title: Organic anion-transporting polypeptides.
abstract: Organic anion-transporting polypeptides or OATPs are central transporters in the disposition of drugs and other xenobiotics. In addition, they mediate transport of a wide variety of endogenous substrates. The critical role of OATPs in drug disposition has spurred research both in academia and in the pharmaceutical industry. Translational aspects with clinical questions are the focus in academia, while the pharmaceutical industry tries to define and understand the role these transporters play in pharmacotherapy. The present overview summarizes our knowledge on the interaction of food constituents with OATPs and on the OATP transport mechanisms. Further, it gives an update on the available information on the structure-function relationship of the OATPs and, finally, covers the transcriptional and posttranscriptional regulation of OATPs.
authors.affiliation: Department of Clinical Pharmacology and Toxicology, University Hospital, Zürich, Switzerland. Electronic address: bstieger@kpt.uzh.ch.
authors.forename: Bruno
authors.initials: B
authors.lastname: Stieger
authors.affiliation: Department of Pharmacology, Toxicology and Therapeutics, The University of Kansas Medical Center, Kansas City, Kansas, USA.
authors.forename: Bruno
authors.initials: B
authors.lastname: Hagenbuch
mesh_terms: D000818:Animals; D001688:Biological Products / Q000378:metabolism; D001692:Biological Transport; D005786:Gene Expression Regulation; D006801:Humans; D027361:Organic Anion Transporters / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D011499:Protein Processing, Post-Translational; D014158:Transcription, Genetic
chemical_list: D001688:Biological Products; D027361:Organic Anion Transporters
keywords: Drug; OATP; Organic anion; Transport
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