Inhibitory effect of 1-beta-D-arabinofuranosylthymine 5'-triphosphate and 1-beta-D-arabinofuranosylcytosine 5'-triphosphate on DNA polymerases from murine cells and oncornavirus

Cancer Res. 1978 Sep;38(9):3076-9.

Abstract

This report compares the effect of the newly synthesized 1-beta-D-arabinofuranosylthymine 5'-triphosphate with 1-beta-D-arabinofuranosylcytosine 5'-triphosphate on the activity of DNA polymerases from mouse cells and oncornavirus. 1-beta-D-Arabinofuranosylthymine 5'-triphosphate inhibited all the activities of DNA polymerase alpha, beta, and gamma and viral DNA polymerase. The mode of inhibition of 1-beta-D-arabinofuranosylthymine 5'-triphosphate as well as 1-beta-D-arabinofuranosylcytosine 5'-triphosphate was competitive to the deoxynucleoside triphosphate with the same base. The inhibition constant (Ki) and the mode of inhibition of nucleotide incorporation varied with changes in the combination of the inhibitor, substrate(s), and enzyme species.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Binding, Competitive
  • Cytarabine / analogs & derivatives*
  • Cytarabine / pharmacology
  • Kinetics
  • Mice
  • Nucleic Acid Synthesis Inhibitors*
  • Rauscher Virus / enzymology
  • Reverse Transcriptase Inhibitors*
  • Substrate Specificity
  • Thymine Nucleotides / pharmacology*

Substances

  • Nucleic Acid Synthesis Inhibitors
  • Reverse Transcriptase Inhibitors
  • Thymine Nucleotides
  • Cytarabine