Tavassoli M, Tavassoli M H, Shall S
Biochim Biophys Acta. 1985 Mar 1;827(3):228-34. doi: 10.1016/0167-4838(85)90207-9.
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.
硫酸原黄素、依沙吖啶(2-乙氧基-6,9-吖啶二胺)、玫瑰树碱、柔红霉素和替洛隆R10556 DA(2,7-双(哌啶丁酰基)-9H-芴-9-酮)可抑制聚(ADP-核糖)糖水解酶活性。硫酸原黄素和替洛隆R10556 DA的Ki值分别为36微摩尔和7.3微摩尔。嵌入剂的抑制作用可被DNA解除,但不能被DNA-组蛋白复合物解除。相反,DNA-组蛋白复合物会增强某些嵌入剂的抑制作用。溴化乙锭本身无抑制作用。然而,在存在DNA-组蛋白复合物的情况下,它会强烈抑制酶活性。m-AMSA(4'-(9-吖啶基氨基)甲磺酰基间茴香胺)和氯喹即使在存在DNA-组蛋白复合物的情况下对酶活性也无影响。