Max-Delbrück-Center for Molecular Medicine, Robert-Rössle-Strasse 10, 13122, Berlin, Germany.,
Cytotechnology. 1998 Sep;27(1-3):271-82. doi: 10.1023/A:1008089512856.
The occurrence of the multidrug resistance phenotype still represents a limiting factor for successful cancer chemotherapy. Numerous efforts have been made to develop strategies for reversal and/or modulation of this major therapy obstacle through targeting at different levels of intervention. The phenomenon of MDR is often associated with overexpression of resistance-associated genes. Since the classical type of MDR in human cancers is mainly mediated by the P-glycoprotein encoded by the multidrug resistance gene 1, mdr1, the majority of reversal approaches target the expression and/or function of the mdr1 gene/P-glycoprotein. Due to the fact that the multidrug phenotype always represents the net effect of a panel of resistance-associated genes/gene products, other resistance genes, e.g. those encoding the multidrug resistance-associated protein MRP or the lung resistance protein LRP, were included in the studies. Cytokines such as tumor necrosis factor alpha and interleukin-2 have been shown to modulate the MDR phenotype in different experimental settings in vitro and in vivo. Several studies have been performed to evaluate their potential as chemosensitizers of tumor cells in the context of a combined application of MDR-associated anticancer drugs like doxorubicin and vincristine with cytokines. Moreover, the capability of cytokines to modulate the expression of MDR-associated genes was demonstrated, either by external addition or by transduction of the respective cytokine gene. Knowledge of the combination effects of cytokines and cytostatics and its link to their MDR-modulating capacity may contribute to a more efficient and to a more individualized immuno-chemotherapy of human malignancies.
多药耐药表型的发生仍然是癌症化疗成功的一个限制因素。为了通过针对不同干预水平来逆转和/或调节这一主要治疗障碍,人们已经做出了许多努力。MDR 现象通常与耐药相关基因的过度表达有关。由于人类癌症中的经典型 MDR 主要是由多药耐药基因 1(mdr1)编码的 P 糖蛋白介导的,因此大多数逆转方法的目标是 mdr1 基因/P-糖蛋白的表达和/或功能。由于多药耐药表型始终代表一组耐药相关基因/基因产物的净效应,因此其他耐药基因,例如编码多药耐药相关蛋白 MRP 或肺耐药蛋白 LRP 的基因,也被包括在研究中。细胞因子,如肿瘤坏死因子-α和白细胞介素-2,已被证明在不同的实验环境中,无论是在体外还是体内,都能调节 MDR 表型。已经进行了几项研究,以评估它们作为与多药耐药相关的抗癌药物(如阿霉素和长春新碱)联合应用时,对肿瘤细胞的化疗增敏作用的潜力。此外,细胞因子能够调节 MDR 相关基因的表达,无论是通过外部添加还是通过转导相应的细胞因子基因。细胞因子和细胞抑制剂的联合作用的知识及其与它们的 MDR 调节能力的联系,可能有助于更有效地进行针对人类恶性肿瘤的个体化免疫化疗。