Differential transport of cytosine-containing nucleosides by recombinant human concentrative nucleoside transporter protein hCNT1

Nucleosides Nucleotides Nucleic Acids. Jan-Feb 2000;19(1-2):415-34. doi: 10.1080/15257770008033018.

Abstract

The transportability of cytosine-containing nucleosides by recombinant hCNT1 was investigated in transfected mammalian cells. Apparent K(m) values for hCNT1-mediated transport of uridine, cytidine and deoxycytidine were, respectively, 59, 140 and 150 microM. Uridine transport was inhibited 89, 32 and 11%, respectively, by 500 microM gemcitabine, cytarabine and lamivudine, demonstrating that, unlike gemcitabine (a high-affinity hCNT1 permeant), cytarabine and lamivudine are poor hCNT1 permeants.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimetabolites, Antineoplastic / pharmacology
  • Antiviral Agents / pharmacology
  • Biological Transport
  • COS Cells
  • Carrier Proteins / metabolism*
  • Cell Division / drug effects
  • Cell Line
  • Cytarabine / pharmacology
  • Cytidine / metabolism*
  • Deoxycytidine / analogs & derivatives
  • Deoxycytidine / metabolism*
  • Deoxycytidine / pharmacology
  • Haplorhini
  • HeLa Cells
  • Humans
  • Immunoblotting
  • Lamivudine / pharmacology
  • Membrane Transport Proteins*
  • Recombinant Proteins / metabolism
  • Substrate Specificity
  • Transfection
  • Uridine / metabolism*

Substances

  • Antimetabolites, Antineoplastic
  • Antiviral Agents
  • Carrier Proteins
  • Membrane Transport Proteins
  • Recombinant Proteins
  • cif nucleoside transporter
  • Cytarabine
  • Deoxycytidine
  • Lamivudine
  • Cytidine
  • gemcitabine
  • Uridine