In vitro assessment of human cytochrome P450

Reference

• ABBOT, M. R. and GREEN, C. E., 1995, Cytochrome P450 isoforms in 26 human liver specimens. ISSX Proceedings, 8, 91.
   Google Scholar
• ANDERSSON, T., MINERS, J. 0., VERONESE, M. E., TASSANEEYAKUL W., MEYER, U. A. and BIRKETT, D. J., 1993, Identification of human liver cytochrome-P450 isoforms mediating omeprazole metabolism. British Journal of Clinical Pharmacology, 36, 521–530.
   Google Scholar
• ANDERSSON, T., MINERS, J. 0., VERONESE, M. E. and BIRKETT, D. J., 1994a, Identification of human liver cytochrome-P450 isoforms mediating secondary omeprazole metabolism. British Journal of Clinical Pharmacology, 37, 597–604.
   Google Scholar
• ANDERSSON, T., MINERS, J. 0., VERONESE, M. E. and BIRKETT, D. J., 1994b, Diazepam metabolism by human liver-microsomes is mediated by both S-mephenytoin hydroxylase and CYP3A isoforms. British Journal of Clinical Pharmacology, 38, 131–137.
   Google Scholar
• AOYAMA, T., GONZALEZ, F. J. and GELBOIN, H. V., 1989a, Human cDNA-expressed cytochrome P450 IA2: mutagen activation and substrate specificity. Molecular Carcinogenesis, 2, 192–198.
   PubMed Web of Science ®Google Scholar
• AOYAMA, T., YAMANO, S., WAXMAN, D. J., LAPENSON, D. P., MEYER, U. A., FISCHER, V., TYNDALE, R., INABA, T., KALOW, W. and GELBOIN, H. V., 1989b, Cytochrome P-450 hPCN3, a novel cytochrome P-450 IIIA gene product that is differentially expressed in adult human liver. cDNA and deduced amino acid sequence and distinct specificities of cDNA-expressed hPCN1 and hPCN3 for the metabolism of steroid hormones and cyclosporine. Journal of Biological Chemistry, 264, 10388–10395.
   PubMed Web of Science ®Google Scholar
• BACK, D. J., TEA, J. F., KARBWANG, J. and COLBERT, J., 1988, In vitro inhibition studies of tolbutamide hydroxylase activity of human liver microsomes by azoles, sulphonamides and quinolines. British Journal of Clinical Pharmacology, 26, 23–29.
   PubMed Web of Science ®Google Scholar
• BALDWIN, S. J., BLOOMER, J. C., SMITH, G. J., AYRTON, A. D., CLARICE, S. E. and CHENERY, R. J., 1995, Ketoconazole and sulfaphenazole as the respective selective inhibitors of P4503A and 2C9. Xenobiotica, 25, 261–270.
   PubMed Web of Science ®Google Scholar
• BALL, S. E., MAURER, G., ZOLLINGER, M., LADONA, M. and VICKERS, A. E., 1992, Characterization of the cytochrome P-450 gene family responsible for the N-dealkylation of the ergot alkaloid CQA 206-291 in humans. Drug Metabolism and Disposition, 20, 56–63.
   PubMed Web of Science ®Google Scholar
• BARDSLEY, W. G., LEFF, P., KAVANAGH, J. and WAIGHT, R., 1980, Deviations from Michaelis-Menten kinetics: The possibility of complicated curves for simple kinetic schemes and the computer fitting of experimental data for acetylcholinesterase, acid phosphatase, adenosine deaminase, arylsulphatase, benzylamine oxidase, chymotrypsin, fumarase, galactose dehydrogenase, )3-galactosidase, lactate dehydrogenase, peroxidase and xanthine oxidase. Biochemical Journal, 187, 739–765.
   PubMed Web of Science ®Google Scholar
• BARNES, H. J., ARLOTTO, M. P. and WATERMAN, M. R., 1991, Expression and enzymatic activity of recombinant cytochrome P450 17-hydroxylase in Escherichia coll. Proceedings of the National Academy of Sciences, USA 88, 5597–5601.
   PubMed Web of Science ®Google Scholar
• BEISCHLAG, T. V., KALOW, W. A., MAHON, W. A. and INABA, T., 1992, Diazepam metabolism by rat and human liver in vitro: inhibition by mephenytoin. Xenobiotica, 22, 559–567.
   PubMed Web of Science ®Google Scholar
• BERTHOU, F., FLINOIS, J. P., RATANASAVANH, D., BEAUNE, P., RICHE, C. and GUILLOUZO, A., 1991, Evidence for the involvement of several cytochromes P-450 in the first steps of caffeine metabolism by human liver microsomes. Drug Metabolism and Disposition, 19, 561–567.
   PubMed Web of Science ®Google Scholar
• BERTHOU, F., RATANASAVANH, D., RICHE, C., PICART, D., VOIRIN, T. and GUILLOUZO, A., 1989, Comparison of caffeine metabolism by slices, microsomes and hepatocyte cultures from adult human liver. Xenobiotica, 19, 401–417.
   PubMed Web of Science ®Google Scholar
• BIRGERSSON, C., MORGAN, E. T., JORNVALL, H. and VON BAHR, C., 1986, Purification of desmethyl-imipramine and debrisoquine hydroxylating cytochrome P450 from human liver. Biochemical Pharmacology, 35, 3165–3166.
   PubMed Web of Science ®Google Scholar
• BIRKETT, D. J., REES, D., ANDERSSON T., GONZALEZ, F. J., MINERS, J. 0. and VERONESE, M., 1994, In-vitro proguanil activation to cycloguanil by human liver-microsomes is mediated by CYP3A isoforms as well as by S-mephenytoin hydroxylase. British Journal of Clinical Pharmacology, 37, 413–420.
   Google Scholar
• BLOOMER, J. C., CLARKE, S. E. and CHENERY, R. J., 1995, Determination of P4501A2 activity in human liver-microsomes using [3-C-14-methyl] caffeine. Xenobiotica, 25, 917–927.
   PubMed Web of Science ®Google Scholar
• BRIAN, W. R., SRIVASTAVA, P. K., UMBENHAUER, D. R., LLOYD, R. S. and GUENGERICH, F. P., 1989, Expression of a human liver cytochrome P-450 protein with tolbutamide hydroxylase activity in Saccharomyces cerevisiae. Biochemistry, 28, 4993–4999.
   PubMed Web of Science ®Google Scholar
• BRIAN, W. R., SARI, M. A., IWASAKI, M., SHIMADA, T., KAMINSKY, L. S. and GUENGERICH, F. P., 1990, Catalytic activities of human liver cytochrome P-450 IIIA4 expressed in Saccharomyces cerevisiae. Biochemistry, 29, 11280–11292.
   PubMed Web of Science ®Google Scholar
• BROSEN, K., SIUELBO, E., RASMUSSEN, B. B., POULSEN, H. E. and Lovr,, S., 1993, Fluvoxamine is a potent inhibitor of cytochrome P4501A2. Biochemical Pharmacology, 45, 1211–1214.
   Google Scholar
• BURICE, M. D., THOMPSON, S., ELCOMBE, C. R., HALPERT, J., HAAPARANTA, T. and MAYER, R. T., 1985, Ethoxy-, pentoxy- and benzyloxyphenoxazones and homologues: a series of substrates to distinguish between different induced cytochromes P450. Biochemical Pharmacology, 34, 3337–3345.
   PubMed Web of Science ®Google Scholar
• BUTERS, J. T. M., KORZEKWA, K. R., KUNZE, K. L., OMATA, Y., HARDWICK, J. P. and GONZALEZ, F. J., 1994, cDNA-directed expression of human cytochrome-P450 CYP3A4 using baculovirus. Drug Metabolism and Disposition, 22, 688–692.
   Google Scholar
• BUTERS, J. T. M., SHOU, M. G., HARDWICK, J. P., KORZEKWA, K. R., GONZALEZ, F. J., SCHMAUX, W. A., BARRENSCHEEN, M., LANDS1EDEL, R., JANZOWSKI, C., EISENBRAND, G., GONZALEZ, F., ELIASSON E., INGELMANSUNDERG, M., PERCHERME1ER, M., GREIM, H. and DOEHMER, J., 1995, cDNA-directed expression of human cytochrome-P450 CYP1A1 using baculovirus—purification, de-pendency on NADPH-P450 oxidoreductase, and reconstitution of catalytic properties without purification Stable expression of human cytochrome-P450 2E1 in V79 chinese-hamster cells. European Journal of Pharmacology-Environmental Toxicology and Pharmacology Section, 293, 123–131.
   Google Scholar
• BUTLER, M. A., IWASAKI, M., GUENGERICH, F. P. and KADLUBAR, F. F., 1989, Human cytochrome P-450PA (P-450IA2), the phenacetin 0-deethylase, is primarily responsible for the hepatic 3-demethylation of caffeine and N-oxidation of carcinogenic arylamines. Proceedings of the National Academy of Sciences, USA, 86, 7696–7700.
   PubMed Web of Science ®Google Scholar
• CAMPBELL, M. E., GRANT, D. M., INABA, T. and KALO W., 1987, Biotransformation of caffeine, paraxanthine, theophylline and theobromine by polycyclic aromatic hydrocarbon-inducible cytochrome(s) P450 in human liver microsomes. Drug Metabolism and Disposition, 15, 237–249.
   PubMed Web of Science ®Google Scholar
• CARRIERE, V., GOASDUFF, T., RATANASAVANH, F. M., GAUTIER, J. C., GUILLOUZO, A., BEAUNE, P. and BERTHOU, F., 1993, Both cytochromes P450 2E1 and 1A1 are involved in the metabolism of chlorzoxazone. Chemical Research in Toxicology, 6, 852–857.
   PubMed Web of Science ®Google Scholar
• CASTLE, P. J., MERDINK, J. L., OKITA, J. R., WRIGHTON, S. A. and OKITA, R. T., 1995, Human liver lauric acid hydroxylase-activities. Drug Metabolism and Disposition, 23, 1037–1043.
   PubMed Web of Science ®Google Scholar
• CHANG, T. K., GONZALEZ, F. J. and WAXMAN, D. J., 1994, Evaluation of triacetyloleandomycin, alpha-naphthoflavone and diethyldithiocarbamate as selective chemical probes for inhibition of human cytochromes P450. Archives of Biochemistry and Biophysics, 311, 437–442.
   PubMed Web of Science ®Google Scholar
• CHANG, T. K., WEBER, G. F., CRESPI, C. L. and WAXMAN, D. J., 1993, Differential activation of cyclophosphamide and ifosphamide by cytochromes P-450 2B and 3A in human liver microsomes. Cancer Research, 53, 5629–5637.
   PubMed Web of Science ®Google Scholar
• CHIBA, K., SAITOH, A., KOYAMA, E., TAM, M., HAYASHI, M. and ISHIZAKI, T., 1994, The role of S-mephenytoin 4'-hydroxylase in imipramine metabolism by human liver-microsomes—a 2-enzyme kinetic-analysis of N-demethylation and 2-hydroxylation. British Journal of Clinical Pharmacology, 37, 237–242.
   PubMed Web of Science ®Google Scholar
• CHING, M. S., LENNARD, M. S., TUCKER, G. T., WOODS, H. F., KELLY, M. E. and KELLY, S. L., 1991, The expression of human cytochrome P450IA1 in the yeast Saccharomyces cerevisiae. Biochemical Pharmacology, 42, 753–758.
   PubMed Web of Science ®Google Scholar
• CHRISTOPHERSON, P. A., MANKOWSKI, D. C., TWEEDIE, D. J. and LAWTON, M. P., 1995, Expression of human cytochromes P450 in insect cells. ISS X Proceedings, 8, 358.
   Google Scholar
• CLARKE, S. E., AYRTON, A. D. and CHENERY, R. J., 1994a, Characterization of the inhibition of P4501A2 by furafylline. Xenobiotica, 24, 517–526.
   PubMed Web of Science ®Google Scholar
• CLARKE, S. E., BALDWIN, S. J., BLOOIVIER, J. C., AYRTON, A. D., Sozio, R. S. and CHENERY, R. J., 1994b, Lauric acid as a model substrate for the simultaneous determination of cytochrome-P450 2E1 and 4A in hepatic microsomes. Chemical Research in Toxicology, 7, 836–842.
   PubMed Web of Science ®Google Scholar
• COCHRAN, W. G. and Cox, G. M., 1957, Experimental Designs, 2nd edn (Chichester: John Wiley). CODE, E. L., CRESPI, C. L., PENMAN, B. W., GONZALEZ, F. J., CHANG, T. and WAXMAN, D. J., 1995, Immunochemical and enzymatic characterization of human hepatic levels of CYP2B6. ISSX Proceedings, 8, 100.
   Google Scholar
• COMBALBERT, J., FABRE, I., FABRE, G., DALET I., DERANCOURT, J., CANO, J. P. and MAUREL, P., 1989, Metabolism of cyclosporin A. IV. Purification and identification of the rifampicin-inducible human liver cytochrome P-450 (cyclosporin A oxidase) as a product of P450IIIA gene subfamily. Drug Metabolism and Disposition, 17, 197–207.
   Google Scholar
• CORNBLEET, P. J., 1979, Incorrect least-squares regression coefficients in method comparison analysis. Clinical Chemistry, 25, 432–438.
   PubMed Web of Science ®Google Scholar
• CRESPI, C. L., CODE, E. L., PENMAN, B. W. and WAXMAN, D. J., 1995a, An activity based method for integrating metabolism data from cDNA-expressed cytochrome P450 enzymes to the balance of enzymes in human liver microsomes. I SS X Proceedings, 8, 420.
   Google Scholar
• CRESPI, C. L., LANGENBACH, R. and PENMAN, B. W., 1990a, The development of a panel of human cell lines expressing specific human cytochrome P450 cDNAs. Progress in Clinical and Biological Research, 340B, 97–106.
   PubMedGoogle Scholar
• CRESPI, C. L., LANGENBACH, R. and PENMAN, B. W., 1993, Human cell lines, derived from AHH-1 TK -H/ — human lymphoblasts, genetically engineered for expression of cytochromes P450. Toxicology, 82, 104.
   Web of Science ®Google Scholar
• CRESPI, C. L., PENMAN, B. W., GELBOIN, H. V. and GONZALEZ, F. J., 1991a, A tobacco smoke-derived nitrosamine, 4-(methylnitrosamino)-1-(3-pyridy1)-1-butanone, is activated by multiple human cytochrome P450s including the polymorphic human cytochrome P4502D6. Carcinogenesis, 12, 1197–1201.
   PubMed Web of Science ®Google Scholar
• CRESPI, C. L., PENMAN, B. W., STEEVIEL, D. T., GELBOIN, H. V. and GONZALEZ, F. J., 1991b, The development of a human cell line stably expressing human CYP3A4: role in the metabolic activation of aflatoxin B1 and comparison to CYP1A2 and CYP2A3. Carcinogenesis, 12, 355–359.
   PubMed Web of Science ®Google Scholar
• CRESPI, C. L., STEEVIEL, D. T., AOYAMA, T., GELBOIN, H. V. and GONZALEZ, F. J., 1990b, Stable expression of human cytochrome P450IA2 cDNA in a human lymphoblastoid cell line: role of the enzyme in the metabolic activation of aflatoxin B1. Molecular Carcinogenesis, 3, 5–8.
   PubMed Web of Science ®Google Scholar
• CRESPI, C. L., STEIMEL, D. T., PENMAN, B. W., KORZEKWA, K. R., FERNANDEZSALGUER 0, P., BUTERS J. T. M., GELBOIN, H. V., GONZALEZ, F. J., IDLE, J. R. and DALY, A. K., 1995b, Comparison of substrate metabolism by wild-type CYP2D6 protein and a variant containing methionine, not valine, at position-374. Pharmacogenetks, 5, 234–243.
   Google Scholar
• CRESTEIL, T., MONSARRAT, B., ALVINERIE, P., TRELUYER, J. M., VIEIRA, I. and WRIGHT, M., 1994, Taxol metabolism by human liver microsomes: identification of cytochrome P450 isozymes involves in its biotransforrnation. Cancer Research, 54, 386–392.
   PubMed Web of Science ®Google Scholar
• DAYER, P., LEEMANN, T. and STRIBERNI, R., 1989, Dextromethorphan 0-demethylation in liver microsomes as a prototype reaction to monitor cytochrome P-450 db1 activity. Clinical Pharmacology and Therapeutics, 45, 34–40.
   PubMed Web of Science ®Google Scholar
• DIRVEN, H. A., PETERS, J. G., GIBSON, G. G., PETERS, W. H. and JONGENEELEN, F. J., 1991, Lauric acid hydroxylase activity and cytochrome P450 IV family proteins in human liver microsomes. Biochemical Pharmacology, 42, 1841–1844.
   PubMed Web of Science ®Google Scholar
• DISTERLATH, L. M., REILLY, P. E., MARTIN, M. V., DAVIS, G. G., WILKINSON, G. R. and GUENGERICH
   Google Scholar
• F. P., 1985, Purification and characterization of the human liver cytochromes P450 involved in debrisoquine 4-hydroxylation and phenacetin 0-deethylation, two prototypes for genetic polymorphisms in oxidative drug metabolism. Journal of Biological Chemistry, 260, 9057–9067.
   PubMed Web of Science ®Google Scholar
• DOECKE, C. J., SANSOM, L. N. and McMANus, M. E., 1990, Phenytoin 4-hydroxylation by rabbit liver P450IIC3 and identification of orthologs in human liver microsomes. Biochemical and Biophysical Research Communications, 166, 860–866.
   PubMed Web of Science ®Google Scholar
• DOECKE, C. J., VERONESE, M. E., POND, S. M., MINERS, J. 0., BIRKETT, D. J., SANSOM, L. N. and McMANus, M. E., 1991, Relationship between phenytoin and tolbutamide hydroxylations in human liver microsomes. British Journal of Clinical Pharmacology, 31, 125–130.
   Google Scholar
• DRAPER, N. R. and SMIT H., 1981, Applied Regression Analysis, 2nd edn (Chichester: John Wiley).
   Google Scholar
• ECHIZEN, H., KAWASAKI, H., CHIBA, K., TANI, M. and ISHIZAKI, T., 1993, A potent inhibitory effect of erythromycin and other macrolide antibiotics on the mono-N-dealkylation metabolism of disopyramide with human liver microsomes. Journal of Pharmacology and Experimental Therapeutics, 264, 1425–1431.
   PubMed Web of Science ®Google Scholar
• ELLIS, S. W., CHING, M. S., WATSON, P. F., HENDERSON, C. J., SIMULA, A. P., LENNARD, M. S., TUCKER, G. T. and WOODS, H. F., 1992, Catalytic activities of human debrisoquine 4-hydro xylase cytochrome P450 (CYP2D6) expressed in yeast. Biochemical Pharmacology, 44, 617–620.
   PubMed Web of Science ®Google Scholar
• ELLIS, S. W., ROWLAND, K., HARLOW, J. R., SIMULA, A. P., LENNARD, M. S., WOODS, H. F., TUCKER, G. T. and WOLF, C. R., 1994, Regioselective and enantioselective metabolism of metoprolol by 2 human cDNA-derived CYP2D6 proteins. British Journal of Pharmacology, 112S, 244P.
   Google Scholar
• EUGSTER, H. P., PROBST, M., WURGLER, F. E. and SENGSTAG C., 1993, Caffeine, estradiol, and progesterone interact with human CYP1A1 and CYP1A2. Evidence from cDNA-directed expression in Saccharomyces cerevisiae. Drug Metabolism and Disposition, 21, 43–49.
   Google Scholar
• EUGSTER, H. P., SENGSTAG, C., MEYER, U. A., HINNEN, A. and WURGLER, F. E., 1990, Constitutive and inducible expression of human cytochrome P450IA1 in yeast Saccharomyces cerevisiae : an alternative enzyme source for in vitro studies. Biochemical and Biophysical Research Communi-cations, 172, 737–744.
   PubMed Web of Science ®Google Scholar
• FISHER, C. W., CAUDLE, D. L., MARTIN -WIXTROM, C., QUATTROCHI, L. C., TUKEY, R. H., WATERMAN, M. R. and ESTABROOK, R. W., 1992, High-level expression of functional human cytochrome P450 1A2 in Escherichia coli. F ASEB Journal, 6, 759–764.
   Google Scholar
• FORRESTER, L. M., HENDERSON, C. J., GLANCEY, M. J., BACK, D. J., PARK, B. K., BALL, S. E., KITTERINGHAM, N. R., MCLAREN, A. W., MILES, J. S. and SKETT, P., 1992, Relative expression of cytochrome P450 isoenzymes in human liver and association with the metabolism of drugs and xenobiotics. Biochemical Journal, 281, 359–368.
   PubMed Web of Science ®Google Scholar
• FUHR, U., STROBL, G., MANAUT, F., ANDERS E. M., SORGEL, F., LOPEZ-DE —BRINAS, E., CHU, D. T., PERNET, A. G., MAHR, G. and SANZ, F., 1993, Quinolone antibacterial agents: relationship between structure and in vitro inhibition of the human cytochrome P450 isoform CYP1A2. Molecular Pharmacology, 43, 191–199.
   Google Scholar
• FURUYA, H., MEYER, U. A., GELBOIN, H. V. and GONZALEZ, F. J., 1991, Polymerase chain reaction-directed identification, cloning, and quantification of human CYP2C18 mRNA. Molecular Pharmacology, 40, 375–382.
   PubMed Web of Science ®Google Scholar
• GASCON, M. P. and DAYER, P., 1991, In vitro forecasting of drugs which may interfere with the biotransformation of midazolam. European Journal of Clinical Pharmacology, 41, 573–578.
   PubMed Web of Science ®Google Scholar
• GED, C., UMBENHAUER, D. R., BELLEW, T. M., BORK, R. W., SRIVASTAVA, P. K., SHINRIKI, N., LLOYD, R. S. and GUENGERICH, F. P., 1988, Characterization of cDNAs, mRNAs, and proteins related to human liver microsomal cytochrome P-450 (S)-mephenytoin 4'-hydroxylase. Biochemistry, 27, 6929–6940.
   PubMed Web of Science ®Google Scholar
• GILLAM, E. M. J., BABA, T., KIM, B. R., OHMORI, S. and GUENGERICH, F. P., 1993, Expression of modified human cytochrome P450 3A4 in Escherichia coli and purification and reconstitution of the enzyme. Archives of Biochemistry and Biophysics, 305, 123–131.
   Google Scholar
• GILLAM, E. M. J., Guo, Z. and GUENGERICH, F. P., 1994, Expression of modified human cytochrome P4502E1 in Escherichia coli, purification and spectral and catalytic properties. Archives of Biochemistry and Biophysics, 312, 59–66.
   Google Scholar
• GILLAM, E. M. J., Guo, Z. Y., MARTIN, M. V., JENKINS, C. M. and GUENGERICH, F. P., 1995a, Expression of cytochrome-P450 2D6 in Escherichia coli, purification, and spectral and catalytic characterization. Archives of Biochemistry and Biophysics, 319, 540–550.
   Google Scholar
• GILLAM, E. M. J., Guo, Z. Y., UENG, Y. F., YAMAZAKI, H., COCK, I., REILLY, P. E. B., HOOPER, W. D. and GUENGERICH, F. P., 1995b, Expression of cytochrome-P450-3A5 in Escherichia coli—effects of 5 modification, purification, spectral characterization, reconstitution conditions, and catalytic activities. Archives of Biochemistry and Biophysics, 317, 374–384.
   Google Scholar
• GOLDSTEIN, J. A., FALETTO, M. B., ROMKESSPARKS, M., SULLIVAN, T., KITAREEWAN, S., RAUCY, J. L., LASKER, J. M. and GHANAYEM, B. I., 1994, Evidence that CYP2C19 is the major (S)-mephenytoin 4'-hydroxylase in humans. Biochemistry, 33, 1743–1752.
   PubMed Web of Science ®Google Scholar
• GONZALEZ, F. J. and KORZEKWA, K. R., 1995, Cytochromes P450 expression systems. Annual Review of Pharmacology and Toxicology, 35, 369–390.
   PubMed Web of Science ®Google Scholar
• GONZALEZ, F. J., SCHMID, B. J., UMENO, M., MuBRIDE, 0. W., HARDWICK, J. P., MEYER, U. A., GELBOIN, H. V. and IDLE, J. R., 1988, Human P450PCN1: sequence, chromosome localization, and direct evidence through cDNA expression that P450PCN1 is nifedipine. DNA, 7, 79–86.
   Google Scholar
• GORSKI, J. C., HALL, S. D., VANDENBRANDEN, M., WRIGHTON, S. A. and Jos, D. R., 1994, Regioselective biotransforrnation of midazolam by members of the human cytochrome-P450-3A (CYP3A) subfamily. Biochemical Pharmacology, 47, 1643–1653.
   PubMed Web of Science ®Google Scholar
• GRANT, D. M., CAMPBELL, M. E., TANG, B. K. and KALO W., 1987, Biotransformation of caffeine by microsomes from human liver. Kinetic and inhibitor studies. Biochemical Pharmacology, 36, 1251–1260.
   PubMed Web of Science ®Google Scholar
• GUENGERICH, F. P., 1990, Mechanism-based inactivation of human liver microsomal cytochrome P-450 II1A4 by gestodene. Chemical Research in Toxicology, 3, 363–371.
   PubMed Web of Science ®Google Scholar
• GUENGERICH, F. P., 1992, Characterization of human cytochrome P450 enzymes. FASEB Journal, 6, 745–748.
   PubMed Web of Science ®Google Scholar
• GUENGERICH, F. P., 1995, Cytochromes P450 of human liver. Classification and activity profiles of the major enzymes. In G. M. Pacifici and G. N. Fracchia (eds), Advances in Drug Metabolism in Man (Luxembourg: European Commission), pp. 179–231.
   Google Scholar
• GUENGERICH, F. P. and KIM, D. H., 1990, In vitro inhibition of dihydropyridine oxidation and aflatoxin B1 activation in human liver microsomes by naringenin and other flavonoids. Carcinogenesis, 11, 2275–2279.
   PubMed Web of Science ®Google Scholar
• GUENGERICH, F. P., KIM, D. H. and IWASAKI, M., 1991, Role of human cytochrome P-450 IIE1 in the oxidation of many low molecular weight cancer suspects. Chemical Research in Toxicology, 4, 168–179.
   PubMed Web of Science ®Google Scholar
• GUENGERICH, F. P., MARTIN, M. V., BEAUNE, P. H., KREIVIERS, P., WOLFF, T. and WAXMAN, D. J., 1986a, Characterization of rat and human liver microsomal cytochrome P450 forms involved in nifedipine oxidation, a prototype for genetic polymorphism in oxidative drug metabolism. Journal of Biological Chemistry, 261, 5051–5060.
   PubMed Web of Science ®Google Scholar
• GUENGERICH, F. P., MULLER -ENOCH, D. and BLAIR, I. A., 1986b, Oxidation of quinidine by human liver cytochrome P450. Molecular Pharmacology, 30, 287–295.
   Google Scholar
• Guo, Z., GILLAM, E. M. J., OHMORI, S., TUKEY, R. H. and GUENGERICH, F. P., 1994, Expression of modified human cytochrome P4501A1 in Escherichia coli effects of 5' substitution, stabilization, purification and catalytic properties. Archives of Biochemistry and Biophysics, 312, 436–446.
   Google Scholar
• GUT, J., CATIN, T., DAYER, P., KRONBACH, T., ZANGER U. and MEYER, U. A., 1986, Debrisoquine/ sparteine-type polymorphism of drug oxidation: purification and characterization of two functionally different human liver cytochrome P450 isozymes involved in impaired hydroxylation of the prototype substrate bufuralol. Journal of Biological Chemistry, 261, 11734–11743.
   Google Scholar
• HA, H. R., CHEN, J., LEUENBERGER, P.M., FREIBURGHAUS, A. U. and FOLLATH, F., 1995, In-vitro inhibition of midazolam and quinidine metabolism by flavonoids. European Journal of Clinical Pharmacology, 48, 367–371.
   PubMed Web of Science ®Google Scholar
• HALL, S. D., HAMIMAN, M. A., RETT1E, A. E., WIENKERS, L. C., TRAGER, W. F., VANDENBRANDEN, M. and WRIGHTON, S. A., 1994, Relationships between the levels of cytochrome P4502C9 and its prototypic catalytic activities in human liver-microsomes. Drug Metabolism and Disposition, 22, 975–978.
   Google Scholar
• HARRIS, J. W., KATKI, A., ANDERSON, L. W., CHMURNY, G. N., PAUKSTELIS J. V., and COLLINS, J. M., 1994, Isolation, structural determination, and biological-activity of 6-alpha-hydroxytaxol, the principal human metabolite of taxol. Journal of Medicinal Chemistry, 37, 706–709.
   Google Scholar
• HERMANS, J. J. and THUSSEN, H. H., 1993, Human liver microsomal metabolism of the enantiomers of warfarin and acenocoumarol: P450 isozyme diversity determines the differences in their pharmacokinetics. British Journal of Pharmacology, 110, 482–490.
   PubMed Web of Science ®Google Scholar
• HEYN, H., STEVENS, J. C. and MARIETTA, M. P., 1995, The N-demethylation of S-mephenytoin by cytochromes P450-2B6 and -3A4. IS S X Proceedings, 8, 73.
   Google Scholar
• IMAOKA, S., OGAWA, H., KIMURA, S. and GONZALEZ, F. J., 1993, Complete cDNA sequence and cDNA-directed expression of CYP4A11, a fatty acid omega-hydroxylase expressed in human kidney. DNA and Cell Biology, 12, 893–899.
   PubMed Web of Science ®Google Scholar
• INABA, T., JuiumA, M., MAHON, W. A. and KALO W. 1985, In vitro inhibition studies of two isozymes of human liver cytochrome P450: mephenytoin p-hydroxylase and sparteine monooxygenase. Drug Metabolism and Disposition, 13, 443–448.
   PubMed Web of Science ®Google Scholar
• JoNssoN, G., ASTROM, A. and ANDERSSON, P., 1995, Budesonide is metabolized by cytochrome-P450 3A (CYP3A) enzymes in human liver. Drug Metabolism and Disposition, 23, 137–142.
   PubMed Web of Science ®Google Scholar
• JURIMA -ROIVIET, M., CRAWFORD, K., CYR, T. and INABA, T., 1994, Terfenadine metabolism in human liver—in vitro inhibition by macrolide antibiotics and azole antifungals. Drug Metabolism and Disposition, 22, 849–857.
   PubMed Web of Science ®Google Scholar
• KAMINSKY, L. S., DE MORAIS, S. M., FALETTO, M. B., DUNBAR, D. A. and GOLDSTEIN, J. A., 1993, Correlation of human cytochrome P4502C substrate specificities with primary structure: warfarin as a probe. Molecular Pharmacology, 43, 234–239.
   PubMed Web of Science ®Google Scholar
• KAWASHIMA, H., KUSUNOSE, E., KUBOTA, I., MAEKAWA, M. and KUSUNOSE, M., 1992, Purification and NH,-terminal amino acid sequences of human and rat kidney fatty acid omega-hydroxylases. Biochimica et Biophyska Acta, 1123, 156–162.
   PubMed Web of Science ®Google Scholar
• KEMPF, A. C., ZANGER, U. M. and MEYER, U. A., 1995, Truncated human p450 2d6—expression in Escherichia coli, Ni,-chelate affinity purification, and characterization of solubility and ag-gregation. Archives of Biochemistry and Biophysics, 321, 277–288.
   PubMed Web of Science ®Google Scholar
• KERR, B. M., THUMMEL, K. E., WURDEN, C. J., KLEIN, S. M., KROETZ, D. L., GONZALEZ, F. J. and LEVY, R. H., 1994, Human liver carbamazepine metabolism—role of CYP3A4 and CYP2C8 in 10, 11-epoxide formation. Biochemical Pharmacology, 47, 1969–1979.
   PubMed Web of Science ®Google Scholar
• KERRY, N. L., SOMOGYI, A. A., BOCHNER, F. and MIKUS, G., 1994, The role of CYP2D6 in primary and secondary oxidative-metabolism of dextromethorphan—in-vitro studies using human liver-microsomes. British Journal of Clinical Pharmacology, 38, 243–248.
   PubMed Web of Science ®Google Scholar
• KHARASCH, E. D. and THUMIVIEL, K. E., 1993, Identification of cytochrome P450 2E1 as the predominant enzyme catalyzing human liver microsomal defluorination of sevoflurane, isoflurane, and methoxyflurane. Anesthesiology, 79, 795–807.
   PubMed Web of Science ®Google Scholar
• KOOP, D. R., LAETHEM, C. L. and TIERNEY, D. J., 1989, The utility of p-nitrophenol hydroxylation in P450I1E1 analysis. Drug Metabolism Reviews, 20, 541–551.
   PubMed Web of Science ®Google Scholar
• KRONBACH, T., 1991, Bufuralol, dextromethorphan, and debrisoquine as prototype substrates for human P450I1D6. Methods in Enzymology, 206, 509–517.
   PubMed Web of Science ®Google Scholar
• KRONBACH, T., FISCHER, V. and MEYER, U. A. 1988, Cyclosporine metabolism in human liver: identification of a cytochrome P45011I gene family as the major cyclosporine-metabolising enzyme explains interactions of cyclosporine with other drugs. Clinical Pharmacology and Therapeutics, 43, 630–635.
   PubMed Web of Science ®Google Scholar
• KRONBACH, T., MATHYS, D., UMENO, M., GONZALEZ, F. J. and MEYER, U. A., 1989, Oxidation of midazolam and triazolam by human liver cytochrome P4501I1A4. Molecular Pharmacology, 36, 89–96.
   PubMed Web of Science ®Google Scholar
• KRYNETSKI, E. Y., DRUTSA, V. L., KOVALEVA, I. E. and Luzmov, V. N., 1995, High-yield expression of functionally active human liver CYP2D6 in yeast-cells. Pharmacogenetics, 5, 103–109.
   PubMedGoogle Scholar
• KUMAR, G. N., WALLE, U. K. and WALLE, T., 1994, Cytochrome-P450 3A-mediated human liver microsomal taxol 6-a-hydroxylation. Journal of Pharmacology and Experimental Therapeutics, 268, 1160–1165.
   PubMed Web of Science ®Google Scholar
• KUNZE, K. L. and TRAGER, W. F., 1993, Isoform-selective mechanism-based inhibition of human cytochrome P450 1A2 by furafylline. Chemical Research in Toxicology, 6, 649–656.
   PubMed Web of Science ®Google Scholar
• LABBE, G., DESCATOIRE V., BEAUNE, P., LETTERON, P., LARREY, D. and PESSAYRE, D., 1989, Suicide inactivation of cytochrome P-450 by methoxsalen. Evidence for the covalent binding of a reactive intermediate to the protein moiety. Journal of Pharmacology and Experimental Therapeutics, 250, 1034–1042.
   Google Scholar
• LANG, D. and BOCKE R., 1995, Highly sensitive and specific high-performance liquid-chromatographic analysis of 7-hydroxywarfarin, a marker for human cytochrome P-4502C9 activity. Journal of Chromatography B—Biomedical Applications, 672, 305–309.
   PubMed Web of Science ®Google Scholar
• LEE, C. A., KADWELL, S. H., KOST, T. A. and SERABJITSINGH, C. J., 1995, CYP3A4 expressed by insect cells infected with a recombinant baculovirus containing both CYP3A4 and human NADPH-cytochrome P450 reductase is catalytically similar to human liver microsomal CYP3A4. Archives of Biochemistry and Biophysics, 319, 157–167.
   PubMed Web of Science ®Google Scholar
• LEEMANN, T., TRANSON, C. and DAYER, P., 1993, Cytochrome P450TB (CYP2C): a major mono-oxygenase catalyzing diclofenac C.-hydroxylation in human liver. Life Sciences 52, 29–34.
   Google Scholar
• LEO, M. A., LASKER, J. M., RAUCY, J. L., KIM, C. I., BLACK, M. and LIEBER, C. S., 1989, Metabolism of retinol and retinoic acid by human liver cytochrome P450I1C8. Archives of Biochemistry and Biophysics, 269, 305–312.
   PubMed Web of Science ®Google Scholar
• LOFT, S., OTTON, S. V., LENNARD, M. S., TUCKER, G. T. and POULSEN, H. E., 1991, Characterization of metronidazole metabolism by human liver microsomes. Biochemical Pharmacology, 41, 1127–1134.
   PubMed Web of Science ®Google Scholar
• LOPEZ GARCIA, M. P., DANSETTE, P. M., VALADON, P., AMAR, C., BEAUNE, P. H., GUENGERICH, F. P. and MANSUY, D., 1994, Human-liver cytochromes P-450 expressed in yeast as tools for reactive-metabolite formation studies. Oxidative activation of tienilic acid by cytochromes P-450 2C9 and 2C10. European Journal of Biochemistry, 213, 223–232.
   Google Scholar
• MADDEN, S., WOOLF, T. F., POOL, W. F. and PARK, B. K., 1993, An investigation into the formation of stable, protein-reactive and cytotoxic metabolites from tacrine in vitro. Studies with human and rat liver microsomes. Biochemical Pharmacology, 46, 13–20.
   PubMed Web of Science ®Google Scholar
• MASUBUCHI, Y., HOSOKAWA, S., HORIE, T., SUZUKI, T., OHMORI, S., KITADA, M. and NARIMATSU, S., 1994, Cytochrome-P450 isozymes involved in propranolol metabolism in human liver-microsomes—the role of CYP2D6 as ring-hydroxylase and CYP1A2 as N-desisopropylase. Drug Metabolism and Disposition, 22, 909–915.
   PubMed Web of Science ®Google Scholar
• MAURICE, M., PICHARD, L., DAUJAT, M., FABRE, I., JOYEUX, H., DOMERGUE, J. and MAUREL, P., 1992, Effects of imidazole derivatives on cytochromes P450 from human hepatocytes in primary culture. FASEB Journal, 6, 752–758.
   PubMed Web of Science ®Google Scholar
• MAYHEW, B. S., GORSKI, J. C. and HALL, S. D., 1995, Midazolam hydroxylation reveals the potential for non-hyperbolic kinetics in cytochrome P450 (CYP) 3A4. IS SX Proceedings, 8, 314.
   Google Scholar
• McMANus, M. E., BURGESS, W. M., VERONESE, M. E., HUGGETT, A., QUATTROCHI, L. C. and TUKEY R. H., 1990, Metabolism of 2-acetylaminofluorene and benzo(a)pyrene and activation of food-derived heterocyclic amine mutagens by human cytochromes P-450. Cancer Research, 50, 3367–3376.
   Google Scholar
• MILES, J. S., MCLAREN, A. W., FORRESTER, L. M., GLANCEY, M. J., LANG, M. A. and WOLF, C. R.,1990, Identification of the human liver cytochrome P-450 responsible for coumarin 7-hydroxylase activity. Biochemical Journal, 267, 365–371.
   PubMed Web of Science ®Google Scholar
• MIMURA, M., BABA, T., YAMAZAKI, H., OHMORI, S., INUI, Y., GONZALEZ, F. J., GUENGERICH, F. P. and SHIMADA, T., 1993, Characterization of cytochrome P-450 2B6 in human liver microsomes. Drug Metabolism and Disposition, 21, 1048–1056.
   PubMed Web of Science ®Google Scholar
• MINERS, J. 0., REES, D. L. P., VALENTE, L., VERONESE, M. E. and BIRKETT, D. J., 1995, Human hepatic cytochrome-P450 2C9 catalyzes the rate-limiting pathway of torsemide metabolism. Journal of Pharmacology and Experimental Therapeutics, 272, 1076–1081.
   Google Scholar
• MINERS, J. 0., SMITH, K. J., ROBSON, R. A., McMANus, M. E., VERONESE, M. E. and BIRKETT, D. J., 1988, Tolbutamide hydroxylation by human liver microsomes: kinetic characterisation and relationship to other cytochrome P450 dependent xenobiotic oxidations. Biochemical Phar-macology, 37, 1137–1144.
   Google Scholar
• MINISCALO, A., LUNDAHL, J., REGARDH, G., EDGAR, B. and ERIKSSON, U. G., 1992, Inhibition of dihydropyridine metabolism in rat and human liver microsomes by flavenoids found in grapefruit juice. Journal of Pharmacology and Experimental Therapeutics, 261, 1195–1199.
   PubMed Web of Science ®Google Scholar
• MOTULSKY, H. J. and RANSNAS, L. A., 1987, Fitting curves to data using nonlinear regression: a practical and nonmathematical review. FASEB Journal, 1, 365–374.
   PubMed Web of Science ®Google Scholar
• MURAKAMI, H., YABUSAKI, Y. and OHKAWA, H., 1986, Expression of rat NADPH-cytochrome P450 reductase in Saccharomyces cerevisiae. DNA and Cell Biology, 5, 1–10.
   Google Scholar
• NEWTON, D.J., WANG, R. W. and Lu, A. Y. H., 1995, 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.
   PubMed Web of Science ®Google Scholar
• OHGIYA, S., KOMORI, M., FUJITANI, T., MIURA, T., SHINRIKI, N. and KAMATAKI, T., 1989, Cloning of human cytochrome P-450 cDNA and its expression in Saccharomyces cerevisiae. Biochemistry International, 18, 429–438.
   PubMedGoogle Scholar
• ONO, S., HATANAKA, T., HOTTA, H., TSUTSUI, M., SATOH, T. and GONZALEZ, F. J., 1995, Chlorzoxazone is metabolized by human CYP1A2 as well as by human CYP2E1. Pharmacogenetics, 5, 143–150.
   PubMedGoogle Scholar
• OTTON, S. V., CREWE, H. K., LENNARD, M. S., TUCKER, G. T. and WOODS, H. F., 1988, Use of quinidine inhibition to define the role of the sparteine/debrisoquine cytochrome P450 in metoprolol oxidation by human liver microsomes. Journal of Pharmacology and Experimental Therapeutics, 247, 242–247.
   PubMed Web of Science ®Google Scholar
• PALMER, C. N., RICHARDSON, T. H., GRIFFIN, K. J., Hsu, M. H., MUERHOFF, A. S., CLARK, J. E. and JOHNSON, E. F., 1993, Characterization of a cDNA encoding a human kidney, cytochrome P-450 4A fatty acid co-hydroxylase and the cognate enzyme expressed in Escherichia coli. Biochimica et Biophyska Acta, 1172, 161–166.
   PubMed Web of Science ®Google Scholar
• PATTEN, C. J., ISHIZAKI, H., AOYAMA, T., LEE, M., NING, S. M., HUANG, W., GONZALEZ, F. J. and YANG, C. S., 1992, Catalytic properties of the human cytochrome P450 2E1 produced by cDNA expression in mammalian cells. Archives of Biochemistry and Biophysics, 299, 163–171.
   PubMed Web of Science ®Google Scholar
• PATTEN, C. J. and KocH, P., 1995, Baculovirus expression of human P450 2E1 and cytochrome b(5)-spectral and catalytic properties and effect of b(5) on the stoichiometry of P450 2E1-catalyzed reactions. Archives of Biochemistry and Biophysics, 317, 504–513.
   PubMed Web of Science ®Google Scholar
• PATTEN, C. J., THOMAS, P. E., GUY, R. L., LEE, M., GONZALEZ, F. J., GUENGERICH, F. P. and YANG, C. S., 1993, Cytochrome P450 enzymes involved in acetaminophen activation by rat and human liver microsomes and their kinetics. Chemical Research in Toxicology, 6, 511–518.
   PubMed Web of Science ®Google Scholar
• PEARCE, R., GREENWAY, D. and PARKINSON, A., 1992, Species differences and interindividual variation in liver microsomal cytochrome P450 2A enzymes: effects on coumarin, dicumarol, and testosterone oxidation. Archives of Biochemistry and Biophysics, 298, 211–225.
   PubMed Web of Science ®Google Scholar
• PEARSON, E. S. and HARTLEY, H. 0., 1976, Biometrika T ables for Statisticians, vol. 1,3rd edn (Cambridge: Cambridge University Press).
   Google Scholar
• PELKONEN, 0., SOTAN1EMI, E. A. and AHOKAS, J. T., 1990, Coumarin 7-hydroxylase activity in human liver microsomes. Properties of the enzyme and interspecies comparison. British Journal of Clinical Pharmacology, 19, 59–66.
   Google Scholar
• PENMAN, B. W., CHEN, L. P., GELBOIN, H. V., GONZALEZ, F. J. and CRESPI, C. L., 1994, Development of a human lymphoblastoid cell-line constitutively expressing human CYP1A1 cDNA—substrate-specificity with model substrates and promutagens. Carcinogenesis, 15, 1931–1937.
   PubMed Web of Science ®Google Scholar
• PENMAN, B. W., REECE, J., SMITH, T., YANG, C. S., GELBOIN, H. V., GONZALEZ, F. J. and CRESPI, C. L., 1993, Characterization of a human cell line expressing high levels of cDNA-derived CYP2D6. Pharmacogenetks, 3, 28–39.
   PubMedGoogle Scholar
• PETER, R., BOCKER, R., BEAUNE, P. H., IWASAKI, M., GUENGERICH, F. P. and YANG, C. S., 1990, Hydroxylation of chlorzoxazone as a specific probe for human liver cytochrome P-4501IE1. Chemical Research in Toxicology, 3, 566–573.
   PubMed Web of Science ®Google Scholar
• PEYRONNEAU, MA., RENAUD, J. P., TRUAN, G., URBAN, P., POMPON, D. and MANSUY, D., 1992, Optimization of yeast-expressed human liver cytochrome P450 3A4 catalytic activities by coexpressing NADPH-cytochrome P450 reductase and cytochrome b5. European Journal of Biochemistry, 207, 109–116.
   PubMedGoogle Scholar
• PICHARD, L., FABRE, I., FABRE, G., DOMERGUE, J., SAINT AUBERT, B., MOURAD, G. and MAUREL, P., 1990, Cyclosporin A drug interactions. Screening for inducers and inhibitors of cytochrome P-450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and in liver microsomes. Drug Metabolism and Disposition, 18, 595–606.
   PubMed Web of Science ®Google Scholar
• PODOLL, T. D., KUNZE, K. L., THUMIVIEL, K. E., FISHER, J. M. and TRAGER, W. F., 1995, Evidence supporting mechanism-based inactivation of CYP3A by midazolam. I S SX Proceedings, 8, 154.
   Google Scholar
• RAHMAN, A., KORZEKWA, K. R., GROGAN, J., GONZALEZ, F. J. and HARRIS, J. W., 1994, Selective biotransformation of taxol to 6-a-hydroxytaxol by human cytochrome-P450 2C8. Cancer Research, 54, 5543–5546.
   PubMed Web of Science ®Google Scholar
• RASMUSSEN, B. B., MAENPAA J., PELKONEN, 0., LOFT, S., POULSEN, H. E., LYKKESFELDT, J. and BROSEN K., 1995, Selective serotonin reuptake inhibitors and theophylline metabolism in human liver-microsomes—potent inhibition by fluvoxamine. British Journal of Clinical Pharmacology, 39, 151–159.
   Google Scholar
• RELLING, M. V., AOYAMA, T., GONZALEZ, F. J. and MEYER, U. A., 1990, Tolbutamide and mephenytoin hydroxylation by human cytochrome P45 Os in the CYP2C subfamily. Journal of Pharmacology and Experimental Therapeutics, 252, 442–447.
   PubMed Web of Science ®Google Scholar
• RELLING, M. V., EVANS, W. E., FONNE -PFISTER, R. and MEYER, U. A., 1989, Anticancer drugs as inhibitors of two polymorphic cytochrome P450 enzymes, debrisoquine and mephenytoin hydroxylase, in human liver microsomes. Cancer Research, 49, 68–71.
   Google Scholar
• REMIVIEL, R. P. and BURCHELL, B., 1993, Validation and use of cloned, expressed human drug-metabolizing enzymes in heterologous cells for analysis of drug metabolism and drug—drug interactions. Biochemical Pharmacology, 46, 559–566.
   PubMed Web of Science ®Google Scholar
• RENAUD, J. P., CuLLIN, C., POMPON, D., BEAUNE, P. and MANSUY, D., 1990, Expression of human liver cytochrome P450 II1A4 in yeast. A functional model for the hepatic enzyme. European Journal of Biochemistry, 194, 889–896.
   PubMedGoogle Scholar
• RETTlE, A. E., KORZEKWA, K. R., KUNZE, K. L., LAWRENCE, R. F., EDDY, A. C., AOYAMA, T., GELBOIN H. V., GONZALEZ, F. J. and TRAGER, W. F., 1992, Hydroxylation of warfarin by human cDNA-expressed cytochrome P-450: a role for P-4502C9 in the etiology of (S)-warfarin-drug interactions. Chemical Research in Toxicology, 5, 54–59.
   Google Scholar
• RETTlE, A. E., WlENKERS, L. C., GONZALEZ, F. J., TRAGER, W. F. and KORZEKWA, K. R., 1994, Impaired (S)-warfarin metabolism catalyzed by the R144C allelic variant of CYP2C9. Pharmacogenetks, 4, 39–42.
   PubMedGoogle Scholar
• RICHARDSON, T. H., JUNG, F., GR1FFEN, K. J., WESTER, M., RAUCY, J. L., KEMPER, B., BORNHELM, L. M., HASSETT, C., 0M1ECINSKI, C. J. and JOHNSON, E. F., 1995, A universal approach to the expression of human and rabbit cytochromeP450s of the 2C subfamily in Escherichia coli. Archives of Biochemistry and Biophysics, 323, 87–96.
   Google Scholar
• RODRIGUES, A. D., 1994, Use of in-vitro human metabolism studies in drug development—an industrial perspective. Biochemical Pharmacology, 48, 2147–2156.
   PubMed Web of Science ®Google Scholar
• RODRIGUES, A. D., KUKULKA, M. J., SURBER, B. W., THOMAS, S. B., UCHIC, J. T., ROTERT, G. A., MICHEL, G., THOIVIEKROIVIER, B. and MACHINIST, J. M., 1994, Measurement of liver microsomal cytochrome-P450 (CYP2D6) activity using [0-methyl-C-14] dextromethorphan. Analytical Biochemistry, 219, 309–320.
   PubMed Web of Science ®Google Scholar
• RODRIGUES, A. D., MULFORD, 0. J., LEE, R. D., SURBER, B. W., KUKULKA, M. J., FERRERO, J. L., THOMAS, S. B., SHET, M. S. and ESTABROOK, R. W., 1995, In-vitro metabolism of terfenadine by a purified recombinant fusion protein containing cytochrome P4503A4 and NADPH-P450 reductase—comparison to human liver-microsomes and precision-cut liver-tissue slices. Drug Metabolism and Disposition, 23, 765–775.
   Google Scholar
• ROMKES, M., FALETTO, M. B., BLAISDELL, J. A., RAUCY, J. L. and GOLDSTEIN, J. A., 1991, Cloning and expression of complementary DNAs for multiple members of the human cytochrome P450I1C subfamily. Biochemistry, 30, 3247–3255.
   PubMed Web of Science ®Google Scholar
• RYAN, D. E. and LEVIN, W., 1990, Purification and characterization of hepatic microsomal cytochrome P-450. Pharmacology and Therapeutics, 45, 153–239.
   PubMed Web of Science ®Google Scholar
• SANDHU, P., BABA, T. and GUENGERICH, F. P., 1993, Expression of modified cytochrome P450 2C10 (2C9) in Escherkhia coli, purification, and reconstitution of catalytic activity. Archives of Biochemistry and Biophysics, 306, 443–450.
   PubMed Web of Science ®Google Scholar
• SANDHU, P., Guo, Z. Y., BABA, T., MARTIN, M. V., TUKEY, R. H. and GUENGERICH, F. P. 1994, Expression of modified human cytochrome-P450 1A2 in Escherichia coll—stabilization, puri-fication, spectral characterization, and catalytic activities of the enzyme. Archives of Biochemistry and Biophysics, 309, 168–177.
   PubMed Web of Science ®Google Scholar
• SARKAR, M., PoLK, R. E., GUZELIAN, P. S., HUNT, C. and KARNES, H. T., 1990, In vitro effect of fluroquinolones on theophylline metabolism in human liver microsomes. Antimicrobial Agents and Chemotherapy, 34, 594–599.
   PubMed Web of Science ®Google Scholar
• SCHWEIKL, H., TAYLOR, J. A., KITAREEWAN, S., LINKO, P., NAGORNEY, D. and GOLDSTEIN, J. A., 1993, Expression of CYP1A1 and CYP1A2 genes in human liver. Pharmacogenetics, 3, 239–249.
   PubMedGoogle Scholar
• SENGSTAG C., EUGSTER, H. P. and WURGLER, F. E., 1994, High promutagen activating capacity of yeast microsomes containing human cytochrome P4501A and human NADPH—cytochrome P450 reductase. Carcinogenesis, 15, 837–844.
   Google Scholar
• SESARDIC, D., Booms, A. R., EDWARDS, R. J. and DAVIES, D. S., 1988, A form of cytochrome P450 in man, orthologous to form d in the rat, catalyses the 0-deethylation of phenacetin and is inducible by cigarette smoking. British Journal of Clinical Pharmacology, 26, 363–372.
   PubMed Web of Science ®Google Scholar
• SESARDIC, D., BOOBIS, A. R., MURRAY, B. P., MURRAY, S., SEGURA, J., DE LA TORRE, R. and DAVIES, D. S., 1990, Furafylline is a potent and selective inhibitor of cytochrome P450IA2 in man. British Journal of Clinical Pharmacology, 29, 651–663.
   PubMed Web of Science ®Google Scholar
• SHET, M. S., FISHER, C. W., HOLMANS, P. L. and ESTABROOK, R. W., 1993, Human cytochrome P450 3A4: enzymatic properties of a purified recombinant fusion protein containing NADPH-P450 reductase. Proceedings of the National Academy of Sciences, USA, 90, 11748–11752.
   PubMed Web of Science ®Google Scholar
• SHIMADA, T., MISONO, K. S. and GUENGERICH, F. P., 1986, Human liver microsomal cytochrome P450 mephenytoin 4-hydroxylase, a prototype of genetic polymorphism in oxidative drug metabolism. Purification and characterization of two similar forms involved in the reaction. Journal of Biological Chemistry, 261, 909–921.
   PubMed Web of Science ®Google Scholar
• SHIMADA, T., YUN, C. H., YAMAZAKI, H., GAUTIER, J. C., BEAUNE, P. H. and GUENGERICH, F. P., 1992, Characterization of human lung microsomal cytochrome P-450 1A1 and its role in the oxidation of chemical carcinogens. Molecular Pharmacology, 41, 856–864.
   PubMed Web of Science ®Google Scholar
• SHIMADA, T., YAMAZAKI, H., MIMURA, M., INUI, Y. and GUENGERICH, F. P., 1994, Interindividual variations in human liver cytochrome-P-450 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
• SHOU, M., GROGAN, J., MANCEWICZ, J. A., KRAUSZ, K. W., GONZALEZ, F. J., GELBOIN, H. V. and KORZEKWA, K. R., 1994, Activation of CYP3A4—evidence for the simultaneous binding of 2 substrates in a cytochrome-P450 active-site. Biochemistry, 33, 6450–6455.
   PubMed Web of Science ®Google Scholar
• SIESS, M. H., LECLERC, J., CANIVENCLAVIER, M. C., RAT, P. and SUSCHETET, M., 1995, Heterogeneous effects of natural flavonoids on monooxygenase activities in human and rat-liver microsomes. Toxicology and Applied Pharmacology, 130, 73–78.
   PubMed Web of Science ®Google Scholar
• SILVERS, K. J., CHAZINSKI, T., McMANus, M. E., BALER, S. L., GONZALEZ, F. J., GELBOIN, H. V., MAUREL, P. and HOWARD, P. C., 1992, Cytochrome P-450 3A4 (nifedipine oxidase) is responsible for the C-oxidative metabolism of 1-nitropyrene in human liver microsomal samples. Cancer Research, 52, 6237–6243.
   PubMed Web of Science ®Google Scholar
• SKJELBO, E. and BROSEN, K., 1992, Inhibitors of imipramine metabolism by human liver microsomes. British Journal of Clinical Pharmacology, 34, 256–261.
   PubMed Web of Science ®Google Scholar
• SPALDIN V., MADDEN, S., ADAMS, D. A., EDWARDS, R. J., DAVIES, D. S. and PARK, B. K., 1995, Determination of human hepatic cytochrome P4501A2 activity in-vitro—use of tacrine as an isoenzyme-specific probe. Drug Metabolism and Disposition, 23, 929–934.
   Google Scholar
• SPALDIN V., MADDEN, S., Poor, W. F., WOOLF, T. F. and PARK, B. K., 1994, The effect of enzyme inhibition on the metabolism and activation of tacrine by human liver microsomes. British Journal of Clinical Pharmacology, 38, 15–22.
   Google Scholar
• SRIVASTAVA, P. K., YUN, C. H., BEAUNE, P. H., GED, C. and GUENGERICH, F. P., 1991, Separation of human liver microsomal tolbutamide hydroxylase and (S)-mephenytoin 4'-hydroxylase cyto-chrome P-450 enzymes. Molecular Pharmacology, 40, 69–79.
   PubMed Web of Science ®Google Scholar
• STUPANS, I. and SANSOM, L. N., 1991, The inhibition of drug oxidation by anhydroerythromycin, an acid degradation product of erythromycin. Biochemical Pharmacology, 42, 2085–2090.
   PubMed Web of Science ®Google Scholar
• TASSANEEYAKUL, W., BIRKETT, D. J., VERONESE, M. E., McMANus, M. E., TUKEY, R. H., QUATTROCHI L. C., GELBOIN, H. V. and MINERS, J. 0., 1993a, Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2. Journal of Pharmacology and Experimental Therapeutics, 265, 401–407.
   Google Scholar
• TASSANEEYAKUL W., MOHAMED, Z., BIRKETT, D. J., McMANus, M. E., VERONESE, M. E., TUKEY, R. H., QUATTROCHI, L. C., GONZALEZ, F. J. and MINERS, J. 0., 1992, Caffeine as a probe for human cyto chromes P450: validation using cDNA-expression, immunoinhibition and microsomal kinetic and inhibitor techniques. Pharmacogenetics, 2, 173–183.
   Google Scholar
• TASSANEEYAKUL W., VERONESE, M. E., BIRKETT, D. J., GONZALEZ, F. J. and MINERS, J. 0., 1993b, Validation of 4-nitrophenol as an in vitro substrate probe for human liver CYP2E1 using cDNA expression and microsomal kinetic techniques. Biochemical Pharmacology, 46, 1975–1981.
   Google Scholar
• THUMIVIEL, K. E., KHARASCH, E. D., PODOLL, T. and KUNZE, K., 1993, Human liver microsomal enflurane defluorination catalyzed by cytochrome P-450 2E1. Drug Metabolism and Disposition, 21, 350–357.
   PubMed Web of Science ®Google Scholar
• TINEL, M., BELGHITI, J., DESCATOIRE V., AMOUYAL, G., LETTERON, P., GENEVE, J., LARREY, D. and PESSAYRE, D., 1987, Inactivation of human liver cytochrome P450 by the drug methoxsalen and other psoralen derivatives. Biochemical Pharmacology, 36, 951–955.
   Google Scholar
• TRACY, T. S., ROSENBLUTH, B. W., WRIGHTON, S. A., GONZALEZ, F. J. and KORZEKWA, K. R., 1995, Role of cytochrome-P450 2C9 and an allelic variant in the C.-hydroxylation of (r)-flurbiprofen and (s)-flurbiprofen. Biochemical Pharmacology, 4, 1269–1275.
   Web of Science ®Google Scholar
• TYNDALE, R., AOYAMA, T., BROLY, F., MATSUNAGA, T., INABA, T., KALOW W., GELBOIN, H. V., MEYER, U. A. and GONZALEZ, F. J., 1991, Identification of a new variant CYP2D6 allele lacking the codon encoding Lys-281: possible association with the poor metabolizer phenotype. Pharmacogenetics, 1, 26–32.
   Google Scholar
• URBAN, P., TRUAN, G., GAUTIER, J. C. and POMPON, D., 1993, Xenobiotic metabolism in humanized yeast: engineered yeast cells producing human NADPH-cytochrome P450 reductase, cytochrome b5, epoxide hydrolase and P450s. Biochemical Society Transactions, 21, 1028–1034.
   PubMed Web of Science ®Google Scholar
• VALERO, F., DE LA TORRE, R., BOOBIS, A. R., MURRAY, S. and SEGURA, J., 1990, Assay of caffeine metabolism in vitro by human liver microsomes using radio-high-performance liquid chromato-graphy. Journal of Pharmacology and Biomedical Analysis, 8, 783–787.
   PubMed Web of Science ®Google Scholar
• VERONESE, M. E., DOECKE, C. J., MACKENZIE, P. I., McMANus, M. E., MINERS, J. 0., REES, D. L., GASSER, R., MEYER, U. A. and BIRKETT, D. J., 1993, Site-directed mutation studies of human liver cytochrome P-450 isoenzymes in the CYP2C subfamily. Biochemical Journal, 289, 533–538.
   Google Scholar
• VERONESE M. E., MACKENZIE P. I., DOECKE, C. J., McMANus, M. E., MINERS, J. 0. and BIRKETT D. J., 1991, Tolbutamide and phenytoin hydroxylations by cDNA-expressed human liver cyto-chrome P4502C9. Biochemical and Biophysical Research Communications, 175, 1112–1118.
   Google Scholar
• VONMOLTKE, L. L., GREENBLATT, D. J., COURT, M. H., DUAN, S. X., HARMATZ, J. S. and SHADER, R. I., 1995, Inhibition of alprazolam and desipramine hydroxylation in-vitro by paroxetine and fluvoxamine—comparison with other selective serotonin reuptake inhibitor antidepressants. Journal of Clinical Psychopharmacology, 15, 125–131.
   PubMed Web of Science ®Google Scholar
• WATERMAN, M. R. and HILDEBRAND, M., 1994, Assessment of the Use of Single Cytochrome P450 Enzymes in Drug Research, (Bohn: Springer).
   Google Scholar
• WATKINS, P. B., WRIGHTON, S. A., MAUREL, P., SCHUETZ, E. G., MENDEZ -PICON, G., PARKER, G. A. and GUZELIAN, P. S., 1985, Identification of an inducible form of cytochrome P450 in human liver. Proceedings of the National Academy of Sciences, USA, 82, 6310–6314.
   Google Scholar
• WAXMAN, D. J., LAPENSON, D. P., AOYAMA, T., GELBOIN, H. V., GONZALEZ, F. J. and KORZEKWA, K., 1991, Steroid hormone hydroxylase specificities of eleven cDNA-expressed human cytochrome P450s. Archives of Biochemistry and Biophysics, 290, 160–166.
   PubMed Web of Science ®Google Scholar
• WEAVER, R. J., DICKINS, M. and BURKE, M. D., 1993, Cytochrome P450 2C9 is responsible for hydroxylation of the naphthoquinone antimalarial drug 58C80 in human liver. Biochemical Pharmacology, 46, 1183–1197.
   PubMed Web of Science ®Google Scholar
• WEISBERG, S., 1980, Applied Linear Regression (Chichester: John Wiley).
   Google Scholar
• WINTERS, D. K. and CEDERBAUM, A. I., 1992, Expression of a catalytically active human cytochrome P-4502E1 in Escherkhia coli. Biochimica et Biophysica Acta, 1156, 43–49.
   PubMed Web of Science ®Google Scholar
• WRIGHT, J. D., HELSBY, N. A. and WARD, S. A., 1995, The role of S-mephenytoin hydroxylase (CYP2C19) in the metabolism of the antimalarial biguanides. British Journal of Clinical Pharmacology, 39, 441–444.
   PubMed Web of Science ®Google Scholar
• WRIGHTON, S. A., THOMAS, P. E., RYAN, D. E. and LEVIN, W., 1987, Purification and characterization of ethanol-inducible human hepatic cytochrome P45OHLj. Archives of Biochemistry and Biophysics, 258, 292–297.
   PubMed Web of Science ®Google Scholar
• WRIGHTON, S. A., BRIAN, W. R., SARI, M. A., IWASAKI, M., GUENGERICH, F. P., RAUCY, J. L., MOLOWA D. T. and VANDENBRANDEN, M., 1990, Studies on the expression and metabolic capabilities of human liver cytochrome P4501I1A5 (HLp3). Molecular Pharmacology, 38, 207–213.
   Google Scholar
• WRIGHTON, S. A., RING, B. J., WATKINS, P. B. and VANDENBRANDEN, M., 1989, Identification of a polymorphically expressed member of the human cytochrome P-450III family. Molecular Pharmacology, 36, 97–105.
   PubMed Web of Science ®Google Scholar
• WRIGHTON, S. A., STEVENS, J. C., BECKER, G. W. and VANDENBRANDEN, M., 1993, Isolation and characterization of human liver cytochrome P450 2C19: correlation between 2C19 and S- mephenytoin C.-hydroxylation. Archives of Biochemistry and Biophysics, 306, 240-245. WRIGHTON, S. A. and VANDENBRANDEN, M., 1989, Isolation and characterization of human fetal liver cytochrome P450HLp2: a third member of the P450III gene family. Archives of Biochemistry and Biophysics, 268, 144–151.
   Web of Science ®Google Scholar
• YAMANO, S., NHAMBURO, P. T., AOYAMA, T., MEYER, U. A., INABA, T., KALOW W., GELBOIN, H. V., MCBRIDE, 0. W. and GONZALEZ, F. J., 1989, cDNA cloning and sequence and cDNA-directed expression of human P450 IIB1: identification of a normal and two variant cDNAs derived from the CYP2B locus on chromosome 19 and differential expression of the JIB mRNAs in human liver. Biochemistry, 28, 7340–7348.
   Google Scholar
• YAMANO S., TATSUNO, J. and GONZALEZ, F. J., 1990, The CYP2A3 gene product catalyzes coumarin 7-hydroxylation in human liver microsomes. Biochemistry, 29, 1322–1329.
   Google Scholar
• YAMAZAKI, H., Guo, Z. Y. and GUENGERICH, F. P., 1995, Selectivity of cytochrome P4502E1 in chlorzoxazone 6-hydroxylation. Drug Metabolism and Disposition, 23, 438–440.
   PubMed Web of Science ®Google Scholar
• YAMAZAI, H., Guo, Z. Y., PERSMARK M., MIMURA M., INOUE, K., GUENGERICH, F. P. and SHIMADA, T., 1994a, Bufuralol hydroxylation by cytochrome-P450 2D6 and 1A2 enzymes in human liver-microsomes. Molecular Pharmacology, 46, 568–577.
   Google Scholar
• YAMAZAKI, H., INUI, Y., YUN, C. H., GUENGERICH, F. P. and SHIMADA, T., 1992, Cytochrome P450 2E1 and 2A6 enzymes as major catalysts for metabolic activation of N-nitrosodialkylamines and tobacco-related nitrosamines in human liver microsomes. Carcinogenesis 13, 1789–1794.
   PubMed Web of Science ®Google Scholar
• YAMAZAKI, H., MIMURA M., SUGAHARA, C. and SHIMADA, T., 1994b, Catalytic roles of rat and human cytochrome-P450-2A enzymes in testosterone 7-a-hydroxylation and coumarin 7-hydroxylation. Biochemical Pharmacology, 48, 1524–1527.
   Google Scholar
• YASUMORI, T., Li, Q. H., YAMAZOE, Y., UEDA, M., TSUZUKI, T. and KATO, R., 1994, Lack of low Km diazepam N-demethylase in livers of poor metabolizers for S-mephenytoin C.-hydroxylation. Pharmacogenetics, 4, 323–331.
   PubMedGoogle Scholar
• YASUMORI, T., MURAYAMA, N., YAMAZOE, Y., ABE, A., NOGI, Y., FUKASAWA, T. and KATO, R., 1989, Expression of a human P-45011C gene in yeast cells using galactose-inducible expression system. Molecular Pharmacology, 35, 443–449.
   PubMed Web of Science ®Google Scholar
• Yoo, J. S., GUENGERICH, F. P. and YANG, C. S., 1988, Metabolism of N-nitrosodialkylamines by human liver microsomes. Cancer Research, 48, 1499–1504.
   PubMed Web of Science ®Google Scholar
• Yoo, J. S., IsuizAxi, H. and YANG, C. S., 1991, Enzyme kinetics of N-nitrosodimethylamine dem ethylas e in rodents and humans. IARC Science Publications, 366–369.
   Google Scholar
• YOSHIMOTO, K., ECHIZEN, H., CHIBA, K., TAM, M. and IsuizAxi, T., 1995, Identification of human CYP isoforrns involved in the metabolism of propranolol enantiomers—N-desisopropylation is mediated mainly by CYP1A2. British Journal of Clinical Pharmacology, 39, 421–431.
   PubMed Web of Science ®Google Scholar
• YUN, C. H., SHIMADA, T. and GUENGERICH, F. P., 1991, Purification and characterization of human liver microsomal cytochrome P-450 2A6. Molecular Pharmacology, 40, 679–685.
   PubMed Web of Science ®Google Scholar
• YUN, C. H., OKERHOLM, R. A. and GUENGERICH, F. P., 1993, Oxidation of the antihistaminic drug terfenadine in human liver microsomes. Role of cytochrome P-450 3A(4) in N-dealkylation and C-hydroxylation. Drug Metabolism and Disposition, 21, 403–409.
   PubMed Web of Science ®Google Scholar
• YUN, C. H., WOOD, M., WOOD, A. J. and GUENGERICH, F. P., 1992, Identification of the pharmacogenetic determinants of alfentanil metabolism: cytochrome P-450 3A4. An explanation of the variable elimination clearance. Anesthesiology, 77, 467–474.
   PubMed Web of Science ®Google Scholar
• ZANGER U. M., VILBOIS, F., HARDWICK, J. P. and MEYER, U. A., 1988, Absence of hepatic cytochrome P450bufI causes genetically deficient debrisoquine oxidation in man. Biochemistry, 27, 5447–5454.
   Google Scholar
• ZELDIN, D. C., DuBois, R. N., FALCK, J. R. and CAPDEVILA, J. H., 1995, Molecular-cloning, expression and characterization of an endogenous human cytochrome-P450 arachidonic-acid epoxygenase isoforrn. Archives of Biochemistry and Biophysics, 322, 76–86.
   PubMed Web of Science ®Google Scholar
• ZHOU, X. J., ZHOU -PAN, X. R., GAUTHIER, T., PLACIDI, M., MAUREL, P. and RAHMANI, R., 1993, Human liver microsomal cytochrome P450 3A isozymes mediated vindesine biotransformation. Metabolic drug interactions. Biochemical Pharmacology, 45, 853–861.
   Google Scholar