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寻找高效、低毒、专属性的多药耐药逆转剂是肿瘤化疗中亟需解决的难题。但是由于其作用机制的本质仍不清楚 ,这一问题的解决很困难。鉴于 P-糖蛋白的重要作用 ,研究其介导的多药耐药逆转剂的构效关系有助于揭示多药耐药性的产生及其逆转机制 ,设计理想的可用于临床的逆转剂。本文概述了对多药耐药逆转剂构效关系研究方法的认识 ,总结了近来出现的一些逆转剂特定的构效关系 ,并介绍了这方面的研究状况。
Looking for efficient, low toxicity, specificity of multidrug resistance reversal agents is an urgent problem to be solved in the chemotherapy of tumors. However, due to the fact that the nature of its mechanism of action is still unclear, the solution to this problem is very difficult. In view of the important role of P-glycoprotein, the study of the structure-activity relationship of its multidrug resistance reversal agents will help reveal the generation of multidrug resistance and its reversal mechanism, and design an ideal reversal agent for clinical use. This article summarizes the understanding of the research methods of structure-activity relationship of multidrug resistance reversal agents, summarizes the recent emergence of some specific structure-activity relationships of reversal agents, and introduces the research status in this aspect.