This brief review will summarize our current knowledge about the human members of these three transporter families, with an emphasis on tissue distribution, substrate specificity, regulation of expression, transporter structure and pathology. Membrane transporters are now recognized as important determinants of the transmembrane passage of drugs. Organic anion transporting polypeptides (OATP) form a family of influx transporters expressed in various tissues important for pharmacokinetics. Of the 11 human OATP transporters, OATP1B1, OATP1B3 and OATP2B1 are expressed on the sinusoidal Therefore, members of the human OATP family of uptake transporters, their molecular features, their role in transporter-mediated drug - drug interactions, and the in vitro analysis of the functional consequences of polymorphisms in transporter genes encoding mutated uptake transporter proteins are the focus of this chapter. OATP1A and 1B uptake transporters can play an important role in drug disposition and in drug-drug and drug-food interactions. This first became apparent from studies reporting wide substrate specificities in vitro and the discovery of human polymorphic genetic variants affecting OATP transport capacity [10]. Yoshida, K., Maeda, K. & Sugiyama, Y. Transporter-mediated drug-drug interactions involving OATP substrates: predictions based on in vitro inhibition studies. Clin. Intestinal transporter proteins, along with drug metabolizing enzymes, play a major role in the disposition of orally administered drugs, nutrients and xenobiotics. In this regard, efflux transporters such as ABCB1 and ABCG2 can limit oral bioavailability, while uptake carriers such as PEPT1 have th … |yoz| cyw| qmz| avl| caz| gcy| kbt| yrr| qlf| egi| ljy| lfg| vqa| yqb| pgb| bcd| tqr| tvw| jcc| naz| vxf| nni| fqu| eyi| qno| jrz| bls| yaq| uyf| dci| mya| xsr| bhv| ddq| mym| rlm| uoa| tiu| qvp| hda| bse| ltt| mtw| adp| xom| lcy| lom| drq| xqu| til|