Induction of cytochromes P450

Current Topics in Medicinal Chemistry

Volumn 4, Issue 16, 2004, Pages 1745-1766

  Dickins, Maurice ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; AROMATIC HYDROCARBON RECEPTOR; CALCIUM CHANNEL BLOCKING AGENT; CELL NUCLEUS RECEPTOR; CLOTRIMAZOLE; CYTOCHROME P450; CYTOCHROME P450 1A; CYTOCHROME P450 1A1; CYTOCHROME P450 1A2; CYTOCHROME P450 2B; CYTOCHROME P450 3A; CYTOCHROME P450 4A; ENZYME INDUCING AGENT; GLUCOCORTICOID RECEPTOR; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; MACROLIDE; MESSENGER RNA; MEVINOLIN; MIFEPRISTONE; NIFEDIPINE; PACLITAXEL; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; PHENOBARBITAL; PREGNANE X RECEPTOR; PROTEINASE INHIBITOR; RIFAMPICIN; RNA DIRECTED DNA POLYMERASE INHIBITOR; TRANSCRIPTION FACTOR; TROGLITAZONE; UNINDEXED DRUG;

CELL CULTURE; CELL LINE; CRYSTAL STRUCTURE; DRUG MECHANISM; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG STRUCTURE; ENZYME INDUCTION; ENZYME REGULATION; ENZYME STRUCTURE; EX VIVO STUDY; GENETIC TRANSFECTION; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; IMMUNOBLOTTING; IN VITRO STUDY; LIGAND BINDING; LIVER CELL; LIVER FAILURE; LIVER TOXICITY; MOLECULAR DYNAMICS; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PHYSICAL CHEMISTRY; PROTEIN EXPRESSION; REPORTER GENE; REVIEW; SENSITIVITY AND SPECIFICITY; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION;

ANIMALS; CYTOCHROME P-450 ENZYME SYSTEM; ENZYME INDUCTION; ENZYME INHIBITORS; GENE EXPRESSION REGULATION, ENZYMOLOGIC; HUMANS; PROTEIN CONFORMATION; RECEPTOR CROSS-TALK; RECEPTORS, CYTOPLASMIC AND NUCLEAR; SIGNAL TRANSDUCTION;

EID: 10644271665     PISSN: 15680266     EISSN: None     Source Type: Journal    
DOI: 10.2174/1568026043387115     Document Type: Review

References (171)

1. Conney, A. H. Pharmacological Implications of Microsomal Enzyme Induction. Pharmacol. Rev. 1967, 19, 317-366.
2. Poland, A.; Glover, E.; Kende, A. S. Stereospecific, High Affinity Binding of 2,3,7,8-Tetrachlorodibenzo-p-Dioxin by Hepatic Cytosol. Evidence That the Binding Species Is Receptor for Induction of Aryl Hydrocarbon Hydroxylase. J. Biol. Chem. 1976, 251, 4936-4946.
3. Nebert, D. W.; Eisen, H. J.; Negishi, M.; Lang, M. A.; Hjelmeland, L. M.; Okey, A. B. Genetic Mechanisms Controlling the Induction of Polysubstrate Monooxygenase (P-450) Activities. Annu. Rev. Pharmacol. Toxicol. 1981, 21, 431-462.
4. Waxman, D. J. P450 Gene Induction by Structurally Diverse Xenochemicals: Central Role of Nuclear Receptors CAR, PXR, and PPAR. Arch. Biochem. Biophys. 1999, 369, 11-23.
5. Savas, U.; Griffin, K. J.; Johnson, E. F. Molecular Mechanisms of Cytochrome P-450 Induction by Xenobiotics: An Expanded Role for Nuclear Hormone Receptors. Mol. Pharmacol. 1999, 56 851-857.
6. Waxman, D. J.; Azaroff, L. Phenobarbital Induction of Cytochrome P-450 Gene Expression. Biochem. J. 1992, 281 (Pt 3), 577-592.
7. Issemann, I.; Green, S. Activation of a Member of the Steroid Hormone Receptor Superfamily by Peroxisome Proliferators. Nature 1990, 347, 645-650.
8. Honkakoski, R; Negishi, M. Regulation of Cytochrome P450 (CYP) Genes by Nuclear Receptors. Biochem. J. 2000, 347 321-337.
9. Jones, S. A.; Moore, L. B.; Shenk, J. L.; Wisely, G. B.; Hamilton, G. A.; McKee, D. D.; Tomkinson, N. C.; LeCluyse, E. L.; Lambert, M. H.; Willson, T. M.; Kliewer, S. A.; Moore, J. T. The Pregnane X Receptor: A Promiscuous Xenobiotic Receptor That Has Diverged During Evolution. Mol. Endocrinol. 2000, 14, 27-39.
10. Guengerich, F. P. Cytochrome P-450 3A4: Regulation and Role in Drug Metabolism. Annu. Rev. Pharmacol. Toxicol. 1999, 39, 1-17.
11. Quattrochi, L. C.; Guzelian, P. S. CYP3A Regulation: From Pharmacology to Nuclear Receptors. Drug Metab. Dispos. 2001, 29, 615-622.
12. Roberts, B. J.; Song, B. J.; Soh, Y.; Park, S. S.; Shoaf, S. E. Ethanol Induces CYP2E1 by Protein Stabilization. Role of Ubiquitin Conjugation in the Rapid Degradation of CYP2E1. J. Biol. Chem. 1995, 270, 29632-29635.
13. Laudet, V. A., J.; Gustafsson, J-A.; Wahli, W. A Unified Nomenclature System for the Nuclear Receptor Superfamily. Cell 1999, 97, 161-163.
14. Moore, L. B.; Parks, D. J.; Jones, S. A.; Bledsoe, R. K.; Consler, T. G.; Stimmel, J. B.; Goodwin, B.; Liddle, C.; Blanchard, S. G.; Willson, T. M.; Collins, J. L.; Kliewer, S. A. Orphan Nuclear Receptors Constitutive Androstane Receptor and Pregnane X Receptor Share Xenobiotic and Steroid Ligands. J. Biol. Chem. 2000, 275 15122-15127.
15. Moore, J. T.; Kliewer, S. A. Use of the Nuclear Receptor PXR to Predict Drug Interactions. Toxicology 2000, 153, 1-10.
16. Sugatani, J.; Kojima, H.; Ueda, A.; Kakizaki, S.; Yoshinari, K.; Gong, Q. H.; Owens, I. S.; Negishi, M.; Sueyoshi, T. The Phenobarbital Response Enhancer Module in the Human Bilirubin UDP-Glucuronosyltransferase UGT1A1 Gene and Regulation by the Nuclear Receptor CAR. Hepatology 2001, 33, 1232-1238.
17. Synold, T. W.; Dussault, I.; Forman, B. M. The Orphan Nuclear Receptor SXR Coordinately Regulates Drug Metabolism and Efflux. Nat. Med. 2001, 7, 584-590.
18. Blumberg, B.; Sabbagh, W., Jr.; Juguilon, H.; Bolado, J., Jr.; van Meter, C. M.; Ong, E. S.; Evans, R. M. SXR, a Novel Steroid and Xenobiotic-Sensing Nuclear Receptor. Genes Dev. 1998, 12 3195-3205.
19. Bertilsson, G.; Heidrich, J.; Svensson, K.; Asman, M.; Jendeberg, L.; Sydow-Backman, M.; Ohlsson, R.; Postlind, H.; Blomquist, P.; Berkenstam, A. Identification of a Human Nuclear Receptor Defines a New Signaling Pathway for CYP3A Induction. Proc. Natl. Acad. Sci. U. S. A. 1998, 95, 12208-12213.
20. Lehmann, J. M.; McKee, D. D.; Watson, M. A.; Willson, T. M.; Moore, J. T.; Kliewer, S. A. The Human Orphan Nuclear Receptor PXR Is Activated by Compounds That Regulate CYP3A4 Gene Expression and Cause Drug Interactions. J. Clin. Invest. 1998, 102, 1016-1023.
21. Kliewer, S. A.; Moore, J. T.; Wade, L.; Staudinger, J. L.; Watson, M. A.; Jones, S. A.; McKee, D. D.; Oliver, B. B.; Willson, T. M.; Zetterstrom, R. H.; Perlmann, T.; Lehmann, J. M. An Orphan Nuclear Receptor Activated by Pregnanes Defines a Novel Steroid Signaling Pathway. Cell 1998, 92, 73-82.
22. Staudinger, J.; Liu, Y.; Madan, A.; Habeebu, S.; Klaassen, C. D. Coordinate Regulation of Xenobiotic and Bile Acid Homeostasis by Pregnane X Receptor. Drug Metab. Dispos. 2001, 29, 1467-1472.
23. Staudinger, J. L.; Goodwin, B.; Jones, S. A.; Hawkins-Brown, D.; MacKenzie, K. I.; LaTour, A.; Liu, Y.; Klaassen, C. D.; Brown, K. K.; Reinhard, J.; Willson, T. M.; Koller, B. H.; Kliewer, S. A. The Nuclear Receptor PXR Is a Lithocholic Acid Sensor That Protects against Liver Toxicity. Proc. Natl. Acad. Sci. U. S. A. 2001, 98, 3369-3374.
24. Kocarek, T. A.; Schuetz, E. G.; Strom, S. C.; Fisher, R. A.; Guzelian, P. S. Comparative Analysis of Cytochrome P4503A Induction in Primary Cultures of Rat, Rabbit, and Human Hepatocytes. Drug Metab. Dispos. 1995, 23, 415-421.
25. Zhang, H.; LeCluyse, E.; Liu, L.; Hu, M.; Matoney, L.; Zhu, W.; Yan, B. Rat Pregnane X Receptor: Molecular Cloning, Tissue Distribution, and Xenobiotic Regulation. Arch. Biochem. Biophys. 1999, 368, 14-22.
26. Moore, J. T.; Moore, L. B.; Maglich, J. M.; Kliewer, S. A. Functional and Structural Comparison of PXR and CAR. Biochim. Biophys. Acta 2003, 1619, 235-238.
27. Zhang, J.; Kuehl, P.; Green, E. D.; Touchman, J. W.; Watkins, P. B.; Daly, A.; Hall, S. D.; Maurel, P.; Relling, M.; Brimer, C.; Yasuda, K.; Wrighton, S. A.; Hancock, M.; Kim, R. B.; Strom, S.; Thummel, K.; Russell, C. G.; Hudson, J. R., Jr.; Schuetz, E. G.; Boguski, M. S. The Human Pregnane X Receptor: Genomic Structure and Identification and Functional Characterization of Natural Allelic Variants. Pharmacogenetics 2001, 11, 555-572.
28. Hustert, E.; Zibat, A.; Presecan-Siedel, E.; Eiselt, R.; Mueller, R.; Fuss, C.; Brehm, I.; Brinkmann, U.; Eichelbaum, M.; Wojnowski, L.; Burk, O. Natural Protein Variants of Pregnane X Receptor with Altered Transactivation Activity toward CYP3A4. Drug Metab. Dispos. 2001, 29, 1454-1459.
29. Trottier, E.; Belzil, A.; Stoltz, C.; Anderson, A. Localization of a Phenobarbital-Responsive Element (PBRE) in the 5′-Flanking Region of the Rat CYP2B2 Gene. Gene 1995, 158, 263-268.
30. Honkakoski, P.; Negishi, M. Characterization of a Phenobarbital-Responsive Enhancer Module in Mouse P450 Cyp2b10 Gene. J. Biol. Chem. 1997, 272, 14943-14949.
31. Sueyoshi, T.; Kawamoto, T.; Zelko, I.; Honkakoski, P.; Negishi, M. The Repressed Nuclear Receptor CAR Responds to Phenobarbital in Activating the Human CYP2B6 Gene. J. Biol. Chem. 1999, 274, 6043-6046.
32. Negishi, M.; Honkakoski, P. Induction of Drug Metabolism by Nuclear Receptor CAR: Molecular Mechanisms and Implications for Drug Research. Eur. J. Pharm. Sci. 2000, 11, 259-264.
33. Ueda, A.; Hamadeh, H. K.; Webb, H. K.; Yamamoto, Y.; Sueyoshi, T.; Afshari, C. A.; Lehmann, J. M.; Negishi, M. Diverse Roles of the Nuclear Orphan Receptor CAR in Regulating Hepatic Genes in Response to Phenobarbital. Mol. Pharmacol. 2002, 61, 1-6.
34. Honkakoski, P.; Negishi, M. Protein Serine/Threonine Phosphatase Inhibitors Suppress Phenobarbital-Induced Cyp2b10 Gene Transcription in Mouse Primary Hepatocytes. Biochem. J. 1998, 330 (Pt 2), 889-895.
35. Kawamoto, T.; Sueyoshi, T.; Zelko, I.; Moore, R.; Washburn, K.; Negishi, M. Phenobarbital-Responsive Nuclear Translocation of the Receptor CAR in Induction of the CYP2B Gene. Mol. Cell. Biol. 1999, 19, 6318-6322.
36. Forman, B. M.; Tzameli, I.; Choi, H. S.; Chen, J.; Simha, D.; Seol, W.; Evans, R. M.; Moore, D. D. Androstane Metabolites Bind to and Deactivate the Nuclear Receptor CAR-Beta. Nature 1998, 395 612-615.
37. Wang, H.; Negishi, M. Transcriptional Regulation of Cytochrome P450 2B Genes by Nuclear Receptors. Curr Drug Metab 2003, 4, 515-525.
38. Maglich, J. M.; Parks, D. J.; Moore, L. B.; Collins, J. L.; Goodwin, B.; Billin, A. N.; Stoltz, C. A.; Kliewer, S. A.; Lambert, M. H.: Willson, T. M.; Moore, J. T. Identification of a Novel Human Constitutive Androstane Receptor (CAR) Agonist and Its Use in the Identification of CAR Target Genes. J. Biol. Chem. 2003, 278, 17277-17283.
39. Wei, P.; Zhang, J.; Egan-Hafley, M.; Liang, S.; Moore, D. D. The Nuclear Receptor CAR Mediates Specific Xenobiotic Induction of Drug Metabolism. Nature 2000, 407, 920-923.
40. Wei, P.; Zhang, J.; Dowhan, D. H.; Han, Y.; Moore, D. D. Specific and Overlapping Functions of the Nuclear Hormone Receptors CAR and PXR in Xenobiotic Response. Pharmacogenomics J 2002, 2 117-126.
41. Pascussi, J. M.; Drocourt, L.; Fabre, J. M.; Maurel, P.; Vilarem, M. J. Dexamethasone Induces Pregnane X Receptor and Retinoid X Receptor-Alpha Expression in Human Hepatocytes: Synergistic Increase of CYP3A4 Induction by Pregnane X Receptor Activators. Mol. Pharmacol. 2000, 58, 361-372.
42. Pascussi, J. M.; Drocourt, L.; Gerbal-Chaloin, S.; Fabre, J. M.; Maurel, P.; Vilarem, M. J. Dual Effect of Dexamethasone on CYP3A4 Gene Expression in Human Hepatocytes. Sequential Role of Glucocorticoid Receptor and Pregnane X Receptor. Eur. J. Biochem. 2001, 268, 6346-6358.
43. Gerbal-Chaloin, S.; Daujat, M.; Pascussi, J. M.; Pichard-Garcia, L.; Vilarem, M. J.; Maurel, P. Transcriptional Regulation of CYP2C9 Gene. Role of Glucocorticoid Receptor and Constitutive Androstane Receptor. J. Biol. Chem. 2002, 277, 209-217.
44. Peters, J. M.; Cattley, R. C.; Gonzalez, F. J. Role of PPAR Alpha in the Mechanism of Action of the Nongenotoxic Carcinogen and Peroxisome Proliferator Wy-14,643. Carcinogenesis 1997, 18 2029-2033.
45. Gonzalez, F. J.; Fernandez-Salguero, P.; Lee, S. S.; Pineau, T.; Ward, J. M. Xenobiotic Receptor Knockout Mice. Toxicol. Lett. 1995, 82-83, 117-121.
46. Luo, G.; Cunningham, M.; Kim, S.; Burn, T.; Lin, J.; Sinz, M.; Hamilton, G.; Rizzo, C.; Jolley, S.; Gilbert, D.; Downey, A.; Mudra, D.; Graham, R.; Carroll, K.; Xie, J.; Madan, A.; Parkinson, A.; Christ, D.; Selling, B.; LeCluyse, E.; Gan, L. S. CYP3A4 Induction by Drugs: Correlation between a Pregnane X Receptor Reporter Gene Assay and CYP3A4 Expression in Human Hepatocytes. Drug Metab. Dispos. 2002, 30, 795-804.
47. El-Sankary, W.; Plant, N. J.; Gibson, G. G.; Moore, D. J. Regulation of the CYP3A4 Gene by Hydrocortisone and Xenobiotics: Role of the Glucocorticoid and Pregnane X Receptors. Drug Metab. Dispos. 2000, 28, 493-496.
48. Schuetz, E. G.; Schmid, W.; Schutz, G.; Brimer, C.; Yasuda, K.; Kamataki, T.; Bornheim, L.; Myles, K.; Cole, T. J. The Glucocorticoid Receptor Is Essential for Induction of Cytochrome P-4502B by Steroids but Not for Drug or Steroid Induction of CYP3A or P-450 Reductase in Mouse Liver. Drug Metab. Dispos. 2000, 28, 268-278.
49. Wang, H.; Faucette, S. R.; Gilbert, D.; Jolley, S. L.; Sueyoshi, T.; Negishi, M.; LeCluyse, E. L. Glucocorticoid Receptor Enhancement of Pregnane X Receptor-Mediated CYP2B6 Regulation in Primary Human Hepatocytes. Drug Metab. Dispos. 2003, 31, 620-630.
50. Bell, A. R.; Savory, R.; Horley, N. J.; Choudhury, A. I.; Dickins, M.; Gray, T. J.; Salter, A. M.; Bell, D. R. Molecular Basis of Non-Responsiveness to Peroxisome Prolifierators: The Guinea-Pig PPARalpha Is Functional and Mediates Peroxisome Proliferator-Induced Hypolipidaemia. Biochem. J. 1998, 332 (Pt 3), 689-693.
51. Palmer, C. N.; Hsu, M. H.; Griffin, K. J.; Raucy, J. L.; Johnson, E. F. Peroxisome Proliferator Activated Receptor-Alpha Expression in Human Liver. Mol. Pharmacol. 1998, 53, 14-22.
52. Richert, L.; Lamboley, C.; Viollon-Abadie, C.; Grass, P.; Hartmann, N.; Laurent, S.; Heyd, B.; Mantion, G.; Chibout, S. D.; Staedtler, F. Effects of Clofibric Acid on mRNA Expression Profiles in Primary Cultures of Rat, Mouse and Human Hepatocytes. Toxicol. Appl. Pharmacol. 2003, 191, 130-146.
53. Ramachandran, V.; Kostrubsky, V. E.; Komoroski, B. J.; Zhang, S.; Dorko, K.; Esplen, J. E.; Strom, S. C.; Venkataramanan, R. Troglitazone Increases Cytochrome P-450 3A Protein and Activity in Primary Cultures of Human Hepatocytes. Drug Metab. Dispos. 1999 27, 1194-1199.
54. Sahi, J.; Black, C. B.; Hamilton, G. A.; Zheng, X; Jolley, S.; Rose, K. A.; Gilbert, D.; LeCluyse, E. L.; Sinz, M. W. Comparative Effects of Thiazolidinediones on in Vitro P450 Enzyme Induction and Inhibition. Drug Metab. Dispos. 2003, 31, 439-446.
55. Wan, Y. J.; An, D.; Cai, Y.; Repa, J. J.; Hung-Po Chen, T.; Flores, M.; Postic, C.; Magnuson, M. A.; Chen, J.; Chien, K. R.; French, S.; Mangelsdorf, D. J.; Sucov, H. M. Hepatocyte-Specific Mutation Establishes Retinoid X Receptor Alpha as a Heterodimeric Integrator of Multiple Physiological Processes in the Liver. Mol. Cell. Biol. 2000, 20, 4436-4444.
56. LeCluyse, E. L. Human Hepatocyte Culture Systems for the in Vitro Evaluation of Cytochrome P450 Expression and Regulation Eur. J. Pharm. Sci. 2001, 13, 343-368.
57. Goodwin, B.; Moore, L. B.; Stoltz, C. M.; McKee, D. D.; Kliewer, S. A. Regulation of the Human CYP2B6 Gene by the Nuclear Pregnane X Receptor. Mol. Pharmacol. 2001, 60, 427-431.
58. Xie, W.; Barwick, J. L.; Simon, C. M.; Pierce, A. M.; Safe, S.; Blumberg, B.; Guzelian, P. S.; Evans, R. M. Reciprocal Activation of Xenobiotic Response Genes by Nuclear Receptors SXR/PXR and CAR. Genes Dev. 2000, 14, 3014-3023.
59. Smirlis, D.; Muangmoonchai, R.; Edwards, M.; Phillips, I. R.; Shephard, E. A. Orphan Receptor Promiscuity in the Induction of Cytochromes P450 by Xenobiotics. J. Biol. Chem. 2001, 276 12822-12826.
60. Xie, W.; Evans, R. M. Orphan Nuclear Receptors: The Exotics of Xenobiotics. J. Biol. Chem. 2001, 276, 37739-37742.
61. Geick, A.; Eichelbaum, M.; Burk, O. Nuclear Receptor Response Elements Mediate Induction of Intestinal MDR1 by Rifampin. J. Biol. Chem. 2001, 276, 14581-14587.
62. LeCluyse, E.; Madan, A.; Hamilton, G.; Carroll, K.; DeHaan, R.; Parkinson, A. Expression and Regulation of Cytochrome P450 Enzymes in Primary Cultures of Human Hepatocytes. J. Biochem. Mol. Toxicol. 2000, 14, 177-188.
63. Gerbal-Chaloin, S.; Pascussi, J. M.; Pichard-Garcia, L.; Daujat, M.; Waechter, F.; Fabre, J. M.; Carrere, N.; Maurel, P. Induction of CYP2C Genes in Human Hepatocytes in Primary Culture Drug Metab. Dispos. 2001, 29, 242-251.
64. Drocourt, L.; Pascussi, J. M.; Assenat, E.; Fabre, J. M.; Maurel, P.; Vilarem, M. J. Calcium Channel Modulators of the Dihydropyridine Family Are Human Pregnane X Receptor Activators and Inducers of CYP3A, CYP2B, and CYP2C in Human Hepatocytes. Drug Metab. Dispos. 2001, 29, 1325-1331.
65. Rae, J. M.; Johnson, M. D.; Lippman, M. E.; Flockhart, D. A. Rifampin Is a Selective, Pleiotropic Inducer of Drug Metabolism Genes in Human Hepatocytes: Studies with eDNA and Oligonucleotide Expression Arrays. J. Pharmacol. Exp. Ther. 2001, 299, 849-857.
66. Xie, W.; Yeuh, M. F.; Radominska-Pandya, A.; Saini, S. P.; Negishi, Y.; Bottroff, B. S.; Cabrera, G. Y.; Tukey, R. H.; Evans, R. M. Control of Steroid, Heme, and Carcinogen Metabolism by Nuclear Pregnane X Receptor and Constitutive Androstane Receptor. Proc. Natl. Acad. Sci. U. S. A. 2003, 100, 4150-4155.
67. Huang, W.; Zhang, J.; Chua, S. S.; Qatanani, M.; Han, Y.; Granata, R.; Moore, D. D. Induction of Bilirubin Clearance by the Constitutive Androstane Receptor (CAR) Proc. Natl. Acad. Sci. U. S. A. 2003, 100, 4156-4161.
68. Dussault, I.; Lin, M.; Hollister, K.; Wang, E. H.; Synold, T. W.; Forman, B. M. Peptide Mimetic HIV Protease Inhibitors Are Ligands for the Orphan Receptor SXR. J. Biol. Chem. 2001, 276, 33309-33312.
69. Kast, H. R.; Goodwin, B.; Tarr, P. T.; Jones, S. A.; Anisfeld, A. M.; Stoltz, C. M.; Tontonoz, P.; Kliewer, S.; Willson, T. M.; Edwards, P. A. Regulation of Multidrug Resistance-Associated Protein 2 (ABCC2) by the Nuclear Receptors Pregnane X Receptor, Farnesoid X-Activated Receptor, and Constitutive Androstane Receptor. J. Biol. Chem. 2002, 277, 2908-2915.
70. Watkins, R. E.; Wisely, G. B.; Moore, L. B.; Collins, J. L.; Lambert, M. H.; Williams, S. P.; Willson, T. M.; Kliewer, S. A.; Redinbo, M. R. The Human Nuclear Xenobiotic Receptor PXR: Structural Determinants of Directed Promiscuity. Science 2001, 292, 2329-2333.
71. Xu, H. E.; Lambert, M. H.; Montana, V. G.; Plunket, K. D.; Moore, L. B.; Collins, J. L.; Oplinger, J. A.; Kliewer, S. A.; Gampe, R. T., Jr.; McKee, D. D.; Moore, J. T.; Willson, T. M. Structural Determinants of Ligand Binding Selectivity between the Peroxisome Proliferator-Activated Receptors. Proc. Natl. Acad. Sci. U S. A. 2001, 98, 13919-13924.
72. Xiao, L.; Cui, X.; Madison, V.; White, R. E.; Cheng, K. C. Insights from a Three-Dimensional Model into Ligand Binding to Constitutive Active Receptor. Drug Metab. Dispos. 2002, 30 951-956.
73. Watkins, R. E.; Maglich, J. M.; Moore, L. B.; Wisely, G. B.; Noble, S. M.; Davis-Searles, P. R.; Lambert, M. H.; Kliewer, S. A.; Redinbo, M. R. 2.1 a Crystal Structure of Human PXR in Complex with the St. John's Wort Compound Hyperforin. Biochemistry (Mosc). 2003 42, 1430-1438.
74. Willson, T. M.; Kliewer, S. A. PXR, CAR and Drug Metabolism. Nat Rev Drug Discov 2002, 1, 259-266.
75. Watkins, R. E.; Davis-Searles, P. R.; Lambert, M. H.; Redinbo, M. R. Coactivator Binding Promotes the Specific Interaction between Ligand and the Pregnane X Receptor. J. Mol. Biol. 2003 331, 815-828.
76. Gillam, E. M. The PXR Ligand-Binding Domain: How to Be Picky and Promiscuous at the Same Time. Trends Pharmacol. Sci. 2001 22, 448.
77. Masimirembwa, C. M.; Thompson, R.; Andersson, T. B. In Vitro High Throughput Screening of Compounds for Favorable Metabolic Properties in Drug Discovery. Comb Chem High Throughput Screen 2001, 4, 245-263.
78. Amacher, D. E.; Schomaker, S. J.; Burkhardt, J. E. The Relationship among Microsomal Enzyme Induction, Liver Weight and Histological Change in Rat Toxicology Studies .Food Chem. Toxicol. 1998, 36, 831-839.
79. Lock, E. A.; Mitchell, A. M.; Elcombe, C. R. Biochemical Mechanisms of Induction of Hepatic Peroxisome Proliferation .Annu. Rev. Pharmacol. Toxicol. 1989, 29, 145-163.
80. Viollon-Abadie, C.; Lassere, D.; Debruyne, E.; Nicod, L.; Carmichael, N.; Richert, L. Phenobarbital, Beta-Naphthoflavone, Clofibrate, and Pregnenolone-16alpha-Carbonitrile Do Not Affect Hepatic Thyroid Hormone UDP-Glucuronosyl Transferase Activity, and Thyroid Gland Function in Mice. Toxicol. Appl. Pharmacol. 1999, 155, 1-12.
81. Madan, A.; DeHaan, R.; Mudra, D.; Carroll, K.; LeCluyse, E.; Parkinson, A. Effect of Cryopreservation on Cytochrome P-450 Enzyme Induction in Cultured Rat Hepatocytes. Drug Metab. Dispos. 1999 27, 327-335.
82. Morris, D. L.; Davila, J. C. Analysis of Rat Cytochrome P450 Isoenzyme Expression Using Semi-Quantitative Reverse Transcriptase-Polymerase Chain Reaction (RT-PCR). Biochem. Pharmacol. 1996, 52, 781-792.
83. Tucker, G. T.; Houston, J. B.; Huang, S. M. Optimizing Drug Development: Strategies to Assess Drug Metabolism/Transporter Interaction Potential - toward a Consensus. Pharm. Res. 2001, 18, 1071-1080.
84. Runge, D.; Kohler, C.; Kostrubsky, V. E.; Jager, D.; Lehmann, T.; Runge, D. M.; May, U.; Stolz, D. B.; Strom, S. C.; Fleig, W. E.; Michalopoulos, G. K. Induction of Cytochrome P450 (CYP)1A1, CYP1A2, and CYP3A4 but Not of CYP2C9, CYP2C19, Multidrug Resistance (MDR-1) and Multidrug Resistance Associated Protein (MRP-1) by Prototypical Inducers in Human Hepatocytes. Biochem. Biophys. Res. Commun. 2000, 273, 333-341.
85. Kocarek, T. A.; Dahn, M. S.; Cai, H.; Strom, S. C.; Mercer-Haines, N. A. Regulation of CYP2B6 and CYP3A Expression by Hydroxymethylglutaryl Coenzyme A Inhibitors in Primary Cultured Human Hepatocytes. Drug Metab. Dispos. 2002, 30, 1400-1405.
86. Madan, A.; Graham, R. A.; Carroll, K. M.; Mudra, D. R.; Burton, L. A.; Krueger, L. A.; Downey, A. D.; Czerwinski, M.; Forster, J.; Ribadeneira, M. D.; Gan, L. S.; LeCluyse, E. L.; Zech, K.; Robertson, P., Jr.; Koch, P.; Antonian, L.; Wagner, G.; Yu, L.; Parkinson, A. Effects of Prototypical Microsomal Enzyme Inducers on Cytochrome P450 Expression in Cultured Human Hepatocytes. Drug Metab. Dispos. 2003, 31, 421-431.
87. Alexandre, E.; Viollon-Abadie, C.; David, P.; Gandillet, A.; Coassolo, P.; Heyd, B.; Mantion, G.; Wolf, P.; Bachellier, P.; Jaeck, D.; Richert, L. Cryopreservation of Adult Human Hepatocytes Obtained from Resected Liver Biopsies. Cryobiology 2002, 44, 103-113.
88. Silva, J. M.; Day, S. H.; Nicoll-Griffith, D. A. Induction of Cytochrome-P450 in Cryopreserved Rat and Human Hepatocytes. Chem. Biol. Interact. 1999, 121, 49-63.
89. Tarabelsi, L. S., B.; Patten, C.; Crespi,C. Analysis of P450 Induction Potential in Cryopreserved Human Hepatocytes. Drug Metah. Rev. 2003, 35, 79.
90. Roymans, D. v. L., C.; Leone, A.; Parker, B. J.;McMillian, M.; Johnson, M. D.; Kogariti, A.; Silber, P. S.; Mannens, G.; Meuldermanns, W. Determination of CYP1A2 and CYP3A4 Induction in Cryopreserved Human Hepatocytes. Drug Metab. Rev. 2003, 35 71.
91. Garcia, M. R., J.; Wang, Q.; Hidalgo, I. J.; Owen, A.; Li, J. Induction of Cytochrome P450 1A1/2 and 3A4 Activities in Cryopreserved Human Hepatocytes. Drug Metab. Rev. 2003, 35, 73.
92. Donato, M. T.; Castell, J. V. Strategies and Molecular Probes to Investigate the Role of Cytochrome P450 in Drug Metabolism: Focus on in Vitro Studies. Clin. Pharmacokinet. 2003, 42, 153-178.
93. Brandon, E. F.; Raap, C. D.; Meijerman, I.; Beijnen, J. H.; Schellens, J. H. An Update on in Vitro Test Methods in Human Hepatic Drug Biotransformation Research: Pros and Cons. Toxicol. Appl. Pharmacol. 2003, 189, 233-246.
94. Schuetz, E. G.; Schuetz, J. D.; Strom, S. C.; Thompson, M. T.; Fisher, R. A.; Molowa, D. T.; Li, D.; Guzelian, P. S. Regulation of Human Liver Cytochromes P-450 in Family 3A in Primary and Continuous Culture of Human Hepatocytes. Hepatology 1993, 18, 1254-1262.
95. Doostdar, H.; Grant, M. H.; Melvin, W. T.; Wolf, C. R.; Burke, M. D. The Effects of Inducing Agents on Cytochrome P450 and UDP-Glucuronyltransferase Activities in Human HepG2 Hepatoma Cells. Biochem. Pharmacol. 1993, 46, 629-635.
96. Gomez-Lechon, M. J.; Donato, T.; Jover, R.; Rodriguez, C.; Ponsoda, X; Glaise, D.; Castell, J. V.; Guguen-Guillouzo, C. Expression and Induction of a Large Set of Drug-Metabolizing Enzymes by the Highly Differentiated Human Hepatoma Cell Line BC2. Eur. J. Biochem. 2001, 268, 1448-1459.
97. Mills, J. B., Faris, R.; Liu, J.; Cascio, S.; de Morais, S.M. An HTS Assay for Induction of Enzymes and Transporters Using a Human Hepatocyte Clonal Line and RNA Detection Drug Metab. Rev. 2002 34, 124.
98. Mills, J. B.; Rose, K. A.; Sadagopan, N.; Sahi, J.; de Morais, S. M. Induction of Drug Metabolism Enzymes and MDR1 Using a Novel Human Hepatocyte Cell Line. J. Pharmacol. Exp. Ther. 2004, 309, 303-309.
99. Rodriguez-Antona, C.; Jover, R.; Gomez-Lechon, M. J.; Castell, J. V. Quantitative RT-PCR Measurement of Human Cytochrome P-450s: Application to Drug Induction Studies. Arch. Biochem. Biophys. 2000, 376, 109-116.
100. 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, 781-788.
101. Czerwinski, M.; Opdam, P.; Madan, A.; Carroll, K.; Mudra, D. R.; Gan, L. L.; Luo, G.; Parkinson, A. Analysis of CYP mRNA Expression by Branched DNA Technology. Methods Enzymol. 2002, 357, 170-179.
102. Eis, P. S.; Olson, M. C.; Takova, T.; Curtis, M. L.; Olson, S. M.; Vener, T. I.; Ip, H. S.; Vedvik, K. L.; Bartholomay, C. T.; Allawi, H. T.; Ma, W. P.; Hall, J. G.; Morin, M. D.; Rushmore, T. H.; Lyamichev, V. I.; Kwiatkowski, R. W. An Invasive Cleavage Assay for Direct Quantitation of Specific RNAs. Nat. Biotechnol. 2001, 19, 673-676.
103. Nguyen, L. T.; Ramanathan, M.; Weinstock-Guttman, B.; Dole, K.; Miller, C.; Planter, M.; Patrick, K.; Brownscheidle, C.; Jacobs, L. D. Detection of Cytochrome P450 and Other Drug-Metabolizing Enzyme Mrnas in Peripheral Blood Mononuclear Cells Using DNA Arrays. Drug Metab. Dispos. 2000, 28, 987-993.
104. Plant, N. J.; Ogg, M.; Crowder, M.; Gibson, G. G. Control and Statistical Analysis of In Vitro Reporter Gene Assays. Anal. Biochem. 2000, 278, 170-174.
105. El-Sankary, W.; Gibson, G. G.; Ayrton, A.; Plant, N. Use of a Reporter Gene Assay to Predict and Rank the Potency and Efficacy of CYP3A4 Inducers. Drug Metab. Dispos. 2001, 29, 1499-1504.
106. Jones, S. A.; Moore, L. B.; Wisely, G. B.; Kliewer, S. A. Use of in Vitro Pregnane X Receptor Assays to Assess CYP3A4 Induction Potential of Drug Candidates. Methods Enzymol. 2002, 357 161-170.
107. Raucy, J.; Warfe, L.; Yueh, M. F.; Allen, S. W. A Cell-Based Reporter Gene Assay for Determining Induction of CYP3A4 in a High-Volume System. J. Pharmacol. Exp. Ther. 2002, 303, 412-423.
108. de Groot, M. J.; Alex, A. A.; Jones, B. C. Development of a Combined Protein and Pharmacophore Model for Cytochrome P450 2C9. J. Med. Chem. 2002, 45, 1983-1993.
109. Williams, P. A.; Cosine, J.; Ward, A.; Angove, H. C.; Matak Vinkovic, D.; Jhoti, H. Crystal Structure of Human Cytochrome P450 2C9 with Bound Warfarin. Nature 2003, 424, 464-468.
110. Ekins, S.; Schuetz, E. The PXR Crystal Structure: The End of the Beginning. Trends Pharmacol. Sci. 2002, 23, 49-50.
111. Ekins, S.; Erickson, J. A. A Pharmacophore for Human Pregnane X Receptor Ligands. Drug Metab. Dispos. 2002, 30, 96-99.
112. Ekins, S. Predicting Undesirable Drug Interactions with Promiscuous Proteins in Silic. Drug Discov Today 2004, 9 276-285.
113. Sarich, T.; Kalhorn, T.; Magee, S.; al-Sayegh, F.; Adams, S.; Slattery, J.; Goldstein, J.; Nelson, S.; Wright, J. The Effect of Omeprazole Pretreatment on Acetaminophen Metabolism in Rapid and Slow Metabolizers of S-Mephenytoin. Clin. Pharmacol. Ther. 1997, 62, 21-28.
114. Chiba, K.; Kobayashi, K.; Manabe, K.; Tani, M.; Kamataki, T., Ishizaki, T. Oxidative Metabolism of Omeprazole in Human Liver Microsomes: Cosegregation with S-Mephenytoin 4′-Hydroxylation J. Pharmacol. Exp. Ther. 1993, 266, 52-59.
115. Karam, W. G.; Goldstein, J. A.; Lasker, J. M.; Ghanayem, B. I. Human CYP2C19 Is a Major Omeprazole 5-Hydroxylase, as Demonstrated with Recombinant Cytochrome P450 Enzymes. Drug Metab. Dispos. 1996, 24, 1081-1087.
116. Backman, J. T.; Olkkola, K. T.; Ojala, M.; Laaksovirta, H.; Neuvonen, P. J. Concentrations and Effects of Oral Midazolam Are Greatly Reduced in Patients Treated with Carbamazepine or Phenytoin. Epilepsia 1996, 37, 253-257.
117. Backman, J. T.; Kivisto, K. T.; Olkkola, K. T.; Neuvonen, P. J. The Area under the Plasma Concentration-Time Curve for Oral Midazolam, Is 400-Fold Larger During Treatment with Itraconazole Than with Rifampicin. Eur. J. Clin. Pharmacol. 1998, 54, 53-58.
118. Backman, J. T.; Olkkola, K. T.; Neuvonen, P. J. Rifampin Drastically Reduces Plasma Concentrations and Effects of Oral Midazolam. Clin. Pharmacol. Ther. 1996, 59, 7-13.
119. Thummel, K. E.; O'Shea, D.; Paine, M. F.; Shen, D. D.; Kunze, K. L.; Perkins, J. D.; Wilkinson, G. R. Oral First-Pass Elimination of Midazolam Involves Both Gastrointestinal and Hepatic CYP3A-Mediated Metabolism. Clin. Pharmacol. Ther. 1996, 59, 491-502.
120. Watkins, P. B.; Murray, S. A.; Winkelman, L. G.; Heilman, D. M.; Wrighton, S. A.; Guzelian, P. S. Erythromycin Breath Test as an Assay of Glucocorticoid-Inducible Liver Cytochromes P-450. Studies in Rats and Patients. J. Clin. Invest. 1989, 83, 688-697.
121. Watkins, P. B. Noninvasive Tests of CYP3A Enzymes. Pharmacogenetics 1994, 4, 171-184.
122. Paine, M. F.; Wagner, D. A.; Hoffmaster, K. A.; Watkins, P. B. Cytochrome P450 3A4 and P-Glycoprotein Mediate the Interaction between an Oral Erythromycin Breath Test and Rifampin. Clin. Pharmacol. Ther. 2002, 72, 524-535.
123. Ged, C.; Rouillon, J. M.; Pichard, L.; Combalbert, J.; Bressot, N.; Bories, P.; Michel, H.; Beaune, P.; Maurel, P. The Increase in Urinary Excretion of 6 Beta-Hydroxycortisol as a Marker of Human Hepatic Cytochrome P450IIIa Induction. Br. J. Clin. Pharmacol. 1989, 28, 373-387.
124. Ohnhaus, E. E.; Breckenridge, A. M.; Park, B. K. Urinary Excretion of 6 Beta-Hydroxycortisol and the Time Course Measurement of Enzyme Induction in Man. Eur. J. Clin. Pharmacol. 1989, 36 39-46.
125. Fleishaker, J. C.; Pearson, L. K.; Peters, G. R. Phenytoin Causes a Rapid Increase in 6 Beta-Hydroxycortisol Urinary Excretion in Humans - a Putative Measure of CYP3A Induction J. Pharm. Sci. 1995, 84, 292-294.
126. Koup, J. R.; Anderson, G. D.; Loi, C. M. Effect of Troglitazone on Urinary Excretion of 6beta-Hydroxycortisol. J. Clin. Pharmacol. 1998, 38, 815-818.
127. Roby, C. A.; Anderson, G. D.; Kantor, E.; Dryer, D. A.; Burstein, A. H. St John's Wort: Effect on CYP3A4 Activity. Clin. Pharmacol. Ther. 2000, 67, 451-457.
128. Bodin, K.; Bretillon, L.; Aden, Y.; Bertilsson, L.; Broome, U.; Einarsson, C.; Diczfalusy, U. Antiepileptic Drugs Increase Plasma Levels of 4beta-Hydroxycholesterol in Humans: Evidence for Involvement of Cytochrome P450 3A4. J. Biol. Chem. 2001, 276, 38685-38689.
129. Perucca, E.; Grimaldi, R.; Frigo, G. M.; Sardi, A.; Monig, H.; Ohnhaus, E. E. Comparative Effects of Rifabutin and Rifampicin on Hepatic Microsomal Enzyme Activity in Normal Subjects. Eur. J. Clin. Pharmacol. 1988, 34, 595-599.
130. Barditch-Crovo, P.; Trapnell, C. B.; Ette, E.; Zacur, H. A.; Coresh, J.; Rocco, L. E.; Hendrix, C. W.; Flexner, C. The Effects of Rifampin and Rifabutin on the Pharmacokinetics and Pharmacodynamics of a Combination Oral Contraceptive. Clin. Pharmacol. Ther. 1999, 65, 428-438.
131. Rutledge, D. R.; Pieper, J. A.; Mirvis, D. M. Effects of Chronic Phenobarbital on Verapamil Disposition in Humans. J. Pharmacol. Exp. Ther. 1988, 246, 7-13.
132. Tartara, A.; Galimberti, C. A.; Manni, R.; Parietti, L.; Zucca, C.; Baasch, H.; Caresia, L.; Muck, W.; Barzaghi, N.; Gatti, G.; et al. Differential Effects of Valproic Acid and Enzyme-Inducing Anticonvulsants on Nimodipine Pharmacokinetics in Epileptic Patients. Br. J. Clin. Pharmacol. 1991, 32, 335-340.
133. Nallani, S. C. G., T.A.; Hariparsad,N.; Desai P.B. Topiramate, an Anti-Epileptic Agent, Activates the Pregnane X Receptor and Induces Cytochrome P450 3A4 Enzyme. Drug Metab. Rev. 2003 35, 80.
134. Rosenfeld, W. E.; Doose, D. R.; Walker, S. A.; Nayak, R. K. Effect of Topiramate on the Pharmacokinetics of an Oral Contraceptive Containing Norethindrone and Ethinyl Estradiol in Patients with Epilepsy. Epilepsia 1997, 38, 317-323.
135. Clarke, S. M.; Mulcahy, F. M.; Tjia, J.; Reynolds, H. E.; Gibbons, S. E.; Barry, M. G.; Back, D. J. Pharmacokinetic Interactions of Nevirapine and Methadone and Guidelines for Use of Nevirapine to Treat Injection Drug Users. Clin. Infect. Dis. 2001, 33, 1595-1597.
136. Clarke, S. M.; Mulcahy, F. M.; Tjia, J.; Reynolds, H. E.; Gibbons, S. E.; Barry, M. G.; Back, D. J. The Pharmacokinetics of Methadone in HIV-Positive Patients Receiving the Non-Nucleoside Reverse Transcriptase Inhibitor Efavirenz. Br. J. Clin. Pharmacol. 2001 51, 213-217.
137. Mouly, S.; Lown, K. S.; Kornhauser, D.; Joseph, J. L.; Fiske, W. D.; Benedek, I. H.; Watkins, P. B. Hepatic but Not Intestinal CYP3A4 Displays Dose-Dependent Induction by Efavirenz in Humans. Clin. Pharmacol. Ther. 2002, 72, 1-9.
138. Loi, C. M.; Stern, R.; Koup, J. R.; Vassos, A. B.; Knowlton, P.; Sedman, A. J. Effect of Troglitazone on the Pharmacokinetics of an Oral Contraceptive Agent. J. Clin. Pharmacol. 1999, 39, 410-417.
139. Loi, C. M.; Young, M.; Randinitis, E.; Vassos, A.; Koup, J. R. Clinical Pharmacokinetics of Troglitazone. Clin. Pharmacokinet. 1999, 37, 91-104.
140. Geletko, S. M.; Erickson, A. D. Decreased Methadone Effect after Ritonavir Initiation. Pharmacotherapy 2000, 20, 93-94.
141. Wang, Z.; Gorski, J. C.; Hamman, M. A.; Huang, S. M.; Lesko, L. J.; Hall, S. D. The Effects of St John's Wort (Hypericum Perforatum) on Human Cytochrome P450 Activity. Clin. Pharmacol. Ther. 2001 70, 317-326.
142. McCune, J. S.; Hawke, R. L.; LeCluyse, E. L,.; Gillenwater, H. H.; Hamilton, G.; Ritchie, J.; Lindley, C. In Vivo and in Vitro Induction of Human Cytochrome P4503A4 by Dexamethasone. Clin. Pharmacol. Ther. 2000, 68, 356-366.
143. Robertson, P., Jr.; Hellriegel, E. T.; Arora, S.; Nelson, M. Effect of Modafinil on the Pharmacokinetics of Ethinyl Estradiol and Triazolam in Healthy Volunteers. Clin. Pharmacol. Ther. 2002, 71, 46-56.
144. Weber, C.; Schmitt, R.; Birnboeck, H.; Hopfgartner, G.; Eggers, H.; Meyer, J.; van Marle, S.; Viischer, H. W.; Jonkman, J. H. Multiple-Dose Pharmacokinetics, Safety, and Tolerability of Bosentan, an Endothelin Receptor Antagonist, in Healthy Male Volunteers. J. Clin. Pharmacol. 1999, 39, 703-714.
145. Sahi, J.; Milad, M. A.; Zheng, X.; Rose, K. A.; Wang, H.; Stilgenbauer, L.; Gilbert, D.; Jolley, S.; Stern, R. H.; LeCluyse, E. L. Avasimibe Induces CYP3A4 and Multiple Drug Resistance Protein 1 Gene Expression through Activation of the Pregnane X Receptor. J. Pharmacol. Exp. Ther. 2003, 306, 1027-1034.
146. Nallani, S., Goodwin, B., Buckley D., Buckley, A., Desai P. Mechanism of Differential Induction of CYP3A by Taxane Anticancer Agents. Drug Metab. Rev. 2002, 34, 125.
147. Roymans, D.; Van Looveren, C.; Leone, A.; Parker, J. B.; McMillian, M.; Johnson, M. D.; Koganti, A.; Gilissen, R.; Silber, P.; Mannens, G.; Meuldermans, W. Determination of Cytochrome P450 1A2 and Cytochrome P450 3A4 Induction in Cryopreserved Human Hepatocytes. Biochem. Pharmacol. 2004, 67, 427-437.
148. Harris, R. Z.; Inglis, A. M.; Miller, A. K.; Thompson, K. A.; Finnerty, D.; Patterson, S.; Jorkasky, D. K.; Freed, M. I. Rosiglitazone Has No Clinically Significant Effect on Nifedipine Pharmacokinetics. J. Clin. Pharmacol. 1999, 39, 1189-1194.
149. Inglis, A. M.; Miller, A. K.; Culkin, K. T.; Finnerty, D.; Patterson, S. D.; Jorkasky, D. K.; Freed, M. I. Lack of Effect of Rosiglitazone on the Pharmacokinetics of Oral Contraceptives in Healthy Female Volunteers. J. Clin. Pharmacol. 2001, 41, 683-690.
150. Prueksaritanont, T.; Vega, J. M.; Zhao, J.; Gagliano, K.; Kuznetsova, O.; Musser, B.; Amin, R. D.; Liu, L.; Roadcap, B. A.; Dilzer, S.; Lasseter, K. C.; Rogers, J. D. Interactions between Simvastatin and Troglitazone or Pioglitazone in Healthy Subjects. J. Clin. Pharmacol. 2001, 41, 573-581.
151. Reinach, B.; de Sousa, G.; Dostert, P.; Ings, R.; Gugenheim, J.; Rahmani, R. Comparative Effects of Rifabutin and Rifampicin on Cytochromes P450 and UDP-Glucuronosyl-Transferases Expression in Fresh and Cryopreserved Human Hepatocytes. Chem. Biol. Interact. 1999 121, 37-48.
152. Li, A. P.; Reith, M. K.; Rasmussen, A.; Gorski, J. C.; Hall, S. D.; Xu, L.; Kaminski, D. L.; Cheng, L. K. Primary Human Hepatocytes as a Tool for the Evaluation of Structure-Activity Relationship in Cytochrome P450 Induction Potential of Xenobiotics: Evaluation of Rifampin, Rifapentine and Rifabutin. Chem. Biol. Interact. 1997 107, 17-30.
153. Vital Durand, D.; Hampden, C.; Boobis, A. R.; Park, B. K.; Davies, D. S. Induction of Mixed Function Oxidase Activity in Man by Rifapentine (MDL 473), a Long-Acting Rifamycin Derivative Br. J. Clin. Pharmacol. 1986, 21, 1-7.
154. Ishigami, M.; Honda, T.; Takasaki, W.; Ikeda, T.; Kornai, T.; Ito, K.; Sugiyama, Y. A Comparison of the Effects of 3-Hydroxy-3-Methylglutaryl-Coenzyme a (HMG-CoA) Reductase Inhibitors on the CYP3A4-Dependent Oxidation of Mexazolam in Vitro Drug Metab. Dispos. 2001, 29, 282-288.
155. Nakai, D.; Nakagomi, R.; Furuta, Y.; Tokui, T.; Abe, T.; Ikeda, T.; Nishimura, K. Human Liver-Specific Organic Anion Transporter, LST-1, Mediates Uptake of Pravastatin by Human Hepatocytes. J. Pharmacol. Exp. Ther. 2001, 297, 861-867.
156. Strom, S. C.; Pisarov, L. A.; Dorko, K.; Thompson, M. T.; Schuetz, J. D.; Schuetz, E. G. Use of Human Hepatocytes to Study P450 Gene Induction. Methods Enzymol. 1996, 272, 388-401.
157. Kelly, J. G.; O'Malley, K. Clinical Pharmacokinetics of Calcium Antagonists. An Update. Clin. Pharmacokinet. 1992, 22, 416-433.
158. Barry, M.; Mulcahy, F.; Merry, C.; Gibbons, S.; Back, D. Pharmacokinetics and Potential Interactions Amongst Antiretroviral Agents Used to Treat Patients with HIV Infection. Clin. Pharmacokinet. 1999, 36, 289-304.
159. Greiner, B.; Eichelbaum, M.; Fritz, P.; Kreichgauer, H. P.; von Richter, O.; Zundler, J.; Kroemer, H. K. Tile Role of Intestinal P-Glycoprotein in the Interaction of Digoxin and Rifampin. J. Clin. Invest. 1999, 104, 147-153.
160. Hariparsad, N., Nallani, S.C.; Desai, P.B. Characterization of the Modulation of the CYP3A4 Activity by Efavirenz. Drug Metab. Rev. 2003, 35, 79.
161. Hayashi, S.; Jayesekera, D.; Jayewardene, A.; Shah, A.; Thevanayagam, L.; Aweeka, F. Altered Pharmacokinetics of Indinavir by a Novel Nonnucleoside Reverse Transcriptase Inhibitor (HBY-097): A Pharmacokinetic Evaluation in HIV-Positive Patients. J. Clin. Pharmacol. 1999, 39, 1085-1093.
162. Moore, K. H.; Cass, L. M.; Dallow, N.; Hardman, T. C.; Jones, A.; Boyce, M.; Prince, W. T. Pharmacokinetics and Tolerability of GW420867x, a Nonnucleoside Reverse Transcriptase Inhibitor, Following Single Escalating Doses in Healthy Male Volunteers. J. Clin. Pharmacol. 2001, 41, 1098-1105.
163. Lin, J.; Fiske, W. D.; Kim, S.; Yang, T. J.; Ding, D.; Jolley, S.; Sinz, M.; LeCluyse, E.; Gan, L. S.; Luo, G. CYP3A4 Induction by DPC 681. Drug Metab. Rev. 2002, 34, 124.
164. Bertilsson, L.; Hojer, B.; Tybring, G.; Osterloh, J.; Rane, A. Autoinduction of Carbamazepine Metabolism in Children Examined by a Stable Isotope Technique. Clin. Pharmacol. Ther. 1980, 27 83-88.
165. Eichelbaum, M.; Tomson, T.; Tybring, G.; Bertilsson, L. Carbamazepine Metabolism in Man. Induction and Pharmacogenetic Aspects. Clin. Pharmacokinet. 1985, 10, 80-90.
166. Wang, H.; LeCluyse, E. L. Role of Orphan Nuclear Receptors in the Regulation of Drug-Metabolising Enzymes. Clin. Pharmacokinet. 2003, 42, 1331-1357.
167. Tirona, R. G.; Leake, B. F.; Wolkoff, A. W.; Kim, R. B. Human Organic Anion Transporting Polypeptide-C (SLC21A6) Is a Major Determinant of Rifampin-Mediated Pregnane X Receptor Activation. J. Pharmacol. Exp. Ther. 2003, 304, 223-228.
168. Tirona, R. G.; Leake, B. F.; Merino, G.; Kim, R. B. Polymorphisms in OATP-C: Identification of Multiple Allelic Variants Associated with Altered Transport Activity among European- and African-Americans. J. Biol. Chem. 2001, 276, 35669-35675.
169. Smith, D. A. Induction and Drug Development. Eur. J. Pharm. Sci. 2000, 11, 185-189.
170. Worboys, P. D.; Carlile, D. J. Implications and Consequences of Enzyme Induction on Preclinical and Clinical Drug Development. Xenobiotica 2001, 31, 539-556.
171. Bjornsson, T. D.; Callaghan, J. T.; Einolf, H. J.; Fischer, V.; Gan, L.; Grimm, S.; Kao, J.; King, S. P.; Miwa, G.; Ni, L.; Kumar, G.; McLeod, J.; Obach, S. R.; Roberts, S.; Roe, A.; Shah, A.; Snikeris, F.; Sullivan, J. T.; Tweedie, D.; Vega, J. M.; Walsh, J.; Wrighton, S. A. The Conduct of in Vitro and in Vivo Drug-Drug Interaction Studies: A PhRMA Perspective. J. Clin. Pharmacol. 2003 43 443-469.