References
- Augustin, E., et al., 2014. CYP3A4-dependent cellular response does not relate to CYP3A4-catalysed metabolites of C-1748 and C-1305 acridine antitumor agents in HepG2 cells. Cell Biology International, 38 (11), 1291–1303.
- Ayajiki, K., et al., 2003. Mediation of arachidonic acid metabolite(s) produced by endothelial cytochrome P-450 3A4 in monkey arterial relaxation. Hypertension Research, 26 (3), 237–243.
- Dambach, D.M., Andrews, B.A., and Moulin, F., 2005. New technologies and screening strategies for hepatotoxicity: use of in vitro models. Toxicologic Pathology, 33 (1), 17–26.
- Donato, M.T., et al., 2004. Fluorescence-based assays for screening nine cytochrome P450 (P450) activities in intact cells expressing individual human P450 enzymes. Drug Metabolism and Disposition, 32 (7), 699–706.
- Du, Y., et al., 2014. Human hepatocytes with drug metabolic function induced from fibroblasts by lineage reprogramming. Cell Stem Cell, 14 (3), 394–403.
- Gomez.-Lechon., M.J., Tolosa, L., and Donato.M.T., 2014. Cell-based models to predict human hepatotoxicity of drugs. Revista de Toxicologia, 31, 149–156.
- Gómez-Lechón, M.J., Tolosa, L., and Donato, M.T., 2016. Metabolic activation and drug-induced liver injury: In vitro approaches for the safety risk assessment of new drugs. Journal of Applied Toxicology, 36 (6), 752–768.
- Greer, M.L., et al., 2010. Cell based approaches for evaluation of drug-induced liver injury. Toxicology, 268 (3), 125–131.
- Grimm, S.W., et al., 1994. Catalytic selectivity and mechanism-based inactivation of stably expressed and hepatic cytochromes P450 2B4 and 2B5: implications of the cytochrome P450 2B5 polymorphism. Molecular Pharmacology, 46, 1090–1099.
- Guillén, M.I., et al., 1998. Oncostatin M down-regulates basal and induced cytochromes P450 in human hepatocytes. The Journal of Pharmacology and Experimental Therapeutics, 285 (1), 127–134.
- Gunness, P., et al., 2013. 3D organotypic cultures of human heparg cells: a tool for in vitro toxicity studies. Toxicological Sciences, 133 (1), 67–78.
- Gupta, R.P., et al., 2004. CYP3A4 is a human microsomal vitamin D 25-hydroxylase. Journal of Bone and Mineral Research, 19 (4), 680–688.
- Gustafsson, F., et al., 2014. A correlation between the in vitro drug toxicity of drugs to cell lines that express human p450s and their propensity to cause liver injury in humans. Toxicological Sciences, 137 (1), 189–211.
- Hashizume, T., et al., 2010. Advantages of human hepatocyte-derived transformants expressing a series of human cytochrome P450 isoforms for genotoxicity examination. Toxicological Sciences, 116 (2), 488–497.
- Hosomi, H., et al., 2011. Development of a highly sensitive cytotoxicity assay system for CYP3A4-mediated metabolic activation. Drug Metabolism and Disposition, 39 (8), 1388–1395.
- Hughes, J.P., et al., 2011. Principles of early drug discovery. British Journal of Pharmacology, 162 (6), 1239–1249.
- Laemmli, U.K., 1970. Cleavage of structural proteins during the assembly of the head of bacteriophage T4. Nature, 227 (5259), 680–685.
- Liebmann, J.E., et al., 1993. Cytotoxic studies of pacfitaxel (Taxol®) in human tumour cell lines. British Journal of Cancer, 68 (6), 1104–1109.
- Liu, Y., et al., 2015. Evaluation of CYP3A4 inhibition and hepatotoxicity using DMSO-treated human hepatoma HuH-7 cells. Cell Biology and Toxicology, 31 (4–5), 221–230.
- Mohedas, A.H., et al., 2014. Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. Journal of Medicinal Chemistry, 57 (19), 7900–7915.
- Mohedas, A.H., et al., 2013. Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chemical Biology, 8 (6), 1291–1302.
- Murayama, N., et al., 2001. Expression of CYP2A6 in tumor cells augments cellular sensitivity to Tegafur. Japanese Journal of Cancer Research, 92 (5), 524–528.
- O’Brien, P.J., et al., 2006. High concordance of drug-induced human hepatotoxicity with in vitro cytotoxicity measured in a novel cell-based model using high content screening. Archives of Toxicology, 80 (9), 580–604.
- Oguro, A., et al., 2011. Overexpression of CYP3A4, but not of CYP2D6, promotes hypoxic response and cell growth of Hep3B cells. Drug Metabolism and Pharmacokinetics, 26 (4), 407–415.
- Oscarson, M., et al., 2002. Characterization of a novelCYP2A7/CYP2A6 hybrid allele (CYP2A6*12) that causes reduced CYP2A6 activity. Human Mutation, 20 (4), 275–283.
- Ott, L.M., Ramachandran, K., and Stehno-Bittel, L., 2017. An Automated multiplexed hepatotoxicity and CYP induction assay using HepaRG cells in 2D and 3D. SLAS Discovery, 22 (5), 614–625.
- Park, K., et al., 2005. Investigation of toxic metabolites during drug development. Toxicology and Applied Pharmacology, 207 (2), 425–434.
- Potente, M., et al., 2002. Cytochrome P450 2C9-induced endothelial cell proliferation involves induction of mitogen-activated protein (MAP) kinase phosphatase-1, inhibition of the c-Jun N-terminal kinase, and up-regulation of cyclin D1. Journal of Biological Chemistry, 277 (18), 15671–15676.
- Rana, P., et al., 2016. Development of a cell viability assay to assess drug metabolite structure–toxicity relationships. Bioorganic and Medicinal Chemistry Letters, 26 (16), 4003–4006.
- Renwick, A.B., et al., 2001. Metabolism of 2,5-bis(trifluoromethyl)-7-benzyloxy-4-trifluoromethylcoumarin by human hepatic CYP isoforms: evidence for selectivity towards CYP3A4. Xenobiotica, 31 (4), 187–204.
- Scannell, J.W. and Bosley, J., 2016. When quality beats quantity: decision theory, drug discovery, and the reproducibility crisis. PLoS ONE, 11 (2), 1–21.
- Sison-Young, R.L., et al., 2017. A multicenter assessment of single-cell models aligned to standard measures of cell health for prediction of acute hepatotoxicity. Archives of Toxicology, 91 (3), 1385–1400.
- Sridar, C., et al., 2008. Differential inhibition of cytochromes P450 3A4 and 3A5 by the newly synthesized coumarin derivatives 7-coumarin propargyl ether and 7-(4-trifluoromethyl)coumarin propargyl ether. Drug Metabolism and Disposition, 36 (11), 2234–2243.
- Thuy Phuong, N.T., et al., 2017. Role of the CYP3A4-mediated 11,12-epoxyeicosatrienoic acid pathway in the development of tamoxifen-resistant breast cancer. Oncotarget, 8 (41), 71054–71069.
- Tolosa, L., et al., 2016. Advantageous use of HepaRG cells for the screening and mechanistic study of drug-induced steatosis. Toxicology and Applied Pharmacology, 302, 1–9.
- Tolosa, L., et al., 2017. Customised in vitro model to detect human metabolism-dependent idiosyncratic drug-induced liver injury. Archives of Toxicology, 92 (1), 383399.
- Tomida, T., et al., 2015. Multiparametric assay using HepaRG cells for predicting drug-induced liver injury. Toxicology Letters, 236 (1), 16–24.
- Towbin, H., Staehelin, T., and Gordon, J., 1979. Electrophoretic transfer of proteins from polyacrylamide gels to nitrocellulose sheets: procedure and some applications. Proceedings of the National Academy of Sciences of the United States of America, 76 (9), 4350–4354.
- Trottier, Y., Waithe, W.I., and Anderson, A., 1992. The detection of promutagen activation by extracts of cells expressing cytochrome P450IA2 cDNA: preincubation dramatically increases revertant yield in the Ames test. Mutation Research, 281 (1), 39–45.
- Valeriote, F. and Putten, L.V., 1975. Proliferation-dependent cytotoxicity of anticancer agents: a review. Cancer Research, 35 (10), 2619–2630.
- Wang, J. and Urban, L., 2004. The impact of early ADME profiling on drug discovery and development strategy. Drug Discovery World, 73–86.
- Wang, X., et al., 2015. Probing mechanisms of CYP3A time-dependent inhibition using a truncated model system. ACS Medicinal Chemistry Letters, 6 (8), 925–929.