/pubmed/chemical/Radiopharmaceuticals,
http://linkedlifedata.com/resource/pubmed/chemical/Thymidine Kinase
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| pubmed:status |
MEDLINE
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| pubmed:month |
Dec
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| pubmed:issn |
0022-2623
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:day |
27
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| pubmed:volume |
50
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
6627-37
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| pubmed:meshHeading |
pubmed-meshheading:18047266-Animals,
pubmed-meshheading:18047266-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:18047266-Carbon Radioisotopes,
pubmed-meshheading:18047266-Cell Line,
pubmed-meshheading:18047266-Chromatography, High Pressure Liquid,
pubmed-meshheading:18047266-Fluorine Radioisotopes,
pubmed-meshheading:18047266-Genes, Reporter,
pubmed-meshheading:18047266-Herpesvirus 3, Human,
pubmed-meshheading:18047266-Humans,
pubmed-meshheading:18047266-Male,
pubmed-meshheading:18047266-Mice,
pubmed-meshheading:18047266-Phosphorylation,
pubmed-meshheading:18047266-Positron-Emission Tomography,
pubmed-meshheading:18047266-Pyrimidine Nucleosides,
pubmed-meshheading:18047266-Radiopharmaceuticals,
pubmed-meshheading:18047266-Structure-Activity Relationship,
pubmed-meshheading:18047266-Thymidine Kinase,
pubmed-meshheading:18047266-Tissue Distribution
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| pubmed:year |
2007
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| pubmed:articleTitle |
A p-[18F]fluoroethoxyphenyl bicyclic nucleoside analogue as a potential positron emission tomography imaging agent for varicella-zoster virus thymidine kinase gene expression.
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| pubmed:affiliation |
Molecular Small Animal Imaging Center, Laboratory for Radiopharmacy-Faculty of Pharmaceutical Sciences, Department of Nuclear Medicine, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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