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拓扑异构酶(topoisomerase,topo)是参与DNA拓扑结构调整和转录、复制、修复的重要工具酶,由活性Tyr残基向DNA发动亲核攻击,导致DNA单股或双股断裂。Topo蛋白的含量、活性、功能改变是卵巢癌耐药发生的重要机制之一,作用于相关信号传导通路的上游。TopoⅡ蛋白表达增加的卵巢癌患者预后较差。TopoⅠ、Ⅱ抑制剂如TPT、VP-16等在复发卵巢癌的有效率大致为13％～25％,现已成为二线用药的首选。
Topoisomerase (topo) is an important tool involved in DNA topology regulation, transcription, replication and repair. The active Tyr residue initiates a nucleophilic attack on DNA, resulting in the breakage of single or double stranded DNA. Topo protein content, activity, function change is one of the important mechanisms of ovarian cancer drug resistance, the role of the relevant signal transduction pathway upstream. Patients with ovarian cancer with increased Topo II protein expression have a poorer prognosis. Topo Ⅰ, Ⅱ inhibitors such as TPT, VP-16 in the recurrence of ovarian cancer, the effective rate of about 13% to 25%, has now become the first choice for second-line drugs.