Marcus S L, Petrylak D P, Burchenal J J, Bacchi C J
Cancer Res. 1985 Jan;45(1):112-5.
Activated DNA-directed DNA synthesis catalyzed by Rauscher leukemia virus (RLV) and other type C mammalian retroviral DNA polymerases is uniquely stimulated by biologically active polyamines. Cationic trypanocides may act as antagonists of polyamine function. As described here, several cationic trypanocides stimulate RLV polymerase-catalyzed DNA-directed DNA synthesis at concentrations significantly inhibiting eukaryotic DNA polymerases. Such stimulation is negated by polyamines. Kinetic analysis of the stimulation of RLV DNA polymerase by three structurally dissimilar cationic trypanocides (Antrycide, Burroughs-Wellcome Compound 64A, and Bayer Compound 1694) suggests that such stimulation is, in part, due to a drug:DNA structural interaction resembling the polyamine:DNA structural complex recognized by the RLV DNA polymerase.
劳氏肉瘤病毒(RLV)和其他C型哺乳动物逆转录病毒DNA聚合酶催化的活化DNA定向DNA合成受到生物活性多胺的独特刺激。阳离子锥虫杀灭剂可能作为多胺功能的拮抗剂。如本文所述,几种阳离子锥虫杀灭剂在显著抑制真核DNA聚合酶的浓度下刺激RLV聚合酶催化的DNA定向DNA合成。这种刺激被多胺抵消。对三种结构不同的阳离子锥虫杀灭剂(安锥赛、伯勒斯-韦尔科姆化合物64A和拜耳化合物1694)刺激RLV DNA聚合酶的动力学分析表明,这种刺激部分是由于药物与DNA的结构相互作用,类似于RLV DNA聚合酶识别的多胺与DNA的结构复合物。