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[靶向抗癌药物的DNA拓扑异构酶及耐药性获得机制]

[DNA topoisomerases targeting anticancer agents and mechanism for acquirement of drug resistance].

作者信息

Furukawa M, Harada T, Tanaka T, Kuwano M

机构信息

Department of Ist Biochemistry, Kyushu University School of Medicine.

出版信息

Nihon Rinsho. 1997 May;55(5):1096-102.

PMID:9155159
Abstract

DNA topoisomerase(topo) I and II regulate the topological conformation and DNA molecules by catalyzing the concerted breakage of single or double strands. Topo I and II targeting anticancer agents such as camptothecins (CPT-II), epipodophyllotoxins (VP16 and VM26), and amsarcine are widely used in cancer chemotherapy. To enhance their therapeutic efficacies, one should understand how cellular sensitivities to these topo-targeting agents are regulated, and one should also understand what mechanisms or factors are involved in the appearance of tumor cells resistant to them. We will discuss if there is any marker useful for determining drug sensitivity to these topo-targeting agents in cancer cells.

摘要

DNA拓扑异构酶(topo)I和II通过催化单链或双链的协同断裂来调节拓扑结构和DNA分子。靶向拓扑异构酶I和II的抗癌药物,如喜树碱(CPT-II)、鬼臼毒素(VP16和VM26)和安吖啶,广泛应用于癌症化疗。为提高其治疗效果,人们应了解细胞对这些靶向拓扑异构酶药物的敏感性是如何调节的,还应了解肿瘤细胞对它们产生抗性的机制或因素。我们将讨论是否存在可用于确定癌细胞对这些靶向拓扑异构酶药物敏感性的标志物。

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