Biochemical Pharmacology volume 81, issue 1, P82-90 2011 DOI: 10.1016/j.bcp.2010.09.009 View full text
Vijaya L. Damaraju, Kyla M. Smith, Delores Mowles, Ireneusz Nowak, Edward Karpinski, James D. Young, Morris J. Robins, Carol E. Cass

Abstract: Human concentrative nucleoside transporters (hCNTs) mediate electrogenic secondary active transport of physiological nucleosides and nucleoside drugs into cells. Six fused-pyrimidine ribonucleosides and one 2'-deoxynucleoside were assessed for their abilities to inhibit [(3)H]uridine transport in the yeast Saccharomyces cerevisiae producing recombinant hCNT1, hCNT2 or hCNT3. Six of the analogs inhibited hCNT1 with K(i) values<1μM whereas only two analogs inhibited hCNT3 with K(i) values<1μM and none inhibited …

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