Effect of DNA intercalators on poly(ADP-ribose) glycohydrolase activity.
Proflavine, ethacridine (2-ethoxy-6,9-acridine diamine), ellipticine, daunomycin and Tilorone R10,556 DA (2,7-bis(piperidinobutyryl)-9H-fluoren-9-one) inhibit poly(ADP-ribose) glycohydrolase activity. The Ki values for proflavine and Tilorone R10,556 DA are 36 microM and 7.3 microM, respectively. The inhibition by intercalators is relieved by DNA but not by DNA-histone complexes. On the contrary, DNA-histone complexes increase the inhibition of some intercalators. Ethidium bromide is not inhibitory by itself. However, in the presence of DNA-histone complexes it strongly inhibits the enzyme activity. m-AMSA (4'-(9-acridinylamino)methanesulphon-m-anisidide) and chloroquine have no effect on the enzyme activity, even in the presence of DNA-histone complexes.
D000609:Aminoacridines / Q000494:pharmacology; D000677:Amsacrine; D000818:Animals; D002738:Chloroquine / Q000494:pharmacology; D004247:DNA / Q000494:pharmacology; D003630:Daunorubicin / Q000494:pharmacology; D004611:Ellipticines / Q000494:pharmacology; D004975:Ethacridine / Q000494:pharmacology; D004996:Ethidium / Q000494:pharmacology; D006026:Glycoside Hydrolases / Q000037:antagonists & inhibitors*; D006657:Histones / Q000494:pharmacology; D007364:Intercalating Agents / Q000494:pharmacology*; D007700:Kinetics; D011370:Proflavine / Q000494:pharmacology; D013552:Swine; D013950:Thymus Gland / Q000201:enzymology; D013994:Tilorone / Q000494:pharmacology
D000609:Aminoacridines; D004611:Ellipticines; D006657:Histones; D007364:Intercalating Agents; D000677:Amsacrine; C034192:ellipticine; D002738:Chloroquine; D004247:DNA; D011370:Proflavine; D006026:Glycoside Hydrolases; C022407:poly ADP-ribose glycohydrolase; D004996:Ethidium; D013994:Tilorone; D004975:Ethacridine; D003630:Daunorubicin