Inhibition of reverse transcriptase activity of avian myeloblastosis virus by pyrophosphate analogues

Antiviral Res. 1982 May;2(1-2):81-95. doi: 10.1016/0166-3542(82)90028-6.

Abstract

Several pyrophosphate analogues have been studied for their effects on avian myeloblastosis virus reverse transcriptase and on cellular DNA polymerase alpha. Examination of structure-activity relationships for these compounds revealed that two acidic groups connected by a short bridge were necessary, but not sufficient, for inhibition of the enzyme activities. Foscarnet sodium (trisodium phosphonoformate) was the most potent inhibitor of reverse transcriptase, giving non-competitive inhibition of reactions primed by (rA)n . (dT)12-18, (rC)n . (dG)12-18, (dC)n . (dG)12-18, and activated DNA. Carbonyldiphosphonate and 2-hydroxyphosphonoacetate also caused non-competitive inhibition patterns, whereas hypophosphate and imidodiphosphonate inhibited AMV reverse transcriptase in a competitive, non-linear manner. The reverse transcriptase reactions directed by (rA)n . (dT)12-18 and activated DNA were most affected by the non-competitive inhibitors. Hypophosphate and imidodiphosphonate inhibited preferentially reactions primed by (dC)n . (dG)12-18 and activated DNA. In all cases the (rC)n . (dG)12-18 directed reaction was the least affected.

MeSH terms

  • Avian Leukosis Virus / enzymology*
  • Avian Myeloblastosis Virus / enzymology*
  • DNA Polymerase II / antagonists & inhibitors
  • Diphosphates / pharmacology*
  • Diphosphonates / pharmacology
  • Foscarnet
  • Kinetics
  • Phosphonoacetic Acid / analogs & derivatives
  • Phosphonoacetic Acid / pharmacology
  • Polydeoxyribonucleotides / pharmacology*
  • Reverse Transcriptase Inhibitors*
  • Structure-Activity Relationship

Substances

  • Diphosphates
  • Diphosphonates
  • Polydeoxyribonucleotides
  • Reverse Transcriptase Inhibitors
  • Foscarnet
  • DNA Polymerase II
  • Phosphonoacetic Acid