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化疗是提高恶性肿瘤疗效的一个重要手段,然而肿瘤细胞对化疗药物产生的多药耐药性往往导致化疗的失败,多药耐药性(multidrug resistance,MDR)是指肿瘤细胞能对多种结构、功能及杀伤机制均不同的化疗药物产生耐受。目前认为多药耐药与下列因素有关:多药耐药基因(MDR1)及其编码的细胞膜P—糖蛋白(P—GP)表达增加;谷胱甘肽解毒酶系统(GST)活性增高;DNA拓朴异构酶Ⅱ(ToP_0Ⅱ)活性减低或结构异常;DNA损伤后修复能力增强;蛋白激酶C活性增强;多药耐药相关蛋白(MRP)基因的扩增或过度表达;肺阻蛋白(LRP)的表达。根据耐药产生的机制不同,逆转剂可分以下几种。
Chemotherapy is an important means to improve the curative effect of malignant tumors. However, multidrug resistance of tumor cells to chemotherapeutic drugs often leads to the failure of chemotherapy. Multidrug resistance (MDR) refers to the effect of tumor cells on a variety of structures , Function and killing mechanism are different chemotherapy drugs tolerance. At present, multidrug resistance is thought to be associated with increased expression of multidrug resistance gene (MDR1) and its encoded P-glycoprotein (P-GP), increased activity of glutathione detoxification system (GST), DNA ToP_0Ⅱ activity is reduced or structurally abnormal; DNA repair ability is enhanced after injury; protein kinase C activity is enhanced; multidrug resistance-related protein (MRP) gene is amplified or overexpressed; and lung resistance protein (LRP) expression. Depending on the mechanism of drug resistance, reversal agents can be divided into the following categories.