Intercalation with DNA is a prerequisite for daunomycin, adriamycin and its congeners in inhibiting DNAase I.

Abstract

DNAase I from bovine pancreas is inhibited by Daunomycin, Adriamycin, Adriamycin-14-acetate and Adriamycin-14-octanoate, whereas it is not inhibited by N-trifluoroacetyladriamycin-14-valerate or N-trifluoroacetyl-adriamycin. The present study suggests that these inhibitors act not directly on the enzyme, but on DNA, forming stable complexes and thus interfering with enzyme activity. The correlation between DNA binding and enzyme inhibition is demonstrated by the fact that the compounds forming complexes with DNA inhibit DNAase I activity, whereas those which do not form complexes with DNA cause no inhibition.

Cite this paper

@article{Facchinetti1978IntercalationWD, title={Intercalation with DNA is a prerequisite for daunomycin, adriamycin and its congeners in inhibiting DNAase I.}, author={Tullio Facchinetti and Alberto Mantovani and Lavinia Cantoni and Rita Maria Cantoni and Mario Salmona}, journal={Chemico-biological interactions}, year={1978}, volume={20 1}, pages={97-102} }