Affinity of the antiviral enantiomers of oxathiolane cytosine nucleosides for human 2'-deoxycytidine kinase

Biochem Pharmacol. 1993 Apr 6;45(7):1540-3. doi: 10.1016/0006-2952(93)90058-5.

Abstract

The two enantiomers of 2',3'-dideoxy-3'-thiacytidine (BCH-189) and their 5-fluoro analogs (FTC) were found to be good substrates for human 2'-deoxycytidine kinase with Km values in the 5.7 to 42.1 microM range. The affinity of the (-)-enantiomers was greater than that of the (+)-compounds. These results may explain the greater in vitro antiviral potency against human immunodeficiency virus and hepatitis B virus of the (-)-enantiomers when compared to their (+)-counterparts. The (+)- and (-)-enantiomers of FTC and BCH-189 are the first nucleoside analogs for which we have observed lower apparent kinetic constants for this enzyme in the presence of ATP compared to UTP.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Antiviral Agents / pharmacology*
  • Cytidine Deaminase / antagonists & inhibitors
  • Deoxycytidine Kinase / metabolism
  • Humans
  • Kinetics
  • Lamivudine
  • Stereoisomerism
  • Uridine Triphosphate / metabolism
  • Zalcitabine / analogs & derivatives*
  • Zalcitabine / pharmacology

Substances

  • Antiviral Agents
  • Lamivudine
  • Zalcitabine
  • Adenosine Triphosphate
  • Deoxycytidine Kinase
  • Cytidine Deaminase
  • Uridine Triphosphate