Article ; Online: Expression of xenobiotic transporters in the human renal proximal tubule cell line RPTEC/TERT1.
Toxicology in vitro : an international journal published in association with BIBRA
2014 Volume 30, Issue 1 Pt A, Page(s) 95–105
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 ... ...
| 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. |
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| MeSH term(s) | Carrier Proteins/genetics ; Carrier Proteins/metabolism ; Cell Line ; Gene Expression Regulation/physiology ; Humans ; Kidney Tubules, Proximal/cytology ; Kidney Tubules, Proximal/metabolism ; RNA, Messenger/genetics ; RNA, Messenger/metabolism | |||||
| Chemical Substances | Carrier Proteins ; RNA, Messenger | |||||
| Language | English | |||||
| Publishing date | 2014-12-10 | |||||
| Publishing country | England | |||||
| Document type | Journal Article ; Research Support, Non-U.S. Gov't | |||||
| ZDB-ID | 639064-x | |||||
| ISSN | 1879-3177 ; 0887-2333 | |||||
| ISSN (online) | 1879-3177 | |||||
| ISSN | 0887-2333 | |||||
| DOI | 10.1016/j.tiv.2014.12.003 | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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