Automated triplexed hepatocyte-based viability and CYP1A and -3A induction assays

Journal of Biomolecular Screening

Volumn 16, Issue 8, 2011, Pages 895-902

  Larson, Brad ^a   Moeller, Timothy ^b   Banks, Peter ^a   Cali, James J ^c  

^a BioTek Instruments   (United States)

^b Celsis In Vitro Technologies   (United States)

^c PROMEGA CORPORATION   (United States)

Author keywords

Automation; Cytochrome P450; Detection; Hepatocytes; Induction; Liquid handling; Luminescence; Multiplexing; Viability

Indexed keywords

3 METHYLCHOLANTHRENE; BETA NAPHTHOFLAVONE; CYTOCHROME P450 1A; CYTOCHROME P450 3A4; DEXAMETHASONE; LANSOPRAZOLE; OMEPRAZOLE; PHENYLBUTAZONE; PREGNANE X RECEPTOR; RIFAMPICIN;

ARTICLE; AUTOMATED TRIPLEX ASSAY; CELL ASSAY; CELL VIABILITY; CONTROLLED STUDY; CYTOTOXICITY; ENZYME ANALYSIS; ENZYME INDUCTION; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; LIVER CELL; LUMINESCENCE; PRIORITY JOURNAL; ROBOTICS;

AUTOMATION, LABORATORY; BIOLOGICAL AGENTS; CELL SURVIVAL; CELLS, CULTURED; CRYOPRESERVATION; CYTOCHROME P-450 CYP1A1; CYTOCHROME P-450 CYP1A2; CYTOCHROME P-450 CYP3A; DRUG EVALUATION, PRECLINICAL; DRUG INTERACTIONS; ENZYME INDUCTION; GENES, REPORTER; HEPATOCYTES; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; KINETICS; LUCIFERASES; REPRODUCIBILITY OF RESULTS;

EID: 80054739532     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057111411482     Document Type: Article

References (20)

1. U. S. Food and Drug Administration. Guidance for Industry: Drug Interaction Studies-Study Design, Data Analysis, and Implications for Dosing and Labeling; U. S. Department of Health and Human Services: Rockville, MD, 2006.
2. Willson, T. M.; Kliewer, S. A. PXR and CAR Drug Metabolism. Nat. Rev. Drug Discov. 2002, 1(4), 259-266.
3. Nebert, D. W.; Dalton, T. P.; Okey, A. B.; Gonzalez, F. J. Role of Aryl Hydrocarbon Receptor-Mediated Induction of the CYP1 Enzymes in Environmental Toxicity and Cancer. J. Biol. Chem. 2004, 279(23), 23847-23850. (Pubitemid 38725238)
4. Roymans, D.; Annaert, P.; Van Houdt, J.; Weygers, A.; Noukens, J.; Sensenhauser, C.; Silva, J.; Van Looveren, C.; Hendrickx, J.; Mannens, G.; et al. Expression and Induction Potential of Cytochromes P450 in Human Cryopreserved Hepatocytes. Drug Metab. Dispos. 2005, 33(7), 1004-1016. (Pubitemid 41002783)
5. Cali, J. J.; Sobol, M.; Ma, D.; Uyeda, H. T.; Meisenheimer, P. CYP3A4 P450-Glo® Assays with Luciferin-IPA: The Most Sensitive and Selective Bioluminescent CYP3A4 Assay. Promega Corporation Web site. http://www.promega. com/resources/articles/pubhub/cellnotes/cyp3a4-p450-gloassays-with-luciferin- ipa-the-most-sensitive-and-selective-bioluminescent-cyp3a4/ (accessed Apr. 15, 2011).
6. Li, A. P. Evaluation of Luciferin-Isopropyl Acetal as a CYP3A4 Substrate for Human Hepatocytes: Effects of Organic Solvents, Cytochrome P450 (P450) Inhibitors, and P450 Inducers. Drug Metab. Dispos. 2009, 37(8), 1598-1603.
7. Zhang, J. H.; Chung, T. D.; Oldenburg, K. R. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. J. Biomol. Screen. 1999, 4(2), 67-73. (Pubitemid 29278954)
8. Li, A. P.; Lu, C.; Brent, J. A.; Pham, C.; Fackett, A.; Ruegg, C. E.; Silber, P. M. Cryopreserved Human Hepatocytes: Characterization of Drug-Metabolizing Enzyme Activities and Applications in Higher Throughput Screening Assays for Hepatotoxicity, Metabolic Stability, and Drug-Drug Interaction Potential. Chem. Biol. Interact. 1999, 121(1), 17-35. (Pubitemid 29240667)
9. Liu, K.; Southall, N.; Titus, S. A.; Inglese, J.; Eskay, R. L.; Shinn, P.; Austin, C. P.; Heilig, M. A.; Zheng, W. A Multiplex Calcium Assay for Identification of GPCR Agonists and Antagonists. Assay Drug Dev. Technol. 2010, 8(3), 367-379.
10. Bjornssen, T. D.; Callaghan, J. T.; Einolf, H. J.; Fischer, V.; Gan, L.; Grimm, S.; Kao, J.; King, S. P.; Miwa, G.; Ni, L.; et al. The Conduct of In Vitro and In Vivo Drug-Drug Interaction Studies: A Pharmaceutical Research and Manufacturers of America (PhRMA) Perspective. Drug Metab. Dispos. 2003, 31(7), 815-832. (Pubitemid 36759050)
11. Bowen, W. P.; Carey, J. E.; Miah, A.; McMurray, H. F.; Munday, P. W.; James, R. S.; Coleman, R. A.; Brown, A. M. Measurement of Cytochrome P450 Gene Induction in Human Hepatocytes Using Quantitative Real-Time Reverse Transcriptase-Polymerase Chain Reaction. Drug Metab. Dispos. 2000, 28(7), 781-788. (Pubitemid 30470828)
12. Ogg, M. S.; Williams, J. M.; Tarbit, M.; Goldfarb, P. S.; Gray, T. J.; Gibson, G. G. A Reporter Gene Assay to Assess the Molecular Mechanisms of Xenobiotic-Dependent Induction of the Human CYP3A4 Gene In Vitro. Xenobiotica 1999, 29(3), 269-279. (Pubitemid 29140096)
13. Ekins, S.; Erickson, J. A. A Pharmacophore for Human Pregnane X Receptor Ligands. Drug Metab. Dispos. 2002, 30(1), 96-99. (Pubitemid 34016946)
14. Lin, J. H.; Lu, A. Y. Interindividual Variability in Inhibition and Induction of Cytochrome P450 Enzymes. Ann. Rev. Pharmacol. 2001, 41, 535-567. (Pubitemid 32385898)
15. Kanebratt, K. P.; Andersson, T. B. HepaRG Cells as an In Vitro Model for Evaluation of Cytochrome P450 Induction in Humans. Drug Metab. Dispos. 2008, 36(1), 137-145.
16. Sahi, J.; Hamilton, G.; Sinz, M.; Barros, S.; Huang, S. M.; Lesko, L. J.; LeCluyse, E. L. Effect of Troglitazone on Cytochrome P450 Enzymes in Primary Cultures of Human and Rat Hepatocytes. Xenobiotica 2000, 30(3), 273-284. (Pubitemid 30179141)
17. Ripp, S. L.; Mills, J. B.; Fahmi, O. A.; Trevena, K. A.; Liras, J. L.; Maurer, T. S.; de Morais, S. M. Use of Immortalized Human Hepatocytes to Predict the Magnitude of Clinical Drug-Drug Interactions Caused by CYP3A4 Induction. Drug Metab. Dispos. 2006, 34(10), 1742-1748. (Pubitemid 44427477)
18. Kajosaari, L. I.; Laitila, J.; Neuvonen, P. J.; Backman, J. T. Metabolism of Repaglinide by CYP2C8 and CYP3A4 In Vitro: Effect of Fibrates and Rifampicin. Basic Clin. Pharmacol. Toxicol. 2005, 97(4), 249-256. (Pubitemid 41433700)
19. Abelö, A.; Andersson, T. B.; Antonsson, M.; Naudot, A. K.; Skânberg, I.; Weidolf, L. Stereoselective Metabolism of Omeprazole by Human Cytochrome P450 Enzymes. Drug Metab. Dispos. 2000, 28(8), 966-972. (Pubitemid 30612617)
20. Pearce, R. E.; Rodrigues, A. D.; Goldstein, J. A.; Parkinson, A. Identification of the Human P450 Enzymes Involved in Lansoprazole Metabolism. J. Pharmacol. Exp. Ther. 1996, 277(2), 805-816. (Pubitemid 27168992)