title: The genetic polymorphism of drug transporters: functional analysis approaches.
abstract: Evidence is accumulating to strongly suggest that drug transporters are one of the determining factors governing the pharmacokinetic profile of drugs. To date, a variety of drug transporters have been cloned and classified as solute carriers and ATP-binding cassette transporters. Such drug transporters are expressed in various tissues such as the intestine, brain, liver, and kidney, and play critical roles in the absorption, distribution and excretion of drugs. However, at the present time, information is limited regarding the genetic polymorphism of drug transporters and its impact on their function. In this context, we have undertaken the functional analyses of the polymorphisms identified in drug transporter genes. This article aims to provide an overview on the functional aspects of the non-synonymous polymorphisms of drug transporters and to present standard methods for the evaluation of the effect of polymorphisms on their function.
authors.affiliation: Department of Biomolecular Engineering, Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology, 4259 Nagatsuta, Midori-ku, Yokohama, 226-8501, Japan. tishikaw@bio.titech.ac.jp
authors.forename: Toshihisa
authors.initials: T
authors.lastname: Ishikawa
authors.forename: Akira
authors.initials: A
authors.lastname: Tsuji
authors.forename: Kenichi
authors.initials: K
authors.lastname: Inui
authors.forename: Yoshimichi
authors.initials: Y
authors.lastname: Sai
authors.forename: Naohiko
authors.initials: N
authors.lastname: Anzai
authors.forename: Morimasa
authors.initials: M
authors.lastname: Wada
authors.forename: Hitoshi
authors.initials: H
authors.lastname: Endou
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Sumino
mesh_terms: D000818:Animals; D001692:Biological Transport / Q000235:genetics; D002352:Carrier Proteins / Q000235:genetics* / Q000378:metabolism; D006801:Humans; D004364:Pharmaceutical Preparations / Q000378:metabolism; D010599:Pharmacokinetics; D020641:Polymorphism, Single Nucleotide; D013379:Substrate Specificity
chemical_list: D002352:Carrier Proteins; D004364:Pharmaceutical Preparations