Hiroshi Omote, Miki Hiasa
The purification and reconstitution technique is a powerful method to determine the functions of multidrug transporters. Elucidation of the transport properties of multidrug transporters is important to understand the pharmacokinetics of drugs; however, their detailed analysis is difficult due to various factors, such as drug hydrophobicity and direction of transport. In this chapter, we describe protocols based on spin label and spin column methods to assess drug transport using purified and reconstituted human multidrug and toxin extrusion protein 1 and P-glycoprotein.