Stieger Bruno, Hagenbuch Bruno
Department of Clinical Pharmacology and Toxicology, University Hospital, Zürich, Switzerland.
Department of Pharmacology, Toxicology and Therapeutics, The University of Kansas Medical Center, Kansas City, Kansas, USA.
Curr Top Membr. 2014;73:205-32. doi: 10.1016/B978-0-12-800223-0.00005-0.
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.
有机阴离子转运多肽（OATPs）是药物和其他外源性物质处置过程中的关键转运蛋白。此外，它们还介导多种内源性底物的转运。OATPs在药物处置中的关键作用激发了学术界和制药行业的研究。学术界关注与临床问题相关的转化研究，而制药行业则试图确定并理解这些转运蛋白在药物治疗中所起的作用。本综述总结了我们关于食物成分与OATPs相互作用以及OATPs转运机制的知识。此外，它还更新了有关OATPs结构-功能关系的现有信息，最后涵盖了OATPs的转录和转录后调控。
