title: Organic Anion Transporter 2: An Enigmatic Human Solute Carrier.
abstract: As a member of the solute carrier 22A (SLC22A) family, organic anion transporter 2 (OAT2; SLC22A7) is emerging as an important drug transporter because of its expression in both the liver and kidney, two major eliminating organs, and its ability to transport not only a wide variety of xenobiotics but also numerous physiologically important endogenous compounds, like creatinine and cGMP. However, OAT2 has received relatively little attention compared with other OATs and solute carriers (SLCs), like organic cation transporters, sodium-dependent taurocholate cotransporting polypeptide, multidrug and toxin extrusion proteins, and organic anion-transporting polypeptides. Overall, the literature describing OAT2 is rapidly evolving, with numerous publications contradicting each other regarding the transport mechanism, tissue distribution, and transport of creatinine and cGMP, two important endogenous OAT2 substrates. Despite its status as a liver and kidney SLC, tools for assessing its activity and inhibition are lacking, and its role in drug disposition and elimination remains to be defined. The current review focuses on the available and emerging literature describing OAT2. We envision that OAT2 will gain more prominence as its expression, substrate, and inhibitor profile is investigated further and compared with other SLCs.
authors.affiliation: Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Research and Development, Princeton, New Jersey (H.S., Y.L.), and Department of Pharmacokinetics, Dynamics, and Metabolism, Pfizer World Wide Research and Development, Groton, Connecticut (A.D.R.) hong.shen1@bms.com.
authors.forename: Hong
authors.initials: H
authors.lastname: Shen
authors.affiliation: Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Research and Development, Princeton, New Jersey (H.S., Y.L.), and Department of Pharmacokinetics, Dynamics, and Metabolism, Pfizer World Wide Research and Development, Groton, Connecticut (A.D.R.).
authors.forename: Yurong
authors.identifier: 0000-0001-9505-333X
authors.initials: Y
authors.lastname: Lai
authors.affiliation: Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Research and Development, Princeton, New Jersey (H.S., Y.L.), and Department of Pharmacokinetics, Dynamics, and Metabolism, Pfizer World Wide Research and Development, Groton, Connecticut (A.D.R.).
authors.forename: A David
authors.initials: AD
authors.lastname: Rodrigues
mesh_terms: D000818:Animals; D001692:Biological Transport; D002460:Cell Line; D002462:Cell Membrane / Q000378:metabolism; D003404:Creatinine / Q000378:metabolism; D006801:Humans; D007668:Kidney / Q000378:metabolism*; D008099:Liver / Q000378:metabolism*; D008657:Metabolic Clearance Rate; D029362:Organic Anion Transporters, Sodium-Independent / Q000235:genetics / Q000378:metabolism*; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D013379:Substrate Specificity; D015262:Xenobiotics / Q000493:pharmacokinetics*
chemical_list: D029362:Organic Anion Transporters, Sodium-Independent; D004364:Pharmaceutical Preparations; C490280:SLC22A7 protein, human; D015262:Xenobiotics; D003404:Creatinine