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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Cancer Research Campaign Laboratories, Department of Pathology, University Medical School, Edinburgh, UK.

Gen Pharmacol. 1995 Dec;26(8):1773-84. doi: 10.1016/0306-3623(95)00108-5.

Drug resistance remains a major obstacle to cancer treatment. Resistance to chemotherapy can be intrinsic, characterised by the nonresponsiveness of the tumour to the initial treatment. Alternatively, cancers that initially respond to chemotherapy can relapse after various times because of acquired resistance. 2. Resistance to drugs used as single agents is generally accompanied by the development of resistance to other drugs that can be structurally and functionally different. 3. Among the drugs commonly used in cancer treatment there are compounds that have been shown to inhibit DNA topoisomerases (Topos). These critical enzymes regulate the topological conformation of the DNA and participate in essential cellular processes. 4. This paper reviews the Topos' cellular functions, their catalytic activities and the mechanisms of resistance to inhibitors of Topos, with particular attention to the atypical multidrug resistance phenotype.

耐药性仍然是癌症治疗的主要障碍。对化疗的耐药性可以是内在的，其特征是肿瘤对初始治疗无反应。或者，最初对化疗有反应的癌症由于获得性耐药，在不同时间后可能会复发。2. 对单一药物产生的耐药性通常伴随着对其他在结构和功能上可能不同的药物产生耐药性。3. 在癌症治疗中常用的药物中，有一些化合物已被证明能抑制DNA拓扑异构酶（Topos）。这些关键酶调节DNA的拓扑构象并参与基本的细胞过程。4. 本文综述了Topos的细胞功能、催化活性以及对Topos抑制剂的耐药机制，特别关注非典型多药耐药表型。

Cancer Research Campaign Laboratories, Department of Pathology, University Medical School, Edinburgh, UK.

Gen Pharmacol. 1995 Dec;26(8):1773-84. doi: 10.1016/0306-3623(95)00108-5.

Drug resistance remains a major obstacle to cancer treatment. Resistance to chemotherapy can be intrinsic, characterised by the nonresponsiveness of the tumour to the initial treatment. Alternatively, cancers that initially respond to chemotherapy can relapse after various times because of acquired resistance. 2. Resistance to drugs used as single agents is generally accompanied by the development of resistance to other drugs that can be structurally and functionally different. 3. Among the drugs commonly used in cancer treatment there are compounds that have been shown to inhibit DNA topoisomerases (Topos). These critical enzymes regulate the topological conformation of the DNA and participate in essential cellular processes. 4. This paper reviews the Topos' cellular functions, their catalytic activities and the mechanisms of resistance to inhibitors of Topos, with particular attention to the atypical multidrug resistance phenotype.

耐药性仍然是癌症治疗的主要障碍。对化疗的耐药性可以是内在的，其特征是肿瘤对初始治疗无反应。或者，最初对化疗有反应的癌症由于获得性耐药，在不同时间后可能会复发。2. 对单一药物产生的耐药性通常伴随着对其他在结构和功能上可能不同的药物产生耐药性。3. 在癌症治疗中常用的药物中，有一些化合物已被证明能抑制DNA拓扑异构酶（Topos）。这些关键酶调节DNA的拓扑构象并参与基本的细胞过程。4. 本文综述了Topos的细胞功能、催化活性以及对Topos抑制剂的耐药机制，特别关注非典型多药耐药表型。