Dideoxycytidine permeation and salvage by mouse leukemia cells and human erythrocytes.
Transmembrane equilibration of dideoxycytidine (ddCyd) in P388 mouse leukemia cells and human erythrocytes was only 1% as rapid as that of uridine and 2'-deoxycytidine which is mediated by the facilitated nucleoside transporter of these cells. ddCyd entry was nonsaturable up to a concentration of 1 mM but was partially inhibited by dipyridamole, nitrobenzylthioinosine and nucleosides, but not by nucleobases. Thus, entry was partly (70-80%) mediated, though very inefficiently, by the nucleoside carrier. Intracellular phosphorylation of ddCyd in P388 cells was also very inefficient compared to that of 2'-deoxycytidine and uridine and not rate limited by its slow entry into the cells.
Plagemann
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PG
Department of Microbiology, University of Minnesota, Medical School, Minneapolis 55455.
Woffendin
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D000818:Animals; D001798:Blood Proteins / Q000502:physiology; D002352:Carrier Proteins / Q000502:physiology; D004176:Dipyridamole / Q000494:pharmacology; D004912:Erythrocytes / Q000378:metabolism*; D006801:Humans; D006918:Hydroxyurea / Q000494:pharmacology; D007942:Leukemia, Experimental / Q000378:metabolism*; D008565:Membrane Proteins / Q000502:physiology; D051379:Mice; D033703:Nucleoside Transport Proteins; D010539:Permeability; D012995:Solubility; D013329:Structure-Activity Relationship; D013868:Thioinosine / Q000494:pharmacology / Q000031:analogs & derivatives; D014529:Uridine / Q000493:pharmacokinetics; D016047:Zalcitabine / Q000493:pharmacokinetics*
D001798:Blood Proteins; D002352:Carrier Proteins; D008565:Membrane Proteins; D033703:Nucleoside Transport Proteins; D013868:Thioinosine; D004176:Dipyridamole; D016047:Zalcitabine; C001789:4-nitrobenzylthioinosine; D014529:Uridine; D006918:Hydroxyurea