Inhibition of DNA polymerase alpha by aphidicolin derivatives

Nucleic Acids Res. 1988 Jun 10;16(11):5107-13. doi: 10.1093/nar/16.11.5107.

Abstract

17-Acetylaphidicolin was 10-fold weaker and two derivatives lacking hydroxyl groups at the 16 and 17 positions were 100-fold weaker than aphidicolin as inhibitors of DNA polymerase alpha from HeLa and Chinese hamster ovary cells. 17,18-Diacetyl, 3,17,18-triacetyl and 3-epi derivatives of aphidicolin were inactive. Active compounds were, like aphidicolin, competitive with dCTP and did not inhibit aphidicolin-resistant DNA polymerases.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Aphidicolin
  • Cricetinae
  • Cricetulus
  • DNA Polymerase II / antagonists & inhibitors*
  • Deoxycytosine Nucleotides / metabolism
  • Diterpenes / pharmacology*
  • Female
  • Fibroblasts / enzymology
  • HeLa Cells / enzymology
  • Ovary

Substances

  • Deoxycytosine Nucleotides
  • Diterpenes
  • 2'-deoxycytidine 5'-triphosphate
  • Aphidicolin
  • DNA Polymerase II