Cytidine and deoxycytidylate deaminase inhibition by uridine analogs

Biochem Pharmacol. 1980 Mar 1;29(5):807-11. doi: 10.1016/0006-2952(80)90561-4.

Abstract

Cytidine deaminase, an enzyme found in the supernatant fluid of hepatocytes, granulocytes and tumor cells, and in plasma, degrades the antitumor agents cytosine arabinoside and 5-azacytidine. Uridine and its analogs, 3-deazauridine, 5-bromodeoxyuridine, 5-fluorodeoxyuridine and 6-azauridine, were found to competitively inhibit cytidine deaminase; the most potent inhibitor was 3-deazauridine (K(i) = 1.9 x 10(-5) M). In addition, deoxycytidylate deaminase, which degrades cytosine arabinoside monophosphate to the inactive uracil arabinoside monophosphate (K(m) = 9 x 10(-4) M), was competitively inhibited by 3-deazauridine monophosphate, as well as by the nucleotides of other uridine analogs. These results suggest that uridine analogs such as 3-deazauridine may have value in protecting cytosine arabinoside, 5-azacytidine and their monophosphate nucleotides from degration by neucleoside and nucleotide deaminases.

MeSH terms

  • 3-Deazauridine / metabolism
  • Azauridine / metabolism
  • Bromodeoxyuridine / metabolism
  • Cytidine Deaminase / analysis
  • Cytidine Deaminase / antagonists & inhibitors*
  • DCMP Deaminase / analysis
  • DCMP Deaminase / antagonists & inhibitors*
  • Floxuridine / metabolism
  • Humans
  • Kinetics
  • Uridine / analogs & derivatives*
  • Uridine / metabolism

Substances

  • Floxuridine
  • 3-Deazauridine
  • Azauridine
  • DCMP Deaminase
  • Cytidine Deaminase
  • Bromodeoxyuridine
  • Uridine