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The first step of this process is the extraction of organic anions from the peritubular blood plasma into proximal tubule cells largely through the organic anion transporter (OAT) pathway. Therefore, the OAT pathway is one of the major sites for body drug clearance\/detoxification. As a result, it is also the site for drug\u2013drug interaction and drug\u2010induced nephrotoxicity. To maximize therapeutic efficacy and minimize toxicity, the structure\u2010function relationships of OATs and their regulation must be defined. The recent cloning and identification of OATs have paved the way for such investigations. This review summarizes the available data on the general properties of OATs, focusing in particular on the recent progress made from the author's laboratory as well as from other's, on the molecular characterization of the structure\u2010function relationships of OATs and their regulatory mechanisms. \u00a9 2002 Wiley Periodicals, Inc. Med Res Rev, 22, No. 6, 602\u2013616, 2002; Published online in Wiley InterScience (<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" xlink:href=\"http:\/\/www.interscience.wiley.com\">www.interscience.wiley.com<\/jats:ext-link>). 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