1. The organic anion transporting polypeptides (humans OATP; other species Oatp) belong to the SLCO gene superfamily of transporters and are twelve transmembrane domain glycoproteins expressed in various epithelial cells. Some OATPs/Oatps are expressed in a single organ, while others are expressed ubiquitously. 2. The functionally characterized members mediate sodium-independent transport of a variety of structurally independent, mainly amphipathic organic compounds, including bile salts, hormones and their conjugates, toxins, and various drugs. 3. This review summarizes the general features and the substrates of the eleven human OATPs. Furthermore, it reviews what is known about the mechanism of their multispecificity, their predicted structure, their role in drug-food interactions, and their role in cancer. 4. Finally, some open questions are raised that need to be addressed to advance OATP research in the near future.