多药耐药性(简称 MDR)是许多药物抗性中的一种。目前国内外对其研究较多,其机制较为复杂,可分为 P-170糖蛋白介异的 MDR(Pgp-MDR)、拓扑异构酶Ⅱ介导的 MDR(at-MDR)和非 P-170糖蛋白介导的 MDR。本文围绕 at-MDR 讲述了真核生物拓扑异构酶Ⅱ的生物学,以拓扑异构酶Ⅱ为靶子的抗癌药物的作用机理,at-MDR 的特征,at-MDR 生化和分子基础,at-MDR 的治疗以及将来研究的重点。 Multidrug resistance (abbreviated as MDR) is one of many drug resistances. At present, there are many studies at home and abroad, and the mechanism is more complicated. It can be divided into P-170 glycoprotein-mediated MDR (Pgp-MDR), topoisomerase II mediated MDR (at-MDR) and non-P- 170 glycoprotein mediated MDR. This paper describes the biology of eukaryotic topoisomerase II, the mechanism of action of anticancer drugs targeting topoisomerase II, the characteristics of at-MDR, the biochemistry and molecular basis of at-MDR, at -MDR treatment and focus of future research.