Warner H R, Persson M L, Bensen R J, Mosbaugh D W, Linn S
Nucleic Acids Res. 1981 Nov 25;9(22):6083-92. doi: 10.1093/nar/9.22.6083.
1-Methyl-9H-pyrido-[3,4-b]indole (harmane) inhibits the apurinic/apyrimidinic (AP) endonuclease activity of the UV endonuclease induced by phage T4, whereas it stimulates the pyrimidine dimer-DNA glycosylase activity of that enzyme. E. coli endonuclease IV, E. coli endonuclease VI (the AP endonuclease activity associated with E. coli exonuclease III), and E. coli uracil-DNA glycosylase were not inhibited by harmane. Human fibroblast AP endonucleases I and II also were only slightly inhibited. Therefore, harmane is neither a general inhibitor of AP endonucleases, nor a general inhibitor of Class I AP endonucleases which incise DNA on the 3'-side of AP sites. However, E. coli endonuclease III and its associated dihydroxythymine-DNA glycosylase activity were both inhibited by harmane. This observation suggests that harmane may inhibit only AP endonucleases which have associated glycosylase activities.
1-甲基-9H-吡啶并[3,4-b]吲哚(哈尔满)抑制噬菌体T4诱导的紫外线内切酶的脱嘌呤/脱嘧啶(AP)内切酶活性,而它刺激该酶的嘧啶二聚体-DNA糖基化酶活性。大肠杆菌内切酶IV、大肠杆菌内切酶VI(与大肠杆菌核酸外切酶III相关的AP内切酶活性)和大肠杆菌尿嘧啶-DNA糖基化酶不受哈尔满抑制。人成纤维细胞AP内切酶I和II也仅受到轻微抑制。因此,哈尔满既不是AP内切酶的通用抑制剂,也不是在AP位点3'侧切割DNA的I类AP内切酶的通用抑制剂。然而,大肠杆菌内切酶III及其相关的二羟基胸腺嘧啶-DNA糖基化酶活性均受到哈尔满抑制。这一观察结果表明,哈尔满可能仅抑制具有相关糖基化酶活性的AP内切酶。