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.