Membrane Transport Proteins and Drug Transport

Abstract To exert their intended therapeutic goal, drugs need to cross epithelial barriers to reach their site of action. Transport proteins have critical physiological roles in nutrient absorption and transport of endogenous compounds. These systems can serve as useful pharmacological targets and may be used as a mechanism to increase drug absorption. However, we have little understanding of these proteins at the molecular level because of the absence of high resolution crystal structures. Numerous efforts have been made to characterize the P‐glycoprotein efflux pump, the peptide transporter PepT1, and the apical sodium‐dependent transporter, which are important not only for their native transporter function but also as drug targets to increase absorption and bioactivity.In vitroand computational approaches have been applied to gain some insight into these transporters with some success. This represents an opportunity for optimizing molecules as substrates for the solute transporters and providing a further screening system for drug discovery. Clearly the future growth in knowledge of transporter function will be led by integratedin vitroandin silicoapproaches.