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非嵌合性抗癌药物队小牛胸腺DNA拓扑异构酶I活力的影响
引用本文:张卫升,林卓坤,黄熙泰. 非嵌合性抗癌药物队小牛胸腺DNA拓扑异构酶I活力的影响[J]. 药学学报, 1990, 25(9): 641-645
作者姓名:张卫升  林卓坤  黄熙泰
作者单位:南开大学生物系,天津300071
摘    要:
本文介绍从小牛胸腺中分离纯化DNA拓扑异构酶Ⅰ(简称拓扑酶Ⅰ)的方法,并用于检测了几种非嵌合性抗癌药物对该酶活力的影响。实验结果表明,一些已知的抗癌药物确有抑制DNA拓扑酶Ⅰ的作用。以抑制DNA拓扑酶Ⅰ为检测指标的方法可为筛选抗癌药物提供新的手段,并为药物抗癌机制的研究开辟了新的途径。

关 键 词:拓扑异构酶Ⅰ  抗癌药物  药物筛选
收稿时间:1989-07-31

Effect of some nonintercalative antitumor drugs on the activity of calf thymus DNA topoisomerase I
WS Zhang,ZK Lin and XT Huang. Effect of some nonintercalative antitumor drugs on the activity of calf thymus DNA topoisomerase I[J]. Acta pharmaceutica Sinica, 1990, 25(9): 641-645
Authors:WS Zhang  ZK Lin  XT Huang
Affiliation:Department of Biology, Nankai University, Tianjin.
Abstract:
DNA topoisomerase I has been isolated from the nuclei of calf thymus by PEG fractionation and chromatography on P11 and on Bio-Rex 70. Either a positive or negative supercoiled pBR322 DNA can be relaxed by the enzyme. The activity of Topo I is Mg2+ and ATP independent. Some of nonintercalative antitumor drugs such as camptothecine, hydroxycamptothecine, cyclophosphamide, methotrexate and mitomycin C were found to inhibit the activity of Topo I. The results suggest that DNA Topo I can be used to screen new nonintercalative antitumor drugs as a target protein.
Keywords:Antitumor drugs  Drugs screening  Topoisomerase Ⅰ
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