P-glycoprotein(P-gp) plays an important role in multidrug resistance(MDR).This article was focused on the protein structure and the mechanism of P-gp,and especially on the current status in anti-P-gp drug research and discovery.The action of P-gp in MDR was also reviewed.Moreover,the potential adverse reaction of P-gp inhibitors were emphasized since P-gp was involved in the normal function of a lot of organs.