Impact of Drug Transport Proteins

Abstract

Drug transporters play critical roles in the absorption, distribution, and excretion of drugs and have been classified into five major families, peptide transporters (PEPT, SLC15), organic anion-transporting polypeptides (OATP, SLCO), organic ion transporters (OCT/OCTN/OAT/URAT, SLC22), H{su+}/organic cation antiporters (MATE, SLC47), and ABC drug transporters, such as P-glycoprotein (P-gp/MDR1, ABCB1). Their structures, tissue distribution, functions, and pharmacokinetic roles vary. The roles of drug transporters can be assessed in vitro and in vivo, using techniques spanning from cellular expression systems to gene knockout animals. Research outcomes from such studies have been applied to clinical science and drug development. In this chapter, the basic characteristics of drug transporters were reviewed with an emphasis on their impact on clinical/preclinical research.