Cellular pharmacology of the D- and L-enantiomers of beta-5-o-carboranyl-2'-deoxyuridine
| Autor: | Alessandra Eleuteri, Janis Wright, Raymond F. Schinazi, Selwyn J. Hurwitz, Li Ma, Josef Moravek |
|---|---|
| Rok vydání: | 2000 |
| Předmět: |
Purine
Boron Compounds Cell Extracts Radiation-Sensitizing Agents Lymphoblast Stereoisomerism Biological Transport General Medicine Biochemistry Deoxyuridine chemistry.chemical_compound chemistry Papaverine Genetics Extracellular Tumor Cells Cultured Molecular Medicine Humans Enantiomer Nucleoside Incubation Chromatography High Pressure Liquid |
| Zdroj: | Nucleosides, nucleotidesnucleic acids. 19(3) |
| ISSN: | 1525-7770 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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