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Organic anion transporters (OATs) mediate the renal absorption and excretion of a wide range of metabolites and xenobiotics. We discuss the recent advances that have been made in elucidating the binding and transport characteristics of OATs, new insights into their physiological role and regulation by various factors, and pharmacogenetics.Overlapping substrate specificity among the OATs is well established. However, recent findings have suggested distinct differences in the structural binding determinants among the OATs, which have important implications for understanding drug interactions and drug design. A potential role for OATs in blood pressure regulation and remote sensing has been reported. Meanwhile, factors regulating the expression of OATs continue to be identified and characterized. The effect of renal ischemia on OAT expression and function is currently being explored. Finally, recent studies identifying various OAT polymorphisms may facilitate prediction of individual drug response and toxicity.As progress is made in unveiling the many functional aspects of the OATs, it is becoming clear that their significance is not only limited to a role in drug elimination from the body, but also extends to other vital physiological roles. Further delineation of the function and regulation of the OATs will uncover enormous potential clinical and pharmacological applications.