Using Structural and Mechanistic Information to Design Novel Inhibitors/Substrates of P-Glycoprotein

Design of inhibitors of P-glycoprotein still represents a challenging task for medicinal chemists. The polyspecificity of the transporter combined with the limited structural information renders rational drug design approaches rather ineffective. Within this article we will exemplify how recent insights into structure and mechanism of Pglycoprotein may aid in design of potent inhibitors. P>