Using purified P-glycoprotein to understand multidrug resistance

Since P-glycoprotein was discovered almost 20 years ago, its causative role in multidrug resistance has been established, but central problems of its biochemistry have not been definitively resolved. Recently, major advances have been made in P-glycoprotein biochemistry with the use of purified and reconstituted P-glycoprotein, as well as membranes from nonmammalian cells containing heterologously expressed P-glycoprotein. In this review we describe recent findings using these systems which are elucidating the molecular mechanism of P-glycoprotein-mediated drug transport.