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However,<jats:italic>in vitro<\/jats:italic>assays currently available are mostly for studying the inhibitory potential of drugs on intestinal transporter proteins, rather than induction. Therefore, this study investigated the suitability of the frequently used intestinal Caco\u20102 cell line to predict transporter\u2010mediated DDIs as caused by induction via activation of nuclear receptors.<\/jats:p><\/jats:sec><jats:sec><jats:title>Methods<\/jats:title><jats:p>TaqMan\u00ae low density arrays and LC\u2013MS\/MS based targeted proteomics were used to evaluate transporter expression in Caco\u20102 cells in comparison with jejunal tissue, in culture\u2013time dependence studies and after incubation with different known inducers of drug metabolism and transport. Additionally, studies on ABCB1 function were performed using Transwell\u00ae assays with [<jats:sup>3<\/jats:sup>H]\u2010digoxin and [<jats:sup>3<\/jats:sup>H]\u2010talinolol as substrates after incubation with the prototypical inducers rifampicin, St John's wort, carbamazepine and efavirenz.<\/jats:p><\/jats:sec><jats:sec><jats:title>Results<\/jats:title><jats:p>The gene and protein expression pattern of drug transporters in Caco\u20102 cells and jejunal tissue differed considerably. For some transporters culture\u2010time dependent differences in mRNA expression and\/or protein abundance could be determined. Finally, none of the studied prototypical inducers showed an effect either on mRNA expression and protein abundance or on the function of ABCB1.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusion<\/jats:title><jats:p>Differences in transporter expression in Caco\u20102 cells compared with jejunal tissue, as well as expression dependence on culture time must be considered in<jats:italic>in vitro<\/jats:italic>studies to avoid under\u2010 or overestimation of certain transporters. The Caco\u20102 cell model is not suitable for the evaluation of DDIs caused by transporter induction. Copyright \u00a9 2016 John Wiley &amp; Sons, Ltd.<\/jats:p><\/jats:sec>","DOI":"10.1002\/bdd.2025","type":"journal-article","created":{"date-parts":[[2016,8,12]],"date-time":"2016-08-12T07:08:40Z","timestamp":1470985720000},"page":"115-126","source":"Crossref","is-referenced-by-count":62,"title":["Caco\u20102 cells \u2013 expression, regulation and function of drug transporters compared with human jejunal tissue"],"prefix":"10.1002","volume":"38","author":[{"given":"S.","family":"Br\u00fcck","sequence":"first","affiliation":[{"name":"Department of Clinical Pharmacology, Center of Drug Absorption and Transport University Medicine Greifswald Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"J.","family":"Strohmeier","sequence":"additional","affiliation":[{"name":"Department of Clinical Pharmacology, Center of Drug Absorption and Transport University Medicine Greifswald 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