5-AZA-2′-Deoxycytidine Synergistic action with Thymidine on Leukemic Cells and Interaction of 5-AZA-dCMP with dCMP Deaminase

  • R. L. Momparler
  • M. Rossi
  • J. Bouchard
  • S. Bartolucci
  • L. F. Momparler
  • C. A. Raia
  • R. Nucci
  • C. Vaccaro
  • S. Sepe
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 131)

Abstract

5-Aza-2′-deoxycytidine (5-AZA-CdR) is a potent antileukemic agent whose inhibitory effects are blocked by deoxycytidine (1-3). In order to be active, 5-AZA-CdR must first be phosphorylated by the enzyme deoxycytidine kinase (4). Leukemic cells deficient in the enzyme are resistant to 5-AZA-CdR (5). The lethal action of 5-AZA-CdR is related to its incorporation into DNA (6,7). The incorporation of 5-azacytosine analogs into DNA has been shown to induce the expression of differentiated phenotypes (8). This induction of differentiation by 5-AZA-CdR appears to be related to the inhibition of DNA methylation produced by these analogs (8, 9).

Keywords

HPLC Leukemia Pyrimidine Thymidine Dine 

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Copyright information

© Plenum Press, New York 1986

Authors and Affiliations

  • R. L. Momparler
    • 1
    • 2
  • M. Rossi
    • 1
    • 2
  • J. Bouchard
    • 1
    • 2
  • S. Bartolucci
    • 1
    • 2
  • L. F. Momparler
    • 1
    • 2
  • C. A. Raia
    • 1
    • 2
  • R. Nucci
    • 1
    • 2
  • C. Vaccaro
    • 1
    • 2
  • S. Sepe
    • 1
    • 2
  1. 1.Dept. pharmacologieUniv. de MontréalMontrealCanada
  2. 2.Dept. Chim. Org. Biol.Univ. of Naples, IIGB, CNRNaplesItaly

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