Expression and transport function of drug uptake transporters in differentiated HepaRG cells

Molecular Pharmaceutics

Volumn 9, Issue 12, 2012, Pages 3434-3441

  Kotani, Naoki ^a   Maeda, Kazuya ^a   Debori, Yasuyuki ^a   Camus, Sandrine ^b   Li, Ruoya ^b   Chesne, Christophe ^b   Sugiyama, Yuichi ^c  

^a UNIVERSITY OF TOKYO   (Japan)

^b BIOPREDIC   (France)

^c RIKEN   (Japan)

Author keywords

cryopreserved human hepatocytes; drug?drug interaction; HepaRG cells; hepatic uptake; Na + taurocholate cotransporting polypeptide (NTCP); organic anion transporting polypeptide (OATP)

Indexed keywords

CHOLECYSTOKININ OCTAPEPTIDE; ESTRADIOL 17 GLUCURONIDE; ESTRONE SULFATE; MESSENGER RNA; OLMESARTAN; ORGANIC ANION TRANSPORTER; ORGANIC ANION TRANSPORTER 1B1; ORGANIC ANION TRANSPORTER 1B3; ORGANIC ANION TRANSPORTER 2B1; PITAVASTATIN; POLYPEPTIDE; SODIUM TAUROCHOLATE COTRANSPORTING POLYPEPTIDE; TAUROCHOLIC ACID; UNCLASSIFIED DRUG;

ARTICLE; CELL DIFFERENTIATION; CELL STRAIN HEK293; DRUG CLEARANCE; DRUG UPTAKE; ENZYME ACTIVITY; HUMAN; HUMAN CELL; LIVER CELL; PRIORITY JOURNAL; PROTEIN BLOOD LEVEL; PROTEIN EXPRESSION; PROTEIN TRANSPORT;

BIOLOGICAL TRANSPORT; BLOTTING, WESTERN; CELL DIFFERENTIATION; CELLS, CULTURED; DETERGENTS; DRUG INTERACTIONS; FLOW CYTOMETRY; HEK293 CELLS; HEPATOCYTES; HUMANS; ORGANIC ANION TRANSPORTERS; ORGANIC ANION TRANSPORTERS, SODIUM-DEPENDENT; ORGANIC ANION TRANSPORTERS, SODIUM-INDEPENDENT; SYMPORTERS; TAUROCHOLIC ACID;

EID: 84870532588     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp300171p     Document Type: Article

References (33)

1. Ieiri, I.; Higuchi, S.; Sugiyama, Y. Genetic polymorphisms of uptake (OATP1B1, 1B3) and efflux (MRP2, BCRP) transporters: implications for inter-individual differences in the pharmacokinetics and pharmacodynamics of statins and other clinically relevant drugs Expert Opin. Drug Metab. Toxicol. 2009, 5, 703-29
2. Maeda, K.; Sugiyama, Y. Impact of genetic polymorphisms of transporters on the pharmacokinetic, pharmacodynamic and toxicological properties of anionic drugs Drug Metab. Pharmacokinet. 2008, 23, 223-35
3. Shou, M.; Hayashi, M.; Pan, Y.; Xu, Y.; Morrissey, K.; Xu, L.; Skiles, G. L. Modeling, prediction, and in vitro in vivo correlation of CYP3A4 induction Drug Metab. Dispos. 2008, 36, 2355-70
4. Giacomini, K. M.; Huang, S. M.; Tweedie, D. J.; Benet, L. Z.; Brouwer, K. L.; Chu, X.; Dahlin, A.; Evers, R.; Fischer, V.; Hillgren, K. M.; Hoffmaster, K. A.; Ishikawa, T.; Keppler, D.; Kim, R. B.; Lee, C. A.; Niemi, M.; Polli, J. W.; Sugiyama, Y.; Swaan, P. W.; Ware, J. A.; Wright, S. H.; Yee, S. W.; Zamek-Gliszczynski, M. J.; Zhang, L. Membrane transporters in drug development Nat Rev. Drug Discovery 2010, 9, 215-36
5. Abe, K.; Bridges, A. S.; Brouwer, K. L. Use of sandwich-cultured human hepatocytes to predict biliary clearance of angiotensin II receptor blockers and HMG-CoA reductase inhibitors Drug Metab. Dispos. 2009, 37, 447-52
6. Watanabe, T.; Kusuhara, H.; Maeda, K.; Kanamaru, H.; Saito, Y.; Hu, Z.; Sugiyama, Y. Investigation of the rate-determining process in the hepatic elimination of HMG-CoA reductase inhibitors in rats and humans Drug Metab. Dispos. 2010, 38, 215-22
7. Garcia, M.; Rager, J.; Wang, Q.; Strab, R.; Hidalgo, I. J.; Owen, A.; Li, J. Cryopreserved human hepatocytes as alternative in vitro model for cytochrome p450 induction studies In Vitro Cell. Dev. Biol.: Anim. 2003, 39, 283-7 (Pubitemid 38200249)
8. Shitara, Y.; Li, A. P.; Kato, Y.; Lu, C.; Ito, K.; Itoh, T.; Sugiyama, Y. Function of uptake transporters for taurocholate and estradiol 17beta-D-glucuronide in cryopreserved human hepatocytes Drug Metab. Pharmacokinet. 2003, 18, 33-41
9. Antherieu, S.; Chesne, C.; Li, R.; Camus, S.; Lahoz, A.; Picazo, L.; Turpeinen, M.; Tolonen, A.; Uusitalo, J.; Guguen-Guillouzo, C.; Guillouzo, A. Stable expression, activity, and inducibility of cytochromes P450 in differentiated HepaRG cells Drug Metab. Dispos. 2010, 38, 516-25
10. Gripon, P.; Rumin, S.; Urban, S.; Le Seyec, J.; Glaise, D.; Cannie, I.; Guyomard, C.; Lucas, J.; Trepo, C.; Guguen-Guillouzo, C. Infection of a human hepatoma cell line by hepatitis B virus Proc. Natl. Acad. Sci. U.S.A. 2002, 99, 15655-60 (Pubitemid 35403987)
11. Aninat, C.; Piton, A.; Glaise, D.; Le Charpentier, T.; Langouet, S.; Morel, F.; Guguen-Guillouzo, C.; Guillouzo, A. Expression of cytochromes P450, conjugating enzymes and nuclear receptors in human hepatoma HepaRG cells Drug Metab. Dispos. 2006, 34, 75-83 (Pubitemid 43042648)
12. Kaneko, A.; Kato, M.; Sekiguchi, N.; Mitsui, T.; Takeda, K.; Aso, Y. In vitro model for the prediction of clinical CYP3A4 induction using HepaRG cells Xenobiotica 2009, 39, 803-10
13. McGill, M. R.; Yan, H. M.; Ramachandran, A.; Murray, G. J.; Rollins, D. E.; Jaeschke, H. HepaRG cells: a human model to study mechanisms of acetaminophen hepatotoxicity Hepatology 2011, 53, 974-82
14. Ndongo-Thiam, N.; Berthillon, P.; Errazuriz, E.; Bordes, I.; De Sequeira, S.; Trepo, C.; Petit, M. A. Long-term propagation of serum hepatitis C virus (HCV) with production of enveloped HCV particles in human HepaRG hepatocytes Hepatology 2011, 54, 406-17
15. Kanebratt, K. P.; Andersson, T. B. Evaluation of HepaRG cells as an in vitro model for human drug metabolism studies Drug Metab. Dispos. 2008, 36, 1444-52 (Pubitemid 351929328)
16. Le Vee, M.; Jigorel, E.; Glaise, D.; Gripon, P.; Guguen-Guillouzo, C.; Fardel, O. Functional expression of sinusoidal and canalicular hepatic drug transporters in the differentiated human hepatoma HepaRG cell line Eur. J. Pharm. Sci. 2006, 28, 109-17
17. Cui, Y.; Konig, J.; Nies, A. T.; Pfannschmidt, M.; Hergt, M.; Franke, W. W.; Alt, W.; Moll, R.; Keppler, D. Detection of the human organic anion transporters SLC21A6 (OATP2) and SLC21A8 (OATP8) in liver and hepatocellular carcinoma Lab. Invest. 2003, 83, 527-38 (Pubitemid 36457707)
18. Hariparsad, N.; Carr, B. A.; Evers, R.; Chu, X. Comparison of immortalized Fa2N-4 cells and human hepatocytes as in vitro models for cytochrome P450 induction Drug Metab. Dispos. 2008, 36, 1046-55 (Pubitemid 351717461)
19. Hirano, M.; Maeda, K.; Shitara, Y.; Sugiyama, Y. Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans J. Pharmacol. Exp. Ther. 2004, 311, 139-46 (Pubitemid 39287793)
20. Sasaki, M.; Suzuki, H.; Ito, K.; Abe, T.; Sugiyama, Y. Transcellular transport of organic anions across a double-transfected Madin-Darby canine kidney II cell monolayer expressing both human organic anion-transporting polypeptide (OATP2/SLC21A6) and Multidrug resistance-associated protein 2 (MRP2/ABCC2) J. Biol. Chem. 2002, 277, 6497-503 (Pubitemid 34968447)
21. Lowry, O. H.; Rosebrough, N. J.; Farr, A. L.; Randall, R. J. Protein measurement with the Folin phenol reagent J. Biol. Chem. 1951, 193, 265-75
22. Konig, J.; Cui, Y.; Nies, A. T.; Keppler, D. Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide J. Biol. Chem. 2000, 275, 23161-8 (Pubitemid 30646210)
23. Konig, J.; Cui, Y.; Nies, A. T.; Keppler, D. A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane Am. J. Physiol. 2000, 278, G156-64
24. Yamaoka, K.; Tanigawara, Y.; Nakagawa, T.; Uno, T. A pharmacokinetic analysis program (multi) for microcomputer J. Pharmacobio-Dyn. 1981, 4, 879-85 (Pubitemid 12174128)
25. Le Vee, M.; Gripon, P.; Stieger, B.; Fardel, O. Down-regulation of organic anion transporter expression in human hepatocytes exposed to the proinflammatory cytokine interleukin 1beta Drug Metab. Dispos. 2008, 36, 217-22 (Pubitemid 351185762)
26. Parent, R.; Marion, M. J.; Furio, L.; Trepo, C.; Petit, M. A. Origin and characterization of a human bipotent liver progenitor cell line Gastroenterology 2004, 126, 1147-56 (Pubitemid 38451185)
27. Hagenbuch, B.; Dawson, P. The sodium bile salt cotransport family SLC10 Pfluegers Arch. 2004, 447, 566-70 (Pubitemid 38241441)
28. Ismair, M. G.; Stieger, B.; Cattori, V.; Hagenbuch, B.; Fried, M.; Meier, P. J.; Kullak-Ublick, G. A. Hepatic uptake of cholecystokinin octapeptide by organic anion-transporting polypeptides OATP4 and OATP8 of rat and human liver Gastroenterology 2001, 121, 1185-90 (Pubitemid 33022099)
29. Yamada, A.; Maeda, K.; Kamiyama, E.; Sugiyama, D.; Kondo, T.; Shiroyanagi, Y.; Nakazawa, H.; Okano, T.; Adachi, M.; Schuetz, J. D.; Adachi, Y.; Hu, Z.; Kusuhara, H.; Sugiyama, Y. Multiple human isoforms of drug transporters contribute to the hepatic and renal transport of olmesartan, a selective antagonist of the angiotensin II AT1-receptor Drug Metab. Dispos. 2007, 35, 2166-76 (Pubitemid 350146202)
30. Chen, C.; Mireles, R. J.; Campbell, S. D.; Lin, J.; Mills, J. B.; Xu, J. J.; Smolarek, T. A. Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1 Drug Metab. Dispos. 2005, 33, 537-46 (Pubitemid 40393197)
31. Gui, C.; Wahlgren, B.; Lushington, G. H.; Hagenbuch, B. Identification, Ki determination and CoMFA analysis of nuclear receptor ligands as competitive inhibitors of OATP1B1-mediated estradiol-17beta-glucuronide transport Pharmacol. Res. 2009, 60, 50-6
32. Hirano, M.; Maeda, K.; Shitara, Y.; Sugiyama, Y. Drug-drug interaction between pitavastatin and various drugs via OATP1B1 Drug Metab. Dispos. 2006, 34, 1229-36
33. Camenisch, G.; Umehara, K. Predicting human hepatic clearance from in vitro drug metabolism and transport data: a scientific and pharmaceutical perspective for assessing drug-drug interactions Biopharm. Drug Dispos. 2012, 33, 179-94