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Organic Cation Transporter OCTs (SLC22) and MATEs (SLC47) in the Human Kidney

  • Review Article
  • Theme: Kidney Transporters: Importance in Clearance, Disease, and Drug-Drug Interactions
  • Published:
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Abstract

In the kidney, human organic cation transporters (OCTs) and multidrug and toxin extrusion proteins (MATEs) are the major transporters for the secretion of cationic drugs into the urine. In the human kidney, OCT2 mediates the uptake of drugs from the blood at the basolateral membrane of tubular epithelial cells, and MATE1 and MATE2-K secrete drugs from cells into the lumen of proximal tubules. However, the expression of these transporters depends on the species of the animal. In the rodent kidney, OCT1 and OCT2 are expressed at the basolateral membrane, and MATE1 localizes at the brush-border membrane. Together, these transporters recognize various compounds and have overlapping, but somewhat different, substrate specificities. OCTs and MATEs can transport important drugs, such as metformin and cisplatin. Therefore, functional variation in OCTs and MATEs, including genetic polymorphisms or inter-individual variation, may seriously affect the pharmacokinetics and/or pharmacodynamics of cationic drugs. In this review, we summarize the recent findings and clinical importance of these transporters.

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ACKNOWLEDGMENTS

This work was supported in part by a grant-in-aid for Scientific Research (KAKENHI) from the Ministry of Education, Culture, Sports, Science and Technology of Japan.

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The authors declare no conflict of interests.

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Authors and Affiliations

  1. Kyoto Pharmaceutical University, Yamashina-ku, Kyoto, 607-8414, Japan

    Hideyuki Motohashi & Ken-ichi Inui

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  1. Hideyuki Motohashi
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  2. Ken-ichi Inui
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Correspondence to Ken-ichi Inui.

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Guest Editors: Marilyn Morris and Colin Brown

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Motohashi, H., Inui, Ki. Organic Cation Transporter OCTs (SLC22) and MATEs (SLC47) in the Human Kidney. AAPS J 15, 581–588 (2013). https://doi.org/10.1208/s12248-013-9465-7

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  • DOI: https://doi.org/10.1208/s12248-013-9465-7

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