多药耐药是肿瘤化疗失败的主要原因之一,以p-glycoprotein(p-gp)的过度表达为主要特征,可将肿瘤细胞内的化疗药物排出胞外,导致化疗效果降低,从而使肿瘤细胞产生耐药性。抑制p-gp外排药物可以提高化疗药物杀伤肿瘤细胞的作用,对提高化疗效果具有重要意义。多药耐药糖蛋白抑制剂的发展经历了三代,并日趋完善,在化疗中起着重要作用,但仍需改进。本文对多药耐药糖蛋白p-gp及其抑制剂的研究进展作一综述。 Multidrug resistance (MDR) is one of the main reasons for the failure of chemotherapy in cancer. The overexpression of p-glycoprotein (p-gp) is the main feature. It can expel extracellular chemotherapeutic drugs in tumor cells and lead to the decrease of chemotherapy effect, Cells develop resistance. Inhibition of p-gp efflux drugs can enhance the role of chemotherapy drugs to kill tumor cells, to improve the effect of chemotherapy is of great significance. The development of multidrug resistance glycoprotein inhibitors has gone through three generations and is becoming more and more perfect. It plays an important role in chemotherapy, but it still needs improvement. This review summarizes the progress of multidrug resistance glycoprotein p-gp and its inhibitors.