Abstract
The cellular pharmacology of the D- and L-enantiomers of beta-5-o-carboranyl-2'-deoxyuridine (CDU), compounds designed for boron neutron capture therapy (BNCT), were studied using human CEM lymphoblast and U-251 glioblastoma cells, at a physiologically achievable concentration (1 microM). Accumulation of the enantiomers was rapid and indistinguishable, reaching cellular concentrations > 40-fold higher than extracellular levels, with approximately 5% persisting in cells after incubation in fresh medium for more than 2 hr. Uptake was not affected by nucleoside uptake inhibitors, but was inhibited by the purine base uptake inhibitor papaverine.
Publication types
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Biological Transport
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Boron Compounds / chemistry
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Boron Compounds / metabolism
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Boron Compounds / pharmacology*
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Cell Extracts
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Chromatography, High Pressure Liquid
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Deoxyuridine / analogs & derivatives*
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Deoxyuridine / chemistry
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Deoxyuridine / metabolism
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Deoxyuridine / pharmacology
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Humans
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Papaverine / pharmacology
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Radiation-Sensitizing Agents / chemistry
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Radiation-Sensitizing Agents / metabolism
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Radiation-Sensitizing Agents / pharmacology*
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Stereoisomerism
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Tumor Cells, Cultured
Substances
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Boron Compounds
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Cell Extracts
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Radiation-Sensitizing Agents
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5-carboranyl-2'-deoxyuridine
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Papaverine
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Deoxyuridine