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部分恶性肿瘤患者经抗肿瘤药物治疗后产生耐药,或先天性对化疗药物不敏感,使治疗疗效不佳而导致复发或转移,造成这种现象的原因目前认为与肿瘤细胞产生多药耐药性(Multidrug-resistance,MDR)有关。MDR是指肿瘤细胞对分子结构不同、作用机制各异的抗肿瘤药物产生交叉耐药。人类肿瘤多药耐药基因家族由mdr_1和mdr_3组成。MDR表型的标志是分子量为170kD的细胞膜蛋白,称之为P-糖蛋白(permeability-glycoprotein,Pgp)。mdr_1和mdr_3有较高的同源性,编码相应的Pgp,但仅mdr_1的表达与肿瘤耐药性有关。mdr_1/Pgp具有以下特性:①对一些亲脂细胞毒药物出现天然交叉耐药;②为能量依赖的跨膜外排泵,可将药物泵出细胞外导致该药物在细胞内的蓄积减
Some patients with malignant tumors develop resistance after treatment with anti-tumor drugs, or congenitality is insensitive to chemotherapeutic drugs, which results in poor therapeutic efficacy and leads to recurrence or metastasis. The reason for this phenomenon is currently believed to be multidrug resistance with tumor cells. Related to Multidrug-resistance (MDR). MDR refers to tumor cells cross-resistance to antitumor drugs with different molecular structures and different mechanisms of action. The human tumor multidrug resistance gene family consists of mdr_1 and mdr_3. The MDR phenotype is marked by a 170 kD cell membrane protein called the permeability-glycoprotein (Pgp). Mdr_1 and mdr_3 have higher homology and encode the corresponding Pgp, but only the expression of mdr_1 is related to tumor drug resistance. Mdr_1/Pgp has the following characteristics: 1 The natural cross-resistance to some lipophilic cytotoxic drugs; 2 is an energy-dependent transmembrane efflux pump that pumps the drug out of the cell and causes the accumulation of the drug in cells.