Hurwitz S J, Ma L, Eleuteri A, Wright J, Moravek J, Schinazi R F
Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Nucleosides Nucleotides Nucleic Acids. 2000 Mar;19(3):691-702. doi: 10.1080/15257770008035016.
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.
