title: Expression of xenobiotic transporters in the human renal proximal tubule cell line RPTEC/TERT1.
abstract: The kidney is a major target for drug-induced injury, primarily due the fact that it transports a wide variety of chemical entities into and out of the tubular lumen. Here, we investigated the expression of the main xenobiotic transporters in the human renal proximal tubule cell line RPTEC/TERT1 at an mRNA and/or protein level. RPTEC/TERT1 cells expressed OCT2, OCT3, OCTN2, MATE1, MATE2, OAT1, OAT3 and OAT4. The functionality of the OCTs was demonstrated by directional transport of the fluorescent dye 4-Di-1-ASP. In addition, P-glycoprotein activity in RPTEC/TERT1 cells was verified by fluorescent dye retention in presence of various P-glycoprotein inhibitors. In comparison to proliferating cells, contact inhibited RPTEC/TERT1 cells expressed increased mRNA levels of several ABC transporter family members and were less sensitive to cyclosporine A. We conclude that differentiated RPTEC/TERT1 cells are well suited for utilisation in xenobiotic transport and pharmacokinetic studies.
authors.affiliation: Medical University of Innsbruck, Department of Physiology and Medical Physics, Division of Physiology, Fritz-Pregl-Str. 3, 6020 Innsbruck, Austria.
authors.forename: Lydia
authors.initials: L
authors.lastname: Aschauer
authors.affiliation: Medical University of Innsbruck, Department of Physiology and Medical Physics, Division of Physiology, Fritz-Pregl-Str. 3, 6020 Innsbruck, Austria.
authors.forename: Giada
authors.initials: G
authors.lastname: Carta
authors.affiliation: Universitätsklinikum Münster, Medizinische Klinik D, Experimentelle Nephrologie, Albert-Schweitzer-Campus 1 (A14), Interdisziplinäres Zentrum für Klinische Forschung (IZKF), 48149 Münster, Germany.
authors.forename: Nadine
authors.initials: N
authors.lastname: Vogelsang
authors.affiliation: Universitätsklinikum Münster, Medizinische Klinik D, Experimentelle Nephrologie, Albert-Schweitzer-Campus 1 (A14), Interdisziplinäres Zentrum für Klinische Forschung (IZKF), 48149 Münster, Germany.
authors.forename: Eberhard
authors.initials: E
authors.lastname: Schlatter
authors.affiliation: Medical University of Innsbruck, Department of Physiology and Medical Physics, Division of Physiology, Fritz-Pregl-Str. 3, 6020 Innsbruck, Austria. Electronic address: Paul.Jennings@i-med.ac.at.
authors.forename: Paul
authors.initials: P
authors.lastname: Jennings
mesh_terms: D002352:Carrier Proteins / Q000235:genetics / Q000378:metabolism*; D002460:Cell Line; D005786:Gene Expression Regulation / Q000502:physiology*; D006801:Humans; D007687:Kidney Tubules, Proximal / Q000166:cytology* / Q000378:metabolism; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism
chemical_list: D002352:Carrier Proteins; D012333:RNA, Messenger
keywords: ABC; Epithelia; OAT; OCT; RPTEC/TERT1; Transport