The HepaRG cell line: a unique in vitro tool for understanding drug metabolism and toxicology in human

Bibliography

• Guo L, Dial S, Shi L, Similarities and differences in the expression of drug-metabolizing enzymes between human hepatic cell lines and primary human hepatocytes. Drug Metab Dispos 2011;39(3):528-38
   PubMed Web of Science ®Google Scholar
• Gripon P, Rumin S, Urban S, Infection of a human hepatoma cell line by hepatitis B virus. Proc Natl Acad Sci USA 2002;99(24):15655-60
   PubMed Web of Science ®Google Scholar
• Hart SN, Li Y, Nakamoto K, A comparison of whole genome gene expression profiles of HepaRG cells and HepG2 cells to primary human hepatocytes and human liver tissues. Drug Metab Dispos 2010;38(6):988-94
   PubMed Web of Science ®Google Scholar
• Turpeinen M, Tolonen A, Chesne C, Functional expression, inhibition and induction of CYP enzymes in HepaRG cells. Toxicol In Vitro 2009;23(4):748-53
   PubMed Web of Science ®Google Scholar
• Aninat C, Piton A, Glaise D, Expression of cytochromes P450, conjugating enzymes and nuclear receptors in human hepatoma HepaRG cells. Drug Metab Dispos 2006;34(1):75-83
   PubMed Web of Science ®Google Scholar
• Rogue A, Lambert C, Spire C, Interindividual variability in gene expression profiles in human hepatocytes and comparison with HepaRG cells. Drug Metab Dispos 2012;40(1):151-8
   PubMedGoogle Scholar
• Cerec V, Glaise D, Garnier D, Transdifferentiation of hepatocyte-like cells from the human hepatoma HepaRG cell line through bipotent progenitor. Hepatology 2007;45(4):957-67
   PubMedGoogle Scholar
• Parent R, Marion MJ, Furio L, Origin and characterization of a human bipotent liver progenitor cell line. Gastroenterology 2004;126(4):1147-56
   PubMed Web of Science ®Google Scholar
• Kanebratt KP, Andersson TB. Evaluation of HepaRG cells as an in vitro model for human drug metabolism studies. Drug Metab Dispos 2008;36(7):1444-52
   PubMed Web of Science ®Google Scholar
• Antherieu S, Chesne C, Li R, Stable expression, activity, and inducibility of cytochromes P450 in differentiated HepaRG cells. Drug Metab Dispos 2010;38(3):516-25
   PubMed Web of Science ®Google Scholar
• Josse R, Aninat C, Glaise D, Long-term functional stability of human HepaRG hepatocytes and use for chronic toxicity and genotoxicity studies. Drug Metab Dispos 2008;36(6):1111-18
   PubMed Web of Science ®Google Scholar
• Mills T, Pilling M, Nicholls G, Affymetrix DMET PLUS genotyping technology: evaluation of cell lines and healthy volunteer samples. ISSX ABSTRACT VOLUME: 9th International Society for the Study of Xenobiotics; 2010
   Google Scholar
• Zanelli U, Caradonna NP, Hallifax D, Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs. Drug Metab Dispos 2012;40(1):104-10
   PubMedGoogle Scholar
• Madec S, Cerec V, Plee-Gautier E, CYP4F3B expression is associated with differentiation of HepaRG human hepatocytes and unaffected by fatty acid overload. Drug Metab Dispos 2011;39(10):1987-96
   PubMedGoogle Scholar
• Antoun J, Amet Y, Simon B, CYP4A11 is repressed by retinoic acid in human liver cells. FEBS Lett 2006;580(14):3361-7
   PubMedGoogle Scholar
• Rogue A, Lambert C, Josse R, Comparative gene expression profiles induced by PPARgamma and PPARalpha/gamma agonists in human hepatocytes. PLoS One 2011;6(4):e18816
   Google Scholar
• Legendre C, Hori T, Loyer P, Drug-metabolising enzymes are down-regulated by hypoxia in differentiated human hepatoma HepaRG cells: HIF-1alpha involvement in CYP3A4 repression. Eur J Cancer 2009;45(16):2882-92
   PubMed Web of Science ®Google Scholar
• International Transporter Consortium. Giacomini KM, Huang SM, Tweedie DJ, Membrane transporters in drug development. Nat Rev Drug Discov 2010;9(3):215-36
   PubMed Web of Science ®Google Scholar
• Swift B, Pfeifer ND, Brouwer KL. Sandwich-cultured hepatocytes: an in vitro model to evaluate hepatobiliary transporter-based drug interactions and hepatotoxicity. Drug Metab Rev 2010;42(3):446-71
   PubMed Web of Science ®Google Scholar
• Le Vee M, Jigorel E, Glaise D, Functional expression of sinusoidal and canalicular hepatic drug transporters in the differentiated human hepatoma HepaRG cell line. Eur J Pharm Sci 2006;28(1-2):109-17
   PubMed Web of Science ®Google Scholar
• Fardel O, Le Vee M. Regulation of human hepatic drug transporter expression by pro-inflammatory cytokines. Expert Opin Drug Metab Toxicol 2009;5(12):1469-81
   PubMed Web of Science ®Google Scholar
• 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(2):217-22
   PubMed Web of Science ®Google Scholar
• Le Vee M, Jouan E, Stieger B, Regulation of drug transporter expression by oncostatin M in human hepatocytes. Biochem Pharmacol 2011;82(3):304-11
   PubMedGoogle Scholar
• Schulze A, Mills K, Weiss TS, Urban S. Hepatocyte polarization is essential for the productive entry of the hepatitis B virus. Hepatology 2012;55(2):373-83
   PubMedGoogle Scholar
• Kanebratt KP, Andersson TB. HepaRG cells as an in vitro model for evaluation of cytochrome P450 induction in humans. Drug Metab Dispos 2008;36(1):137-45
   PubMed Web of Science ®Google Scholar
• McGinnity DF, Zhang G, Kenny JR, Evaluation of multiple in vitro systems for assessment of CYP3A4 induction in drug discovery: human hepatocytes, pregnane X receptor reporter gene, and Fa2N-4 and HepaRG cells. Drug Metab Dispos 2009;37(6):1259-68
   PubMed Web of Science ®Google Scholar
• Kaneko A, Kato M, Endo C, Prediction of clinical CYP3A4 induction using cryopreserved human hepatocytes. Xenobiotica 2010;40(12):791-9
   PubMed Web of Science ®Google Scholar
• Le Vee M, Jouan E, Fardel O. Involvement of aryl hydrocarbon receptor in basal and 2,3,7,8-tetrachlorodibenzo-p-dioxin-induced expression of target genes in primary human hepatocytes. Toxicol In Vitro 2010;24(6):1775-81
   PubMedGoogle Scholar
• Grime K, Ferguson DD, Riley RJ. The use of HepaRG and human hepatocyte data in predicting CYP induction drug-drug interactions via static equation and dynamic mechanistic modelling approaches. Curr Drug Metab 2010;11(10):870-85
   PubMedGoogle Scholar
• McGill MR, Yan HM, Ramachandran A, HepaRG cells: a human model to study mechanisms of acetaminophen hepatotoxicity. Hepatology 2011;53(3):974-82
   PubMed Web of Science ®Google Scholar
• Park BK, Boobis A, Clarke S, Managing the challenge of chemically reactive metabolites in drug development. Nat Rev Drug Discov 2011;10(4):292-306
   PubMed Web of Science ®Google Scholar
• Lee WM. Drug-induced hepatotoxicity. N Engl J Med 2003;349(5):474-85
   PubMed Web of Science ®Google Scholar
• Antherieu S, Rogue A, Fromenty B, Induction of vesicular steatosis by amiodarone and tetracycline is associated with up-regulation of lipogenic genes in HepaRG cells. Hepatology 2011;53(6):1895-905
   PubMed Web of Science ®Google Scholar
• Petit E, Langouet S, Akhdar H, Differential toxic effects of azathioprine, 6-mercaptopurine and 6-thioguanine on human hepatocytes. Toxicol In Vitro 2008;22(3):632-42
   PubMed Web of Science ®Google Scholar
• Dumont J, Josse R, Lambert C, Preferential induction of the AhR gene battery in HepaRG cells after a single or repeated exposure to heterocyclic aromatic amines. Toxicol Appl Pharmacol 2010;249(1):91-100
   PubMed Web of Science ®Google Scholar
• Bazin E, Mourot A, Humpage AR, Fessard V. Genotoxicity of a freshwater cyanotoxin, cylindrospermopsin, in two human cell lines: caco-2 and HepaRG. Environ Mol Mutagen 2010;51(3):251-9
   PubMed Web of Science ®Google Scholar
• Le Hegarat L, Dumont J, Josse R, Assessment of the genotoxic potential of indirect chemical mutagens in HepaRG cells by the comet and the cytokinesis-block micronucleus assays. Mutagenesis 2010;25(6):555-60
   PubMedGoogle Scholar
• Josse R, Dumont J, Fautrel A, Identification of early target genes of aflatoxin B1 in human hepatocytes, inter-individual variability and comparison with other genotoxic compounds. Toxicol Appl Pharmacol 2012;258:176-87
   PubMed Web of Science ®Google Scholar
• Pernelle K, Le Guevel R, Glaise D, Automated detection of hepatotoxic compounds in human hepatocytes using HepaRG cells and image-based analysis of mitochondrial dysfunction with JC-1 dye. Toxicol Appl Pharmacol 2011;254(3):256-66
   PubMedGoogle Scholar
• Gerets HH, Tilmant K, Gerin B, Characterization of primary human hepatocytes, HepG2 cells, and HepaRG cells at the mRNA level and CYP activity in response to inducers and their predictivity for the detection of human hepatotoxins. Cell Biol Toxicol 2012;28:69-87
   PubMed Web of Science ®Google Scholar
• Elliott NT, Yuan F. A microfluidic system for investigation of extravascular transport and cellular uptake of drugs in tumors. Biotechnol Bioeng 2012;109(5):1326-35
   Google Scholar
• Zeilinger K, Schreiter T, Darnell M, Scaling down of a clinical three-dimensional perfusion multicompartment hollow fiber liver bioreactor developed for extracorporeal liver support to an analytical scale device useful for hepatic pharmacological in vitro studies. Tissue Eng C Methods 2011;17(5):549-56
   PubMedGoogle Scholar
• Darnell M, Schreiter T, Zeilinger K, Cytochrome P450-dependent metabolism in HepaRG cells cultured in a dynamic three-dimensional bioreactor. Drug Metab Dispos 2011;39(7):1131-8
   PubMed Web of Science ®Google Scholar
• Hoekstra R, Nibourg GA, van der Hoeven TV, The HepaRG cell line is suitable for bioartificial liver application. Int J Biochem Cell Biol 2011;43(10):1483-9
   PubMedGoogle Scholar
• Jiang L, Li JG, Lan L, Human hepatoma HepaRG cell line engraftment in severe combined immunodeficient x beige mice using mouse-specific anti-fas antibody. Transplant Proc 2010;42(9):3773-8
   PubMedGoogle Scholar