Multidrug efflux pump is the main reason for bacterial multidrug resistance, and it’s a challenge for the treatment of infectious diseases. Analysis of multidrug efflux pump offers us the mechanism and treatment ideas of bacterial multidrug resistance. New advances have been made in the study of Escherichia coli AcrAB-TolC efflux pump structure and its regulation, which provides data for the multidrug resistance research in pathogenic bacterium. Progress in this area is reviewed here.