Abstract
In the past decade, a comprehensive list of membrane transporters has become available owing to the progress in genome analysis, as well as extensive membrane physiological and molecular biological studies on membrane transporters. Major membrane transporters have been classified into the solute carrier (SLC) transporter family and the ATP-binding cassette (ABC) transporter family. The SLC family consists of 43 gene subfamilies and a total of about 319 family members, including ion-coupled transporters, facilitated transporters, and exchangers. In the ABC transporter family, 49 genes have been identified and classified into nine subfamilies. Some of these transporters accept not only physiological or endogenous substrates, but also xenobiotics, including drugs. Such drug transporters are very important, because they play pivotal roles in determining the pharmacokinetic profiles of particular drugs and thereby determine the overall pharmacological effects, i.e., drug absorption, distribution, elimination, and concentration at the target sites. This review aims to provide clues that will allow us to establish efficient strategies to use transporters for target and lead discovery.
