Receptor-dependent transcriptional activation of cytochrome P4503A genes: induction mechanisms, species differences and interindividual variation in man

References

• AOYAMA, T., YAMANO, S., WAXMAN, D. J., LAPENSON, D. P., MEYER, U. A., FISCHER, V., TYNDALE, R., INABA, T., KALOW, W., GELBOIN, H. V. and GONZALEZ, F. J., 1989, Cytochrome p450 hpcn3, a novel cytochrome p450 IIIA-gene product that is differentially expressed in adult human liver-cDNA and deduced amino-acid sequence and distinct specificities of cDNA-expressed hpcnl and hpcn3 for the metabolism of steroid-hormones and cyclosporine. Journal of Biological Chemistry, 264, 10388–10395.
   PubMed Web of Science ®Google Scholar
• AUSTIN, K. L., MATHER, L. E., PHILPOT, C. R. and MCDONALD, P. J., 1980, Inter-subject and dose-related variability after intravenous administration of erythromicin. British Journal of Clinical Pharmacology, 10, 273–279.
   PubMed Web of Science ®Google Scholar
• BAES, M., GULICK, T., Cum, H. S., MARTINOLI, M. G., SimitA, D. and MOORE, D. D., 1994, A new orphan member of the nuclear hormone receptor family that interacts with a subset of retinoic acid response elements. Molecular and Cellular Biology, 14, 1544–1551.
   PubMed Web of Science ®Google Scholar
• BALL, S., SCATINA, J., KAO, J., FERRON, G., FRUNCILLO, R., MAYER, P., HOPKINS, P., WARNER, N. and HALL, J., 1999, Population distribution and effects on drug metabolism of a genetic variant in the 5' promoter region of CYP3A4. Clinical Pharmacology and Therapeutics, 66, 288–294.
   PubMed Web of Science ®Google Scholar
• BARNES, K. M., DICKSTEIN, B., CUTLER, G. B., Fojo, T. and BATES, S. E., 1996, Steroid transport, accumulation and antagonism of P-glycoprotein in multidrug-resistant cells. Biochemistry, 35, 4820A–827.
   Web of Science ®Google Scholar
• BARWICK, J. L., QUATTROCHI, L. C., MILLS, A. S., POTENZA, C., TUKEY, R. H. and GUZELIAN, P. S., 1996, Trans-species gene transfer for analysis of glucocorticoid-inducible transcriptional activation of transiently expressed human CYP3A4 and rabbit CYP3A6 in primary cultures of adult rat and rabbit hepatocytes. Molecular Pharmacology, 50, 10–16.
   PubMed Web of Science ®Google Scholar
• BEATO, M., 1989, Gene regulation by steroid hormones. Cell, 56, 335–344.
   PubMed Web of Science ®Google Scholar
• BERTILSSON, F., BERKENSTAM, A. and BLOMQUIST, P., 2001, Functionally conserved xenobiotic responsive enhancer in cytochrome P450 3A7. Biochemical and Biophysical Research Communications, 280, 139–144.
   PubMed Web of Science ®Google Scholar
• BERTILSSON, G., HEIDRICH, J., SVENSSON, K., ASMAN, M., JENDEBERG, L., SYDOW-BACKMAN, M., OHLSSON, R., PosmiND, H., BLOMQUIST, P. and BERKENSTAM, A., 1998, Identification of a human nuclear receptor defines a new signalling pathway for CYP3A induction. Proceedings of the National Academy of Sciences, USA, 95, 12208–12213.
   Google Scholar
• BLIZARD, D., SUEYOSHI, T., NEGISHI, M., DEHAL, S. S. and KUPFER, D., 2001, Mechanism of induction of cytochrome P450 enzymes by the proestrogenic endocrine disrupter pesticide-methoxychlor: interactions of methoxychlor metabolites with the constitutive androstane receptor system. Drug Metabolism and Disposition, 29, 781–785.
   PubMed Web of Science ®Google Scholar
• BLUMBERG, B., SABBAGH, W., JR, JUGUILON, H., BOLO, J., JR, VAN METER, C. M., ONG, E. S. and EVANS, R. M., 1998, SXR, a novel steroid and xenobiotic- sensing nuclear receptor. Genes and Development, 12, 3195–3205.
   Google Scholar
• BROOKS, B. A., MCBRIDE, O. W., DOLPHIN, C. T., FARRALL, M., SCAMBLER, P. J., GONZALEZ, F. J. and IDLE, J. R., 1988, The gene CYP3 encoding P450pcn1 (nifedipine oxidase) is tightly linked to the gene COL1A2 encoding collagen type 1 alpha on 7q21-q22. 1. American Journal of Human Genetics, 43, 280–284.
   PubMed Web of Science ®Google Scholar
• BURGER, H. J., SCHUETZ, J. D., SCHUETZ, E. G. and GUZELIAN, P. S., 1992, Paradoxical transcriptional activation of rat-liver cytochrome-P-450 3A1 by dexamethasone and the antiglucocorticoid pregnenolone 16-alpha-carbonitrile — analysis by transient transfection into primary monolayer-cultures of adult-rat hepatocytes. Proceedings of the National Academy of Sciences, USA, 89, 2145–2149.
   PubMed Web of Science ®Google Scholar
• CAIRNS, W., SMITH, C. A., MCLAREN, A. W. and WOLF, C. R., 1996, Characterization of the human cytochrome P4502D6 promoter. A potential role for antagonistic interactions between members of the nuclear receptor family. Journal of Biological Chemistry, 271, 25269–25276.
   PubMed Web of Science ®Google Scholar
• CASHMAN, J. R., 1996, Drug discovery and drug metabolism. Drug Discovely Today, 1, 209–216.
   Web of Science ®Google Scholar
• CHEN, D., LEPAR, G. and KEMPER, B., 1994, A transcriptional regulatory element common to a large family of hepatic cytochrome P450 genes is afunctional binding site of the orphan receptor HNF-4. Journal of Biological Chemistry, 269, 5420–5427.
   PubMed Web of Science ®Google Scholar
• CHEN, H., BRZEZINSKI, M. R., FANTEL, A. G. and JuciLku, M. R., 1999, Catalysis of drug oxidation during embryogenesis in human hepatic tissues using imipramine as a model substrate. Drug Metabolism and Disposition, 27, 1306–1308.
   PubMed Web of Science ®Google Scholar
• CHOI, H.-S., CHUNG, M., TZAMELI, I., SIMHA, D., LEE, Y.-K., SEOL, W. and MOORE, D. D., 1997, Differential transactivation by two isoforms of the orphan nuclear hormone receptor CAR. Journal of Biological Chemistry, 272, 23565–23571.
   PubMed Web of Science ®Google Scholar
• CHOLERTON, S., DALY, A. K. and IDLE, J. R., 1992, The role of individual human cytochromes P450 in drug-metabolism and clinical-response. Trends in Pharmacological Sciences, 13, 434–439.
   PubMed Web of Science ®Google Scholar
• CIACCIO, P. J., GRAVES, P. E., BOURQUE, D. P., GLINSMANN-GIBSON, B. and HALPERT, J. R., 1991, cDNA and deduced amino acid sequences of a dog liver cytochrome P450 of the Ma gene sub-family. Biochimica et Biophysica Ada, 1088, 319–322.
   Google Scholar
• DALY, A. K., BROCKMOLLER, J., BADLY, F., EICHELBAUM, M., EVANS, W. E., GONZALEZ, F. J., HUANG, J. D., IDLE, J. R., INGELMAN-SUNDBERG, M., ISHIZAKI, T., JACQZAIGRAIN, E., MEYER, U. A., NEBERT, D. W., STEEN, V. M., WOLF, C. R. and ZANGER, U. M., 1996, Nomenclature for human CYP2D6 alleles. Pharmacogenetics, 6, 193–201.
   Google Scholar
• DAMKIER, P., HANSEN, L. L. and BROSEN, K., 1999, Rifampicin treatment greatly increases the apparent oral clearance of quinidine. Pharmacology and Toxicology, 85, 257–262.
   PubMedGoogle Scholar
• DE WILDT, S. N., KEARNS, G. L., LEEDER, J. S. and VAN DEN ANKER, J. N., 1999, Cytochrome P450 3A — ontogeny and drug disposition. Clinical Pharmacokinetics, 37, 485–505.
   Google Scholar
• DOMANSKI, T., FINTA, C., HALPERT, J. and ZAPHIROPOULOS, P., 2001, cDNA cloning and initial characterization of CYP3A43, a novel human cytochrome P450. Molecular Pharmacology, 59, 386–392.
   PubMed Web of Science ®Google Scholar
• DOTZLAW, H., LEYGUE, E., WATSON, P. and MURPHY, L. C., 1999, The human orphan receptor PXR messenger RNA is expressed in both normal and neoplastic breast tissue. Clinical Cancer Research, 5, 2103–2107.
   PubMed Web of Science ®Google Scholar
• EL-SANKARY, W., PLANT, N. and GIBSON, G., 2000, Regulation of the CYP3A4 gene by hydrocortisone and xenobiotics: role of the glucocorticoid and pregnane x receptors. Drug Metabolism and Disposition, 28, 493–496.
   PubMed Web of Science ®Google Scholar
• EL-SANKARY, W., PLANT, N. J. and GIBSON, G. G., 2001, Use of a reporter gene assay to predict and rank the potency and efficacy of CYP3A4 inducers. Drug Metabolism and Disposition, 29, 1499–1504.
   Google Scholar
• ELIASSON, E., MKRTCHIAN, S., HALPERT, J. R. and INGELMAN-SUNDBERG, M., 1994, Substrate-regulated, c-AMP- dependent phosphorylation, denaturation and degradation of glucocorticoid-inducible cytochrome P4503A1. Journal of Biological Chemistry, 269, 1 8378–1 8383.
   Google Scholar
• EVANS, R. M., 1988, The steroid and thyroid hormone receptor superfamily. Science, 240, 889-895. FERRO, M., BASSI, A. M., PENCO, S. and NANNI, G., 1993, Use of established hepatoma cell lines in biotoxicology. Cytotechno/ogy, 11, S126–129.
   Google Scholar
• FINTA, C. and ZAPHIROPOULOS, P. G., 2000, The human cytochrome P450 3A locus. Gene evolution by capture of downstream exons. Gene, 260, 13–23.
   PubMed Web of Science ®Google Scholar
• FORMAN, B. M., TZAMELI, I., CHOI, H. S., CHEN, L., SIMHA, D., SEOL, W., EVANS, R. M. and MOORE, D. D., 1998, Androstane metabolites bind to and deactivate the nuclear receptor CAR-beta. Nature, 395, 612–615.
   PubMed Web of Science ®Google Scholar
• FRASER, D. J., FEYEREISEN, R., HARLOW, G. R. and HALPERT, J. R., 1997, Isolation, heterologous expression and functional characterisation of a novel cytochrome P450 3A enzyme from a canine liver cDNA library. Journal of Pharmacology and Experimental Therapeutics, 283, 1425–1432.
   PubMed Web of Science ®Google Scholar
• FUHR, U., 2000, Induction of drug metabolising enzymes - pharmacokinetic and toxicological consequences in humans. Clinical Pharmacokinetics, 38, 493–504.
   PubMed Web of Science ®Google Scholar
• FUKUDA, Y., IsPim, N., Nouucin, T., KAPPAS, A. and SAssA, S., 1992, Interleukin-6 down regulates the expression of transcripts encoding cytochrome P450 1A1, 1A2 and 3A3 in human hepatoma cells. Biochemical and Biophysical Research Communications, 184, 960–965.
   PubMed Web of Science ®Google Scholar
• GEICK, A., EICHELBAUM, M. and BURR, O., 2001, Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. Journal of Biological Chemistry, 276, 14581–14587.
   PubMed Web of Science ®Google Scholar
• GERBAL-CHALOIN, S., PASCUSSI, J. M., PICHARD-GARCIA, L., DAUJAT, M., WAECHTER, F., FABRE, J. M., CARRERE, N. and MAUREL, P., 2001, Induction of CYP2C genes in human hepatocytes in primary culture. Drug Metabolism and Disposition, 29, 242–251.
   Google Scholar
• GERVOT, L., CARRIERE, V., COSTET, P., CUGNENC, P. H., BERGER, A., BEAUNE, P. H. and DE WAZIERS, I., 1996, CYP3A5 is the major cytochrome P450 3A expressed in human colon and colonic cell lines. Environmental Toxicology and Pharmacology, 2, 381–388.
   PubMed Web of Science ®Google Scholar
• GILLAM, E. M., Guo, Z., UENG, Y. F., YAMAZAKI, H., COCK, I., REILLY, P. E., HOOPER, W. D. and GUENGERICH, F. P., 1995, Expression of cytochrome P450 3A5 in Escherichia co/i: effects of 5' modification, purification, spectral characterization, reconstitution conditions, and catalytic activities. Archives of Biochemistry and Biophysics, 317, 374–378.
   PubMed Web of Science ®Google Scholar
• GONZALEZ, F. J., SONG, B. J. and HARDWICK, J. P., 1986, Pregnenolone 16 alpha- carbonitrile-inducible P-450 gene family: gene conversion and differential regulation. Molecular and Cellular Biology, 6, 2969–2976.
   PubMed Web of Science ®Google Scholar
• GOODWIN, B., HODGSON, E. and LIDDLE, C., 1999a, The orphan human pregnane X receptor mediates the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer module. Molecular Pharmacology, 56, 1329–1339.
   PubMed Web of Science ®Google Scholar
• GOODWIN, B. J., HODGSON, E. and LIDDLE, C., 1999b, The orphan nuclear receptor hCAR supports constitutive expression of the human cytochrome P450 3A4 gene in Hep G2 cells. Hepatology, 30, 929.
   Web of Science ®Google Scholar
• GORSKI, J. C., HALL, S. D., JONES, D. R., BANDEN-BRANDEN, M. and WRIGTON, S. A., 1994, Regioselective biotransformation of midazolam by members of the human cytochrome P4503A (CYP3A) subfamily. Biochemical Pharmacology, 47, 1643–1653.
   Google Scholar
• GRANGE, T., Roux, J., RIGAUD, G. and PICTET, R., 1991, Cell-type specific activity of two glucocorticoid responsive units of rat tyrosine aminotransferase gene is associated with multiple binding sites for c/e bp and a novel liver-specific nuclear factor. Nucleic Acids Research, 19, 131–139.
   PubMed Web of Science ®Google Scholar
• GREUET, J., PICHARD, L., BONFILS, C., DOMERGUE, J. and MAUREL, P., 1996, The fetal specific gene CYP3A7 is inducible by rifampicin in adult human hepatocytes in primary culture. Biochemical and Biophysical Research Communications, 225, 689–694.
   PubMed Web of Science ®Google Scholar
• GUENGERICH, F., 1999, Cytochrome P450 3A4: regulation and role in drug metabolism. Annual Review in Pharmacology and Toxicology, 39, 1–17.
   PubMed Web of Science ®Google Scholar
• GUENGERICH, F. P. and TURVY, C. G., 1991, Comparison of levels of several human microsomal cytochrome P-450 enzymes and epoxide hydrolase in normal and disease states using irnmunochemical analysis of surgical liver samples. Journal of Pharmacology and Experimental Therapeutics, 256, 1189–1194.
   PubMed Web of Science ®Google Scholar
• HAEHNER, B. D., GORSKI, J. C., VANDENBRANDEN, M., WRIGHTON, S. A., JANARDAN, S. K., WATKINS, P. B. and HALL, S. D., 1996, Bimodal distribution of renal cytochrome P450 3A activity in humans. Molecular Pharmacology, 50, 52–59.
   PubMed Web of Science ®Google Scholar
• HANDSCHIN, C., PODVINEC, M. and MEYER, U., 2000, CXR, a chicken xenobiotic- sensing orphan nuclear receptor is related to both mammalian pregnane X receptor (PXR) and constitutive androstane receptor (CAR). Proceedings of the National Academy of Sciences, USA, 97, 10769–10774.
   PubMed Web of Science ®Google Scholar
• HASHIMOTO, H., TOIDE, K., KITAMURA, R., FUJITA, M., TAGAWA, S., ITOH, S. and KAMATAKI, T., 1993, Gene structure of CYP3A4, and adult specific form of cytochrome P450 in human livers, and its transcriptional control. European Journal of Biochemistry, 218, 585–595.
   PubMedGoogle Scholar
• HE, Y. A., HE, Y. Q., SZKLARZ, G. D. and HALPERT, J. R., 1997, Identification of three key residues in substrate recognition site 5 of human cytochrome P450 3A4 by cassette and site-directed mutagenesis. Biochemistry, 36, 8831–8839.
   PubMed Web of Science ®Google Scholar
• HONKAKOSKI, P., JAASKELAINEN, I., KORTELAHTI, M. and URTTI, A., 2001, A novel drug-regulated gene expression system based on the nuclear receptor constitutive androstane receptor (CAR). Pharmaceutical Research, 18, 146–150.
   PubMed Web of Science ®Google Scholar
• HONKAKOSKI, P., ZELKO, I., SUEYOSHI, T. and NEGISHI, M., 1998, The nuclear orphan receptor CAR-retinoid x receptor heterodimer activates the phenobarbital-responsive enhancer module of the CYP2B6 gene. Molecular and Cellular Biology, 18, 5652–5658.
   PubMed Web of Science ®Google Scholar
• HOSTETLER, K. A., WRIGHTON, S. A., MOLOWA, D. T., THOMAS, P. E., LEVIN, W. and GUZELIAN, P. S., 1989, Co-induction of multiple hepatic cytochrome P-450 proteins and their messenger-RNAs in rats treated with irnidazole antimycotic agents. Molecular Pharmacology, 35, 279–285.
   PubMed Web of Science ®Google Scholar
• HSEIH, K -P., LIN, Y.-Y., CHENG, C.-L., LAI, M.-L., LIN, M.-S., SIEST, J.-P. and HUANG, J.-D., 2001, Novel mutations of CYP3A4 in Chinese. Drug Metabolism and Disposition, 29, 268–273.
   Google Scholar
• HUNT, C. M., WESTERKAM, W. R. and STAVE, G. M., 1992, Effect of age and gender on the activity of human hepatic CYP3A. Biochemical Pharmacology, 44, 275–283.
   PubMed Web of Science ®Google Scholar
• HUSS, J. M. and KASPER, C. B., 1998, Nuclear receptor involvement in the regulation of rat cytochrome P450 3A23 expression. Journal of Biological Chemistry, 273, 16155–16162.
   PubMed Web of Science ®Google Scholar
• HUSS, J. M. and KASPER, C. B., 2000, Two-stage glucocorticoid induction of CYP3A23 through both the glucocorticoid and pregnane X receptors. Molecular Pharmacology, 58, 48–57.
   PubMed Web of Science ®Google Scholar
• HUSS, J. M., WANG, S. I., ASTROM, A., MCOUIDDY, P. and KASPER, C. B., 1996, Dexamethasone responsiveness of a major glucocorticoid-inducible CYP3A gene is mediated by elements unrelated to a glucocorticoid receptor binding motif. Proceedings of the National Academy of Sciences, USA, 93, 4666–4670.
   PubMed Web of Science ®Google Scholar
• ING, N. H. and O'MALLEY, B., 1995, The steroid hormone receptor superfamily: molecular mechanisms of action. In B. D. Weintrub (ed.), Endocrinology: Basic Concepts and Clinical Correlations (New York: Raven), pp. 195–215.
   Google Scholar
• INGELMAN-SUNDBERG, M., 2001, Implications of polymorphic cytochrome P450-dependent drug metabolism for drug development. Drug Metabolism and Disposition, 29, 570–573.
   PubMed Web of Science ®Google Scholar
• IOANNIDES, C., 1996, Cytochromes P450: Metabolic and Toxicological Aspects (Boca Raton: CRC Press). IRIBARNE, C., DREANO, Y., BARDOU, G., MENEZ, J. F. and BERmou, F., 1997, Interaction of methadone with substrates of human hepatic cytochrome P450. Toxicology, 117, 13–23.
   Web of Science ®Google Scholar
• ITOH, SATOH, M., ABE, Y., HASHIMOTO, H., YANAGAMITO, T. and KAMATAKI, T., 1994, A novel form of mouse cytochrome P450 3A (Cyp3a-16): its cDNA cloning and expression in fetal liver. European Journal of Biochemistry, 226, 877–882.
   Google Scholar
• ITOH, S., YANAGIMOTO, T., TAGAWA, S., HASHIMOTO, H., KITAMURA, R., NAKAJIMA, Y., °KOCHI, T., FUJIMOTO, S., UCHINO, J. and KAMATAKI, T., 1992, Genomic organization of human fetal specific P-45011IA7 (cytochrome P-45 OHFLa)-related gene(s) and interaction of transcriptional regulatory factor with its DNA element in the 5' flanking region. Biochimica et Biophysica Acta, 1130, 133–138.
   Google Scholar
• JANTZEN, H.M., STRAHLE, U., GLOSS, B., STEWART, F., SCHMID, W., BOSHART, M., MIKSICEK, R. and SCHUTZ, G., 1987, Cooperativity of glucocorticoid response elements located far upstream of the tyrosine aminotransferase gene. Cell, 49, 29–38.
   PubMed Web of Science ®Google Scholar
• JENKINS, B. D., PULLEN, C. B. and DARIMONT, D., 2001, Novel glucocorticoid receptor coactivator mechanisms. Trends in Endocrinology and Metabolism, 12, 122–126.
   PubMed Web of Science ®Google Scholar
• JOUNAIDI, Y., GUZELIAN, P. S., MAUREL, P. and VILAREM, M. J., 1994, Sequence of the 5'-flanking region of CYP3A5 — comparative-analysis with CYP3A4 and CYP3A7. Biochemical and Biophysical Research Communications, 205, 1741–1747.
   PubMed Web of Science ®Google Scholar
• JOVER, R., BORT, R., GOMEZ-LECHON, M. and CASTELL, J., 2001, Cytochrome P450 regulation by hepatocyte nuclear factor 4 in human hepatocytes: a study using adenovirus-mediated antisense targeting. Hepatology, 33, 668–675.
   Google Scholar
• KAWAMOTO, T., SUEYOSHI, T., ZELCO, I., MOORE, R., WASGBURN, K. and NEGISHI, M., 1999, Phenobarbitone-responsive nuclear translocation of the receptor CAR in induction of the Cyp2b gene. Molecular and Cell Biology, 19, 6318–6322.
   Web of Science ®Google Scholar
• KITADA, M., KAMATAKI, T., ITAHASHI, K., RIKIHISI, M., KATO, R. and KANAKUBO, Y., 1995, Purification and properties of cytochrome P450 from homogenates of human fetal livers. Archives of Biochemistry and Biophysics, 241, 275–280.
   Web of Science ®Google Scholar
• 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. and LEHMANN, J. M., 1998, An orphan nuclear receptor activated by pregnanes defines a novel steroid signalling pathway. Cell, 92, 73–82.
   PubMed Web of Science ®Google Scholar
• KOCAREK, T. A., SCHUETZ, E. G., STROM, S. C., FISHER, R. A. and GUZELIAN, P. S., 1995, Comparative-analysis of cytochrome P4503A induction in primary cultures of rat, rabbit, and human hepatocytes. Drug Metabolism and Disposition, 23, 415–421.
   PubMed Web of Science ®Google Scholar
• KOLARS, J. C., LOWN, K. S., SCHMIEDLINREN, P., GHOSH, M., FANG, C., WRIGHTON, S. A., MERION, R. M. and WATKINS, P. B., 1994, CYP3A gene-expression in human gut epithelium. Pharmacogenetics, 4, 247–259.
   PubMedGoogle Scholar
• KOLARS, J. C., SCHMIEDLINREN, P., SCHUETZ, J. D., FANG, C. and WATKINS, P. B., 1992, Identification of rifampin-inducible P4501I1A4 (CYP3A4) in human small-bowel enterocytes. Journal of Clinical Investigation, 90, 1871–1878.
   Web of Science ®Google Scholar
• KOMORI, M., HASHIZUME, T., OHI, H., MIURA, T., KITADA, M., NAGASHIMA, K. and KAMATAKI, T., 1998, Cytochrome P450 in human liver microsomes: high performance liquid chromatographic isolation of three forms and their characterisation. Journal of Biochemistry, 104, 912–916.
   Web of Science ®Google Scholar
• KOMORI, M. and ODA, Y., 1994, A major glucocorticoid-inducible P450 in rat liver is not P450 3A1. Journal of Biochemistry, 116, 114–120.
   PubMed Web of Science ®Google Scholar
• KUEHL, P., ZHANG, J., LIN, Y., LANBA, J., ASSEM, M., SCHEUTZ, J., WATKINS, P., DALY, A., WRIGHTON, S., HALL, S., MAUREL, P., RELLING, M., BRIMER, C., YASUDA, K., VENKATARAMANAN, R., STROM, S., THUMMEL, K., BOGUSKI, M. and SCHUETZ, E., 2001, Sequence diversity in CYP3A promoters and characterisation of the genetic basis of polymorphic CYP3A5 expression. Nature Genetics, 27, 383–391.
   PubMed Web of Science ®Google Scholar
• LANGE, B., BALNY, C. and MAUREL, P., 1984, Inductive and repressive effects of rifampicin on rabbit liver microsomal cytochrome P450. Biochemical Pharmacology, 33, 2771–2776.
   PubMed Web of Science ®Google Scholar
• LARSEN, M. C., BRAKE, P. B., PARMAR, D. and JEFCGATE, C. R., 1994, The induction of five rat hepatic P450 cytochromes by phenobarbital and similarly acting compounds is regulated by a sexually dimorphic, dietary-dependent endocrine factor that is highly strain specific. Archives of Biochemistry and Biophysics, 315, 24–34.
   PubMed Web of Science ®Google Scholar
• LE CLUYSE, E. L., 2001a, Pregnane X receptor: molecular basis for species differences in CYP3A induction by xenobiotics. Chemico-Biological Interactions, 134, 283–289.
   PubMed Web of Science ®Google Scholar
• LE CLUYSE, E. L., 2001b, Human hepatocyte culture systems for the in vitro evaluation of cytochrome P450 expression and regulation. European Journal of Pharmaceutical Sciences, 13, 343–368.
   PubMed Web of Science ®Google Scholar
• LEHMANN, J. M., McKEE, D. D., WATSON, M. A., WILLSON, T. M., MOORE, J. T. and KLIEWER, S. A., 1998, The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. Journal of Clinical Investigation, 102, 1016–1023.
   PubMed Web of Science ®Google Scholar
• LI, A. P., KAMINSKI, L. and RASMUSSEN, A., 1995, Substrates of human hepatic cytochrome P450 3A4. Toxicology, 104, 1–8.
   PubMed Web of Science ®Google Scholar
• LI, J., NING, G. and DUNCAN, S., 2000, Mammalian hepatocyte differentiation requires the transcription factor HNF-4 alpha. Genes and Development, 14, 464–474.
   PubMed Web of Science ®Google Scholar
• LIDDLE, C., GOODWIN, B. J., GEORGE, J., TAPNER, M. and FARRELL, G. C., 1998, Separate and interactive regulation of cytochrome P450 3A4 by triiodothyronine, dexamethasone, and growth hormone in cultured hepatocytes. Journal of Clinical Endocrinology and Metabolism, 83, 2411–2416.
   PubMed Web of Science ®Google Scholar
• LOWN, K. S., KOLARS, J. C., THUMMEL, K. E., BARNETT, J. L., KUNZE, K. L., WRIGHTON, S. A. and WATKINS, P. B., 1994, Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small-bowel — lack of prediction by the erythromycin breath test. Drug Metabolism and Disposition, 22, 947–955.
   PubMed Web of Science ®Google Scholar
• LUCEY, M. R., KOLARS, J. C., MERION, R. M., CAMPBELL, D. A., ALDRICH, M. and WATKINS, P. B., 1990, Cyclosporin toxicity at therapeutic blood levels and cytochrome P4503A. Lancet, 335, 11–15.
   PubMed Web of Science ®Google Scholar
• MASUYAMA, H., HIRAMATSU, Y., KUNITOMI, M., KUDO, T. and MACDONALD, P. N., 2000, Endocrine disrupting chemicals, phthalic acid and nonylphenol activate pregnane X receptor-mediated transcription. Molecular Endocrinology, 14, 421–428.
   PubMed Web of Science ®Google Scholar
• MASUYAMA, H., HIRAMATSU, Y., MIZUTANI, Y., INosurrA, H. and KUDO, T., 2001, The expression of pregnane X receptor and its target gene, cytochrome P450 3a1, in perinatal mouse. Molecular and Cellular Endocrinology, 172, 47–56.
   PubMed Web of Science ®Google Scholar
• MEYER, U. and ZANGER, U., 1997, Molecular mechanisms of genetic polymorphisms of drug metabolism. Annual Review of Pharmacology and Toxicology, 37, 269–296.
   PubMed Web of Science ®Google Scholar
• MIYATA, M., NAGATA, K., YAMAZOE, Y. and KATO, R., 1991, A gene structure of testosterone 6 beta-hydroxylase (P450IIIA). Biochemical and Biophysical Research Communications, 31, 68–73.
   Web of Science ®Google Scholar
• MIYATA, M., NAGATA, K., YAMAZOE, Y. and KATO, R., 1995, Transcriptional elements directing a liver-specific expression of P450/6 beta A (CYP3A2) gene-encoding testosterone 6 beta-hydroxylase. Archives of Biochemistry and Biophysics, 318, 71–79.
   PubMed Web of Science ®Google Scholar
• MOORE, L. B., PARKS, D. J., JONES, S. A., BLEDSOE, R. K., CONSLER, T. G., STI MME L, J. B., GOODW IN, B., LIDDLE, C., BLANCHARD, G., WILLSON, T. M., COLLINS, J. L. and KLIEWER, S. A., 2000, Orphan nuclear receptors CAR and PXR share xenobiotic and steroid ligands. Journal of Biological Chemistry, 275, 15122–15127.
   PubMed Web of Science ®Google Scholar
• MUANGMOONCHAI, R., SMIRLIS, D., WONG, S. C., EDWARDS, M., PHILLIPS, I. R. and SHEPHARD, E. A., 2001, Xenobiotic induction of cytochrome P4502b1 (CYP2B1) is mediated by the orphan nuclear receptor constitutive androstane receptor (CAR) and requires steroid co-activator 1 (src-1) and the transcription factor spl. Biochemical Journal, 355, 71–78.
   PubMed Web of Science ®Google Scholar
• MUENIER, V., BOURRIE, M., BERGER, Y. and FABRE, G., 1995, The human intestinal epithelial cell line Caco- 2: pharmacological and pharmacokinetic applications. Cell Biology and Toxicology, 11, 187–194.
   PubMed Web of Science ®Google Scholar
• NEGISHI, M. and HONKAKOSKI, P., 2000, Induction of drug metabolism by nuclear receptor CAR: molecular mechanisms and implications for drug research. European Journal of Pharmaceutical Sciences, 11, 259–264.
   PubMed Web of Science ®Google Scholar
• NELSON, D. R., KOYMANS, L., KAMATAKI, T., STEGEMAN, J. J., FEYEREISEN, R., WAXMAN, D. J., WATERMAN, M. R., GOTOH, O., COON, M. J., ESTABROOK, R. W., GUNSALUS, I. C. and NEBERT, D. W., 1996, P450 superfamily: update on new sequences, gene mapping, accession numbers and nomenclature. Pharmacogenetics, 6, 1–42.
   PubMedGoogle Scholar
• NEWTON, D. J., WANG, R. W. and Lu, A. Y. H., 1994, Cytochrome P450 inhibitors: evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes. Drug Metabolism and Disposition, 23, 154–158.
   Web of Science ®Google Scholar
• NUCLEAR RECEPTOR NOMENCLATURE COMMITTEE, 1999, A unified nomenclature system for the nuclear receptor superfamily. Cell, 97, 161–163.
   PubMed Web of Science ®Google Scholar
• OGG, M., WILLIAMS, J., TARBIT, M., GOLDFARB, P., GRAY, T. and GIBSON, G., 1999, A reporter gene assay to assess the molecular mechanisms of xenobiotic-dependent induction of the human CYP3A4 gene in vitro. Xenobiotica, 29, 269–279.
   PubMed Web of Science ®Google Scholar
• OGINO, M., NAGATA, K., MIYATA, M. and YAMAZOE, Y., 1999, Hepatocyte nuclear factor 4-mediated activation of rat CYP3A1 gene and its modes of modulation by apolipoprotein Al regulatory protein 1 and v-erba-related protein 3. Archives of Biochemistry and Biophysics, 362, 32–37.
   PubMed Web of Science ®Google Scholar
• OHMORI, S., NAKASA, H., ASANOME, K., KUROSE, Y., IsHii, I., HOSOKAWA, M. and KITADA, M., 1998, Differential catalytic properties in metabolism of endogenous and exogenous substrates among CYP3A enzymes expressed in cos-7 cells. Biochimka et Biophysica Ada, 1380, 297–304.
   PubMed Web of Science ®Google Scholar
• OZDEMIR, V., KALOW, W., TANG, BK., PATERSON, A., WALKER, S., ENDRENYI, L. and KASHUB A., 2000, Evaluation of the genetic component of variability in CYP3A4 activity: a repeated drug administration method. Pharmacogenetics, 10, 373–388.
   PubMedGoogle Scholar
• PAINE, M. F., KHALIGHI, M., FISHER, J. M., SHEN, D. D., KUNZE, K. L., MARSH, C. L., PERKINS, J. D. and THUMMEL, K. E., 1997, Characterisation of inter- and intra-intestinal differences in human CYP3A-mediated metabolism. Journal of Pharmacology and Experimental Therapeutics, 283, 1552–1562.
   PubMed Web of Science ®Google Scholar
• PARIANTE, C. M., PEARCE, B. D., PISELL, T. L., Su, C. and MILLER, A. H., 2001, The steroid receptor antagonists RU40555 and RU486 activate glucocorticoid receptor translocation and are not excreted by the by the steroid hormones transporter in L929 cells. Journal of Endocrinology, 169, 309–320.
   PubMed Web of Science ®Google Scholar
• PASCUSSI, J., JOUNAIDI, Y., DROCOURT, L., DOMERGUE, J., BALABAUD, C., MAUREL, P. and VILARE M., 1999, Evidence for the presence of a functional pregnane X receptor response element in the CYP3A7 promoter gene. Biochemical and Biophysical Research Communications, 260, 377–381.
   PubMed Web of Science ®Google Scholar
• PASCUSSI, J.-M., DROCOURT, L., FABRE, J.-M., MAUREL, P. and VILAREM, M. J, 2000a, Dexamethasone induces pregnane X receptor and retinoid X receptor-a expression in human hepatocytes: synergistic increase of CYP3A4 induction by pregnane X receptor. Molecular Pharmacology, 58, 361–372.
   PubMed Web of Science ®Google Scholar
• PASCUSSI, J. M., GERBAL-CHALOIN, S., FABRE, J. M., MAUREL, P. and VILAREM, M. J., 2000b, Dexamethasone enhances constitutive androstane receptor expression in human hepatocytes: consequences on cytochrome P450 gene regulation. Molecular Pharmacology, 58, 1441–1450.
   Google Scholar
• PASCUSSI, J. M., GERBAL-CHALOIN, S., PICHARD-GARCIA, L., DAUJAT, M., FABRE, J. M., MAUREL, P. and VILAREM, M. J., 2000c, Interleukin-6 negatively regulates the expression of pregnane X receptor and constitutively activated receptor in primary human hepatocytes. Biochemical and Biophysical Research Communications, 274, 707–713.
   Google Scholar
• PAULUSSEN, A., LAVRIJSEN, K., BOHETS, H., HENDRICKX, J., VERSASSELT, P., LUYTEN, W. and KONINGS, F., 2000, Two linked mutations in transcriptional regulatory elements of the CYP3A5 gene constitute the major genetic determinant of polymorphic activity in humans. Pharmacogentics, 10, 415–424.
   PubMedGoogle Scholar
• PEREIRA, T. M., CARLSTEDT-DUKE, J., LECKNER, M. C. and GUSTAFSSON, J. A., 1998, Identification of a functional glucocorticoid response element in the CYP3A1/igc2 gene. DNA and Cell Biology, 17, 39–49.
   Google Scholar
• PICARD, D. and YAmAmom, K. R., 1987, Two signals mediate hormone-dependent nuclear localization of the glucocorticoid receptor. EMBO Journal, 6, 3333–3340.
   PubMed Web of Science ®Google Scholar
• PICKWELL, G. V., QUATTROCHI, L. C., SHIH, H. and GUZELIAN, P. S., 1996, Transcriptional activation of human fetal cytochrome P450 CYP3A7. FASEB Journal, 10, 1346.
   Web of Science ®Google Scholar
• PLANT, N., OGG, M., CROWDER, M. and GIBSON, G., 2000, Control and statistical analysis of in vitro reporter gene assays. Analytical Biochemistry, 278, 170–174.
   PubMed Web of Science ®Google Scholar
• POWELL, W. A., MITCHELL, B. F. and CHALLIS, J. R., 1986, Effect of steroids on progesterone output by explants of human chorion. Gynecological and Obstetrk Investigation, 22, 64–72.
   PubMed Web of Science ®Google Scholar
• PRATT, W. B., 1993, The role of heat shock proteins in regulating the function, folding and trafficking of the glucocorticoid receptor. Journal of Biological Chemistry, 268, 21455–21458.
   PubMed Web of Science ®Google Scholar
• QUATTROCHI, L. and GUZELIAN, P., 2001, CYP3A regulation: from pharmacology to nuclear receptors. Drug Metabolism and Disposition, 29, 615–622.
   PubMed Web of Science ®Google Scholar
• QUATTROCHI, L. C., MILLS, A. S., BARWICK, J. L., YOCKEY, C. B. and GUZELIAN, P. S., 1995, A novel cis-acting element in a liver cytochrome-P450 3A gene confers synergistic induction by glucocorticoids plus antiglucocorticoids. Journal of Biological Chemistry, 270, 28917–28923.
   PubMed Web of Science ®Google Scholar
• REBBECK, T., JAFFE, J., WALKER, A., VEIN, A. and MALKOWICZ, S., 1998, Modification of clinical presentation of prostate tumours by a novel genetic variant in CYP3A4. Journal of the National Cancer Institute, 90, 1225–1230.
   PubMed Web of Science ®Google Scholar
• RIVORY, L. P., QIN, H., CLARKE, S. J., ERIS, J., DUGGIN, G., Ray, E., TRENT, R. J., BISHOP, J. F., 2000, Frequency of cytochrome P450 3A4 variant genotype in transplant population and lack of association with cyclosporin clearance. European Journal of Clinical Pharmacology, 56, 395–398.
   PubMed Web of Science ®Google Scholar
• ROBERTSON, G., GOODWIN, B., FIELD, J. and LIDDLE, C., 2000, Transgenic mouse models of CYP3A4 regulation. In 13th International Symposium on Microsonzes and Drug Oxidations, Stresa, Italy, abst 46.
   Google Scholar
• SAKUMA, T., TAKAI, M., ENDO, Y., KUROIWA, M., OHARA, A., JARUKAMJORN, K., HONMA, R. and NEMOTO, N., 2000, A novel female-specific member of the CYP3A gene subfamily in the mouse liver. Archives of Biochemistry and Biophysics, 377, 153–162.
   PubMed Web of Science ®Google Scholar
• SATA, F., SAPONE, A., ELIZONDO, G., STOCKER, P., MILLER, V., ZHENG, W., RAUNIO, H., CRESPI, C. and GONZALEZ, F., 2000, CYP3A4 allelic variants with amino acid substitutions in exons 7 and 12: evidence for an allelic variant with altered catalytic activity. Clinical Pharmacology and Therapeutics, 67, 48–56.
   PubMed Web of Science ®Google Scholar
• SAVAS, U., GRIFFEN, K. and JOHNSON, E., 1999, Molecular mechanisms of cytochrome P450 induction by xenobiotics: an expanded role for nuclear hormone receptors. Molecular Pharmacology, 56, 851–857.
   PubMed Web of Science ®Google Scholar
• SAVAS, U., WESTER, M. R., GRIFFIN, K. J. and JOHNSON, E. F., 2000, Rabbit pregnane X receptor is activated by rifampicin. Drug Metabolism and Disposition, 28, 529–537.
   PubMed Web of Science ®Google Scholar
• SCHUETZ, E. G., BRIMER, C. and SCHEUTZ, J. D., 1998, Environmental xenobiotics and the antihormones cyproterone acetate and spironolactone use the nuclear hormone pregnane X receptor to activate the CYP3A23 hormone response element. Molecular Pharmacology, 54, 1113–1117.
   PubMed Web of Science ®Google Scholar
• SCHUETZ, E. G. and GUZELIAN, P. S, 1984, Induction of cytochrome P-450 by glucocorticoids in rat liver. II. Evidence that glucocorticoids regulate induction of cytochrome P-450 by a non-classical receptor mechanism. Journal of Biological Chemistry, 259, 2007–2012.
   PubMed Web of Science ®Google Scholar
• SCHUETZ, E. G., SCHINKEL, A. H., RELLING, M. V. and SCHUETZ, J. D., 1996b, P-glycoprotein: a major determinant of rifampicin-inducible expression of cytochrome P450 3A in mice and humans. Proceedings of the National Academy of Sciences, USA, 93, 4001–4005.
   PubMed Web of Science ®Google Scholar
• SCHUETZ, E., SCHMID, W., SCHUTZ, G., BRIMER, C., YASUDA, K., KAMATAKI, T., BORNHEIM, L., MYLES, K. and COLE, T., 2000, The glucocorticoid receptor is essential for induction of cytochrome P-450 2b by steroids but not for drug or steroid induction of cyp3a or P-450 reductase in mouse liver. Drug Metabolism and Disposition, 28, 268–277.
   PubMed Web of Science ®Google Scholar
• SCHUETZ, E. G., SCHUETZ, J. D., STROM, S. C., THOMPSON, M. T., FISHER, R. A., MOLOWA, D. T., Li, D. and GUZELIAN, P. S., 1993, Regulation of human liver cytochromes P-450 in family 3A in primary and continuous-culture of human hepatocytes. Hepatology, 18, 1254-1 262.
   Google Scholar
• SCHUETZ, J., BEACH, D. and GUZELIAN, P., 1994, Selective expression of cytochrome P450 CYP3A mRNA's in embryonic and adult human liver. Pharmacogenetics, 4, 11–20.
   PubMedGoogle Scholar
• SCHUETZ, J. D. and GUZELIAN, P. S., 1995, Isolation of CYP3A5p cDNA from human liver — a reflection of a novel cytochrome P-450 pseudogene. Biochimica et Biophysica Ada, 1261, 161–165.
   PubMed Web of Science ®Google Scholar
• SCHUETZ, J. D., SCHUETZ, E. G., THOTTASSERY, J. V., GUZELIAN, P. S., STROM, S. and SUN, D., 1996a, Identification of a novel dexamethasone responsive enhancer in the human CYP3A5 gene and its activation in human and rat liver cells. Molecular Pharmacology, 49, 63–72.
   PubMed Web of Science ®Google Scholar
• SHIMADA, T., YAMAZAKI, H., MIMURA, M., INUI, Y. and GUENGERICH, F., 1994, Interindividual variations in human liver cytochrome P450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals — studies with liver microsomes of 30 Japanese and 30 Caucasians. Journal of Pharmacology and Experimental Therapeutics, 270, 414–423.
   PubMed Web of Science ®Google Scholar
• SMIRLIS, D., MUANGMOONCHAI, R., EDWARDS, M., PHILLIPS, I. R. and SHEPHARD, E. A., 2001, Orphan receptor promiscuity in the induction of cytochromes P450 by xenobiotics. Journal of Biological Chemistry, 276, 12822–12826.
   PubMed Web of Science ®Google Scholar
• SMITH, D. A., ABEL, S. M., HYLAND, R. and JoNEs, B. C., 1998, Human cytochrome P450s: selectivity and measurement in vivo. Xenobiotica, 28, 1095–1128.
   PubMed Web of Science ®Google Scholar
• SMITH, D. A., 2000, Induction and drug development. European Journal of Pharmaceutical Sciences, 11, 185–189.
   PubMed Web of Science ®Google Scholar
• SONDERFAN, A. J., ARLOTTO, M. P., DUTTON, D. R., MCMILLAN, S. K. and PARKINSON, A., 1987, Regulation of testosterone hydroxylation by rat liver microsomal cytochrome P450. Archives of Biochemistry and Biophysics, 255, 27–41.
   PubMed Web of Science ®Google Scholar
• STAUDINGER, J., GOODWIN, B., JONE S., HAWKINS-BROWN, D., MACKENZIE, K., LATouE, A., Liu, Y., KLAASSEN, C., BROWN, K., REINHARD, J., WILLSON, T., KOLLER, B. and KLIEWER, S., 2001, The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proceedings of the National Academy of Sciences, USA, 98, 3369–3374.
   Google Scholar
• STROM, A., WESTIN, S., EGUCHI, H., GUSTAFSSON, J. A. and MODE, A., 1995, Characterization of orphan nuclear receptor binding elements in sex-differentiated members of the CYP2C gene family expressed in rat liver. Journal of Biological Chemistry, 12, 11276–11281.
   Web of Science ®Google Scholar
• SUEYOSHI, T., KAWAMOTO, T., ZELCO, I., HONKAKOWSKI, P. and NEGISHI, M., 1999, The repressed nuclear receptor CAR responds to phenobarbital in activating the human CYP2B6 gene. Journal of Biological Chemistry, 274, 6043–6046.
   PubMed Web of Science ®Google Scholar
• SUEYOSHI, T. and NEGISHI, M., 2001, Phenobarbitone response elements of cytochrome P450 genes and nuclear receptors. Annual Review of Pharmacology and Toxicology, 41, 123–143.
   PubMed Web of Science ®Google Scholar
• SZKLARZ, G. D. and HALPERT, J. R., 1997, Molecular modelling of cytochrome P450 3A4. Journal of Computer Aided Molecular Design, 11, 265–272.
   PubMed Web of Science ®Google Scholar
• TAYLOR, W. and LESNA, M., 1997, The hepatotoxicity of lithocholic acid in male mice. British Journal of Pharmacology, 61, 133–134.
   Google Scholar
• TELHADA, M. B., PEREIRA, T. M. and LECHNER, M. C., 1992, Effect of dexamethasone and phenobarbital on run-on transcription rate and CYP3A mRNA concentration in rat liver: changes during development. Archives of Biochemistry and Biophysics, 298, 715–725.
   PubMed Web of Science ®Google Scholar
• THUMMEL, K. E., LEE, C. A., KUNZE, K. L., NELSON, S. D. and SLATTERY, J. T., 1993, Oxidation of acetaminophen to N-acetyl-p-aminobenzoquinoneirnine by human CYP3A4. Biochemical Pharmacology, 45, 1563–1569.
   PubMed Web of Science ®Google Scholar
• THUMMEL, K. E., SHEN, D. D., PODOLL, T. D., KUNZE, K. L., TRAGER, W. F., Racciii, C. E., MARSH, C. L., McVicAk, J. P., BARR, D. M., PERKINS, J. D. and CARITHERS, R. L., 1994, Use of midazolam as a human cytochrome P4503A probe. 2. Characterization of interindividual and intraindividual hepatic CYP3A variability after liver-transplantation. Journal of Pharmacology and Experimental Therapeutics, 271, 557–566.
   PubMed Web of Science ®Google Scholar
• Tow', T., NAKAI, D., NAKAGOMI, R., Yawo, H., ABE, T. and SUGIYAMA, Y., 1999, Pravastatin, an HMG-CoA reductase inhibitor, is transported by rat organic anion transporting polypeptide, OATP-2. Pharmaceutical Research, 16, 904–9088.
   Google Scholar
• TUCKER, G. T., ROSTAMI-HODJEGAN, A. and JACKSON, P. R., 1998, Determination of drug-metabolizing enzyme activity in vivo: pharmacokinetic and statistical issues. Xenobiotica, 28, 1255–1273.
   Google Scholar
• TZAMELI, I. and MOORE, D. D., 2001, Role reversal: new insights from new ligands for the xenobiotic receptor CAR. Trends in Endocrinology and Metabolism, 12, 7–10.
   Google Scholar
• TZAMELI, I., Pissios, P., So-ourz, E. G. and MOORE, D. D., 2000, The xenobiotic compound 1,4-bis[3,5- dichloropyridyloxy)] benzene is an agonist ligand for the nuclear receptor CAR. Molecular and Cell Biology, 20, 2951–2958.
   Google Scholar
• VENKATESAN, K., 1992, Pharmacokinetic drug-interactions with rifampicin. Clinical Pharmacokinetics, 22, 47–65.
   PubMed Web of Science ®Google Scholar
• WALKER, A. H., JAFFE, J. M., GUNASEGARAM, S., CUMMINGS, S. A., HUANG, C. S., CHERN, H. D., OLOPADE, O. I., WEBER, B. L. and REBBECK, T. R., 1998, Characterization of an allelic variant in the nifedipine-specific element of CYP3A4: ethnic distribution and implications for prostate cancer risk. Human Mutation, 12, 289.
   PubMedGoogle Scholar
• WAN, Y.U. Y., AN, D., CAI, Y., REPA, J., CHEN, T. H.-P., FLORES, M., POSTIC, C., MAGNUSON, M., CHEN, J., CHIEN, K., FRENCH, S., MANGELSDORF, D. and Sucov, H., 2000, Hepatocyte-specific mutation establishes retionid X receptor as a heterodimeric integrator of multiple physiological processes in the liver. Molecular and Cellular Biology, 20, 4436–4444.
   Google Scholar
• WANG, J. C., STAFFORD, J. M. and GRANNER, D. K., 1998, SRC-1 and GRIP1 coactivate transcription with hepatocyte nuclear factor 4. Journal of Biological Chemistry, 273, 30847–30850.
   PubMed Web of Science ®Google Scholar
• WATKINS, P., 1994, Noninvasive tests of CYP3A enzymes. Pharmacogenetics, 4, 171–184.
   PubMedGoogle Scholar
• WATKINS, P., MURRAY, S., WINKELMAN, L., HEUMAN, D., WRIGHTON, S. and GUZELIAN, P., 1988, Erythromycin breath test as an assay of glucocorticoid-inducible liver cytochromes P45 O. Journal of Clinical Investigation, 83, 688–697.
   Web of Science ®Google Scholar
• WATKINS, P. B., WniuirroN, S. A., Soiuwrz, E. G., MAUREL, P. and GUZELIAN, P. S., 1986, Macrolide antibiotics inhibit the degradation of the glucocorticoid-responsive cytochrome P-450p in rat hepatocytes in vivo and in primary monolayer- culture. Journal of Biological Chemistry, 261, 6264–6271.
   PubMed Web of Science ®Google Scholar
• WATKINS, R. E., WISELY, G. B., MOORE, L. B., COLLINS, J. L., LAMBERT, M. H., WILLIAMS, S. P., WILLSON, T. M., KLIEWER, S. A. and REDINBO, M. R., 2001, The human nuclear xenobiotic receptor PXR: structural determinants of directed promiscuity. Science, 292, 2329–2333.
   PubMed Web of Science ®Google Scholar
• WAXMAN, D. J., 1999, P450 gene induction by structurally diverse xenochemicals: central role of nuclear receptors CAR, PXR and PPAR. Archives of Biochemistry and Biophysics, 369, 11–23.
   PubMed Web of Science ®Google Scholar
• WEAVER, R. J., 2001, Assessment of drug—drug interactions: concepts and approaches. Xenobiotica, 31, 499–538.
   PubMed Web of Science ®Google Scholar
• WEI, P., ZHANG, J., EGAN-HAFLEY, M., LIANG, S. G. and MOORE, D. D., 2000, The nuclear receptor CAR mediates specific xenobiotic induction of drug metabolism. Nature, 407, 920–923.
   Google Scholar
• WESTLIND, A., LOFBERG, L., TINDBERG, N., ANDERSSON, T. B. and INGELMAN-SUNDBERG, M., 1999, Interindividual differences in hepatic expression of CYP3A4: relationship to genetic polymorphism in the 5'-upstream regulatory region. Biochemical and Biophysical Research Communications, 259, 201–205.
   Google Scholar
• WESTLIND, A., MALMEBO, S., JOHANSSON, I., OTTER, C., ANDERSSON, T. B., INGELMAN-SUNDBERG, M. and OSCARSON, M., 2001, Cloning and tissue distribution of a novel human cytochrome P450 of the CYP3A subfamily, CYP3A43. Biochemical and Biophysical Research Communications, 281, 1349–1355.
   Google Scholar
• WILKINSON, G. R., 1996, Cytochrome P4503A (CYP3A) metabolism: prediction of in vivo activity in humans. Journal of Pharmacokinetks and Biopharmaceutks, 24, 475–490.
   PubMedGoogle Scholar
• WORBOYS, P. D. and CAROLE, D. J., 2001, Implications and consequences of enzyme induction on preclinical and clinical drug development. Xenobiotica, 31, 539–556.
   PubMed Web of Science ®Google Scholar
• WRIGHT, M. C. and PAINE, A. J., 1994, Induction of the cytochrome P450 3A subfamily in rat liver correlates with the binding of inducers to a microsomal protein. Biochemical and Biophysical Research Communications, 201, 973–979.
   PubMed Web of Science ®Google Scholar
• WRIGHT, M. C., WANG, X. J., PIMENTA, M., RIBEIRO, V., PAINE, A. J. and LECHNER, M. C., 1996, Glucocorticoid receptor-independent transcriptional induction of cytochrome P450 3A1 by metyrapone and its potentiation by glucocorticoid. Molecular Pharmacology, 50, 856–863.
   PubMed Web of Science ®Google Scholar
• WRIGHTON, S. A., BRIAN, W. R., SARI, M. A., IwAsAxi, M., OUENGERICH, F. P., RAUCY, J. L., MoLowa, D. T. and VANDENBRANDEN, M., 1990, Studies on the expression and metabolic capabilities of human liver cytochrome P451I1A5 (h1p3). Molecular Pharmacology, 38, 207–213.
   PubMed Web of Science ®Google Scholar
• WRIGHTON, S. A., RING, B. J., WATKINS, P. B. and VAN DEN BRANDEN, M., 1989, Identification of a polymorphically expressed member of the human cytochrome P-45011I family. Molecular Pharmacology, 36, 97–105.
   Google Scholar
• WRIGHTON, S. A., SCHUETZ, E. G., THUMMEL, K. E., SHEN, D. D., KORZEKWA, P. B. and WATKINS, P. B., 2000, The human CYP3A subfamily: practical considerations. Drug Metabolism Reviews, 32, 339–362.
   PubMed Web of Science ®Google Scholar
• WRIGHTON, S. A. and VAN DEN BRANDEN, M., 1989, Isolation and characterisation of human liver fetal liver cytochrome P45OHLp2: a third member of the P450III gene family. Archives of Biochemistry and Biophysics, 268, 144–151.
   Google Scholar
• XIE, W., BARWICK, J., SIMMON, C., PIERCE, A., SAFE, S., BLUMBERG, B., OUZELIAN, P. and EVANS, R., 2000a, Reciprocal activation of xenobiotic response genes by nuclear receptors SXR/PXR and CAR. Genes and Development, 14, 3014–3023.
   PubMed Web of Science ®Google Scholar
• XIE, W., BARWICK, J. L., DOWNES, M., BLUMBERG, B., SIMON, C. M., NELSON, M. C., NEUSCHWANDER-TETRI, B. A., BRUNTK, E. M., OUZELIAN, P. S. and EVANS, R. M., 2000b, Humanized xenobiotic response in mice expressing nuclear receptor SXR. Nature, 406, 435–439.
   Google Scholar
• XIE, W., RADOMINSKA-PANDYA, A., SHI, Y., SIMON, C. M., NELSON, M. C., ONG, E. S., WAXMAN, D. J. and EVANS, R. M., 2001, An essential role for nuclear receptors SXR/PXR in detoxification of cholestatic bile acids. Proceedings of the National Academy of Sciences, USA, 98, 3375–3380.
   Google Scholar
• YANAGIMOTO, T., Prot', S., MULLER-ENOCH, D. and KAMATAKI, T., 1992, Mouse liver cytochrome P450(P-450111AM1): its cDNA cloning and inducibility by dexamethasone. Biochimka et Biophysica Ada, 1130, 319–332.
   Google Scholar
• YANAGIMOTO, T., Prot', S., SAWADA, M., HASHIMOTO, H. and KAMATAKI, T, 1994, Molecular cloning and functional expression of a mouse cytochrome P450 (Cyp3a13): examination of Cyp3a13 to activate aflatoxin B1. Biochimka et Biophyska Acta, 1201, 405–410.
   Google Scholar
• YANAGIMOTO, T., Prot', S., SAWADA, M. and KAMATAKI, T., 1997, Mouse cytochrome P450 (Cyp3A11): predominant expression in liver and capacity to activate aflatoxin B1. Archives of Biochemistry and Biophysics, 340, 215–218.
   Google Scholar
• YANG, H. Y., LEE, Q. P., RETTIE, A. E. and JucHwu, M. R., 1994, Functional cytochrome P4503A isoforms in human embryonic tissues: expression during organogenesis. Molecular Pharmacology, 46, 922–928.
   PubMed Web of Science ®Google Scholar
• ZELCO, I., SUEYOSHI, T., KAWAMOTO, T., MOORE, R. and NEGISHI, M., 2001, The peptide near the C-terminus regulates receptor CAR nuclear translocation induced by xenochemicals in mouse liver. Molecular and Cellular Biology, 21, 2838–2846.
   PubMed Web of Science ®Google Scholar
• ZHANG, H., LE CULYSE, E., Liu, L., Hu, M., MATONEY, L., Zito, W. and YAN, B., 1999, Rat pregnane X receptor: molecular cloning, tissue distribution and xenobiotic regulation. Archives of Biochemistry and Biophysics, 368, 14–22.
   PubMed Web of Science ®Google Scholar
• ZHAO, X. J. and Isitiz.uti, T., 1997, The in vitro hepatic metabolism of quinine in mice, rats and dogs: comparison with human liver microsomes. Journal of pharmacology and Experimental Therapeutics, 283, 1168–1176.
   Google Scholar