Cytochrome P450 3A and their regulation

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 369, Issue 1, 2004, Pages 105-124

  Burk, Oliver ^a   Wojnowski, Leszek ^b  

^a DR MARGARETE FISCHER BOSCH INSTITUTE OF CLINICAL PHARMACOLOGY   (Germany)

^b Department of Clinical Pharmacology ^*  (Germany)

Author keywords

CYP3A; Gene regulation; GR; HNF4 ; Induction; Pharmacogenetics; Polymorphism; PXR

Indexed keywords

CARBAMAZEPINE; CARCINOGEN; CLOTRIMAZOLE; CYCLOPHOSPHAMIDE; CYPROTERONE ACETATE; CYTOCHROME P450 3A; DEXAMETHASONE; ERYTHROMYCIN; HYPERFORIN; IFOSFAMIDE; ISOENZYME; LANSOPRAZOLE; LIVER PROTEIN; METYRAPONE; MEVINOLIN; MIDAZOLAM; MIFEPRISTONE; NIFEDIPINE; OMEPRAZOLE; PACLITAXEL; PANTOPRAZOLE; PHENOBARBITAL; PHENYLBUTAZONE; PHENYTOIN; PREDNISOLONE; PREDNISONE; RIFAMPICIN; RITONAVIR; SPIRONOLACTONE; UNINDEXED DRUG;

CANCER; CANCER RISK; CELL SUBPOPULATION; DISEASE PREDISPOSITION; DRUG DISTRIBUTION; DRUG METABOLISM; ENZYME ACTIVITY; GASTROINTESTINAL TRACT; GENE EXPRESSION; GENE LOCUS; GENETIC VARIABILITY; HUMAN; IMMUNOHISTOCHEMISTRY; KIDNEY; LIVER METABOLISM; NONHUMAN; PROTEIN ANALYSIS; PROTEIN EXPRESSION; REGULATORY MECHANISM; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; REVIEW;

ANIMALS; ARYL HYDROCARBON HYDROXYLASES; CYTOCHROME P-450 CYP3A; GENE EXPRESSION REGULATION, ENZYMOLOGIC; HUMANS; METABOLIC DETOXICATION, DRUG; OXIDOREDUCTASES, N-DEMETHYLATING; POLYMORPHISM, GENETIC; XENOBIOTICS;

EID: 0742321729     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00210-003-0815-3     Document Type: Review

References (180)

1. Ahsan CH, Renwick AG, Macklin B, Challenor VF, Waller DG, George CF (1991) Ethnic differences in the pharmacokinetics of oral nifedipine. Br J Clin Pharmacol 31:399-403
2. Amirimani B, Walker AH, Weber BL, Rebbeck TR (1999) RESPONSE: re: modification of clinical presentation of prostate tumors by a novel genetic variant in CYP3A4. J Natl Cancer Inst 91:1588-1590
3. Ando Y, Tateishi T, Sekido Y, Yamamoto T, Satoh T, Hasegawa Y, Kobayashi S, Katsumata Y, Shimokata K, Saito H (1999) Re: modification of clinical presentation of prostate tumors by a novel genetic variant in CYP3A4. J Natl Cancer Inst 91:1587-1590
4. Anttila S, Hukkanen J, Hakkola J, Stjernvall T, Beaune P, Edwards RJ, Boobis AR, Pelkonen O, Raunio H (1997) Expression and localization of CYP3A4 and CYP3A5 in human lung. Am J Respir Cell Mol Biol 16:242-249
5. Aoyama T, Yamano S, Waxman DJ, Lapenson DP, Meyer UA, Fischer V, Tyndale R, Inaba T, Kalow W, Gelboin HV et al (1989) 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. J Biol Chem 264:10388-10395
6. Ball SE, Scatina J, Kao J, Ferron GM, Fruncillo R, Mayer P, Weinryb I, Guida M, Hopkins PJ, Warner N, Hall J (1999) Population distribution and effects on drug metabolism of a genetic variant in the 5′ promoter region of CYP3A4. Clin Pharmacol Ther 66:288-294
7. Barwick JL, Quattrochi LC, Mills AS, Potenza C, Tukey RH, Guzelian PS (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. Mol Pharmacol 50:10-16
8. Bertilsson G, Heidrich J, Svensson K, Asman M, Jendeberg L, Sydow-Backman M, Ohlsson R, Postlind H, Blomquist P, Berkenstam A (1998) Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction. Proc Natl Acad Sci USA 95:12208-12213
9. Bertilsson G, Berkenstam A, Blomquist P (2001) Functionally conserved xenobiotic responsive enhancer in cytochrome P450 3A7. Biochem Biophys Res Commun 280:139-144
10. Blanco JG, Edick MJ, Hancock ML, Winick NJ, Dervieux T, Amylon MD, Bash RO, Behm FG, Camitta BM, Pui CH, Raimondi SC, Relling MV (2002) Genetic polymorphisms in CYP3A5, CYP3A4 and NQO1 in children who developed therapy-related myeloid malignancies. Pharmacogenetics 12:605-611
11. Blumberg B, Sabbagh Jr W, Juguilon H, Bolado Jr J, van Meter CM, Ong ES, Evans RM (1998) SXR, a novel steroid and xenobiotic-sensing nuclear receptor. Genes Dev 12:3195-3205
12. Boobis AR, Edwards RJ, Adams DA, Davies DS (1996) Dissecting the function of cytochrome P450. Br J Clin Pharmacol 42:81-89
13. Burk O, Tegude H, Koch I, Hustert E, Wolbold R, Glaeser H, Klein K, Fromm MF, Nuessler AK, Neuhaus P, Zanger UM, Eichelbaum M, Wojnowski L (2002) Molecular mechanisms of polymorphic CYP3A7 expression in adult human liver and intestine. J Biol Chem 277:24280-24288
14. Castaneda-Hernandez G, Hoyo-Vadillo C, Palma-Aguirre JA, Flores-Murrieta FJ (1993) Pharmacokinetics of oral nifedipine in different populations. J Clin Pharmacol 33:140-145
15. Chang TK, Yu L, Maurel P, Waxman DJ (1997) Enhanced cyclophosphamide and ifosfamide activation in primary human hepatocyte cultures: response to cytochrome P-450 inducers and autoinduction by oxazaphosphorines. Cancer Res 57:1946-1954
16. Chang TK, Bandiera SM, Chen J (2003) Constitutive androstane receptor and pregnane X receptor gene expression in human liver: interindividual variability and correlation with CYP2B6 mRNA levels. Drug Metab Dispos 31:7-10
17. Chou FC, Tzeng SJ, Huang JD (2001) Genetic polymorphism of cytochrome P450 3A5 in Chinese. Drug Metab Dispos 29:1205-1209
18. Curi-Pedrosa R, Daujat M, Pichard L, Ourlin JC, Clair P, Gervot L, Lesca P, Domergue J, Joyeux H, Fourtanier G et al (1994) Omeprazole and lansoprazole are mixed inducers of CYP1A and CYP3A in human hepatocytes in primary culture. J Pharmacol Exp Ther 269:384-392
19. Cvetkovic R, Goa K (2003) Lopinavir/ritonavir: a review of its use in the management of HIV infection. Drugs 63:769-802
20. Dai D, Tang J, Rose R, Hodgson E, Bienstock RJ, Mohrenweiser HW, Goldstein JA (2001) Identification of variants of CYP3 A4 and characterization of their abilities to metabolize testosterone and chlorpyrifos. J Pharmacol Exp Ther 299:825-831
21. Desai PB, Nallani SC, Sane RS, Moore LB, Goodwin BJ, Buckley DJ, Buckley AR (2002) Induction of cytochrome P450 3A4 in primary human hepatocytes and activation of the human pregnane X receptor by tamoxifen and 4-hydroxytamoxifen. Drug Metab Dispos 30:608-612
22. Domanski TL, He YA, Harlow GR, Halpert JR (2000) Dual role of human cytochrome P450 3A4 residue Phe-304 in substrate specificity and cooperativity. J Pharmacol Exp Ther 293:585-591
23. Domanski TL, Finta C, Halpert JR, Zaphiropoulos PG (2001) cDNA cloning and initial characterization of CYP3A43, a novel human cytochrome P450. Mol Pharmacol 59:386-392
24. Drocourt L, Pascussi JM, Assenat E, Fabre JM, Maurel P, Vilarem MJ (2001) Calcium channel modulators of the dihydropyridine family are human pregnane X receptor activators and inducers of CYP3A, CYP2B, and CYP2C in human hepatocytes. Drug Metab Dispos 29:1325-1331
25. Dussault I, Lin M, Hollister K, Wang EH, Synold TW, Forman BM (2001) Peptide mimetic HIV protease inhibitors are ligands for the orphan receptor SXR. J Biol Chem 276:33309-33312
26. Dussault I, Yoo HD, Lin M, Wang E, Fan M, Batta AK, Salen G, Erickson SK, Forman BM (2003) Identification of an endogenous ligand that activates pregnane X receptor-mediated sterol clearance. Proc Natl Acad Sci USA 100:833-838
27. Eiselt R, Domanski TL, Zibat A, Mueller R, Presecan-Siedel E, Hustert E, Zanger UM, Brockmoller J, Klenk HP, Meyer UA, Khan KK, He YA, Halpert JR, Wojnowski L (2001) Identification and functional characterization of eight CYP3A4 protein variants. Pharmacogenetics 11:447-458
28. Evans AM (2000) Influence of dietary components on the gastrointestinal metabolism and transport of drugs. Ther Drug Monit 22:131-136
29. Evans WE, Relling MV (1999) Pharmacogenomics: translating functional genomics into rational therapeutics. Science 286:487-491
30. Felix CA, Walker AH, Lange BJ, Williams TM, Winick NJ, Cheung NK, Lovett BD, Nowell PC, Blair IA, Rebbeck TR (1998) Association of CYP3A4 genotype with treatment-related leukemia. Proc Natl Acad Sci USA 95:13176-13181
31. Finta C, Zaphiropoulos PG (2000) The human cytochrome P450 3A locus. Gene evolution by capture of downstream exons. Gene 260:13-23
32. Finta C, Zaphiropoulos PG (2002) Intergenic mRNA molecules resulting from trans-splicing. J Biol Chem 277:5882-5890
33. Fukuen S, Fukuda T, Matsuda H, Sumida A, Yamamoto I, Inaba T, Azuma J (2002a) Identification of the novel splicing variants for the hPXR in human livers. Biochem Biophys Res Commun 298:433-438
34. Fukuen S, Fukuda T, Maune H, Ikenaga Y, Yamamoto I, Inaba T, Azuma J (2002b) Novel detection assay by PCR-RFLP and frequency of the CYP3A5 SNPs, CYP3A5*3 and *6, in a Japanese population. Pharmacogenetics 12:331-334
35. Garcia-Martin E, Martinez C, Pizarro RM, Garcia-Gamito FJ, Gullsten H, Raunio H, Agundez JA (2002) CYP3A4 variant alleles in white individuals with low CYP3A4 enzyme activity. Clin Pharmacol Ther 71:196-204
36. Geick A, Eichelbaum M, Burk O (2001) Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem 276:14581-14587
37. Gellner K, Eiselt R, Hustert E, Arnold H, Koch I, Haberl M, Deglmann CJ, Burk O, Buntefuss D, Escher S, Bishop C, Koebe HG, Brinkmann U, Klenk HP, Kleine K, Meyer UA, Wojnowski L (2001) Genomic organization of the human CYP3A locus: identification of a new, inducible CYP3A gene. Pharmacogenetics 11:111-121
38. Gibson GG, Plant NJ, Swales KE, Ayrton A, El-Sankary W (2002) Receptor-dependent transcriptional activation of cytochrome P4503A genes: induction mechanisms, species differences and interindividual variation in man. Xenobiotica 32:165-206
39. Gillam EM, Guo Z, Ueng YF, Yamazaki H, Cock I, Reilly PE, Hooper WD, Guengerich FP (1995) Expression of cytochrome P450 3A5 in Escherichia coli: effects of 5′ modification, purification, spectral characterization, reconstitution conditions, and catalytic activities [published erratum appears in Arch Biochem Biophys 1995 318:498]. Arch Biochem Biophys 317:374-384
40. Gillum JG, Israel DS, Polk RE (1993) Pharmacokinetic drug interactions with antimicrobial agents. Clin Pharmacokinet 25:450-482
41. Goh BC, Lee SC, Wang LZ. Fan L, Guo JY, Lamba J, Schuetz E, Lim R, Lim HL, Ong AB, Lee HS (2002) Explaining interindividual variability of docetaxel pharmacokinetics and pharmacodynamics in Asians through phenotyping and genotyping strategies. J Clin Oncol 20:3683-3690
42. Goodwin B, Hodgson E, Liddle C (1999) The orphan human pregnane X receptor mediates the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer module. Mol Pharmacol 56:1329-1339
43. Goodwin B, Hodgson E, D'Costa DJ, Robertson GR, Liddle C (2002) Transcriptional regulation of the human CYP3A4 gene by the constitutive androstane receptor. Mol Pharmacol 62:359-365
44. Goodwin B, Gauthier KC, Umetani M, Watson MA, Lochansky MI, Collins JL, Leitersdorf E, Mangelsdorf DJ, Kliewer SA, Repa JJ (2003) Identification of bile acid precursors as endogenous ligands for the nuclear xenobiotic pregnane X receptor. Proc Natl Acad Sci USA 100:223-228
45. Gorski JC, Hall SD, Jones DR, VandenBranden M, Wrighton SA (1994) Regioselective biotransformation of midazolam by members of the human cytochrome P450 3A (CYP3A) sub-family. Biochem Pharmacol 47:1643-1653
46. Goto M, Masuda S, Saito H, Uemoto S, Kiuchi T, Tanaka K, Inui K (2002) C3435T polymorphism in the MDR1 gene affects the enterocyte expression level of CYP3A4 rather than Pgp in recipients of living-donor liver transplantation. Pharmacogenetics 12:451-457
47. Grange JM, Winstanley PA, Davies PD (1994) Clinically significant drug interactions with antituberculosis agents. Drug Saf 11:242-251
48. Guengerich FP (1997) Role of cytochrome P450 enzymes in drug-drug interactions. Adv Pharmacol 43:7-35
49. Haehner BD, Gorski JC, Vandenbranden M, Wrighton SA, Janardan SK, Watkins PB, Hall SD (1996) Bimodal distribution of renal cytochrome P450 3A activity in humans. Mol Pharmacol 50:52-59
50. Hakkola J, Pasanen M, Purkunen R, Saarikoski S, Pelkonen O, Maenpaa J, Rane A, Raunio H (1994) Expression of xenobiotic-metabolizing cytochrome P450 forms in human adult and fetal liver. Biochem Pharmacol 48:59-64
51. Hamzeiy H, Vahdati-Mashhadian N, Edwards HJ, Goldfarb PS (2002) Mutation analysis of the human CYP3A4 gene 5′ regulatory region: population screening using non-radioactive SSCP. Mutat Res 500:103-110
52. Hashimoto H, Toide K, Kitamura R, Fujita M, Tagawa S, Itoh S, Kamataki T (1993) Gene structure of CYP3A4, an adult-specific form of cytochrome P450 in human livers, and its transcriptional control. Eur J Biochem 218:585-595
53. Hayhurst GP, Lee YH, Lambert G, Ward JM, Gonzalez FJ (2001) Hepatocyte nuclear factor 4alpha (nuclear receptor 2A1) is essential for maintenance of hepatic gene expression and lipid homeostasis. Mol Cell Biol 21:1393-1403
54. Hirota N, Ito K, Iwatsubo T, Green CE, Tyson CA, Shimada N, Suzuki H, Sugiyama Y (2001) In vitro/in vivo scaling of alprazolam metabolism by CYP3A4 and CYP3A5 in humans. Biopharm Drug Dispos 22:53-71
55. Hoffmeyer S, Burk O, von Richter O, Arnold HP, Brockmoller J, Johne A, Cascorbi I, Gerloff T, Roots I, Eichelbaum M, Brinkmann U (2000) Functional polymorphisms of the human multidrug-resistance gene: multiple sequence variations and correlation of one allele with P-glycoprotein expression and activity in vivo. Proc Natl Acad Sci USA 97:3473-3478
56. Honkakoski P, Zelko I, Sueyoshi T, Negishi M (1998) The nuclear orphan receptor CAR-retinoid X receptor heterodimer activates the phenobarbital- responsive enhancer module of the CYP2B gene. Mol Cell Biol 18:5652-5658
57. Hoyo-Vadillo C, Castaneda-Hernandez G, Herrera JE, Vidal-Garate J, Moreno-Ramos A, Chavez F, Hong E (1989) Pharmacokinetics of nifedipine slow release tablet in Mexican subjects: further evidence for an oxidation polymorphism. J Clin Pharmacol 29:816-820
58. Hsieh KP, Lin YY, Cheng CL, Lai ML, Lin MS, Siest JP, Huang JD (2001) Novel mutations of CYP3A4 in Chinese. Drug Metab Dispos 29:268-273
59. Huang Z, Fasco MJ, Figge HL, Keyomarsi K, Kaminsky LS (1996) Expression of cytochromes P450 in human breast tissue and tumors. Drug Metab Dispos 24:899-905
60. Hukkanen J, Hakkola J, Anttila S, Piipari R, Karjalainen A, Pelkonen O, Raunio H (1997) Detection of mRNA encoding xenobiotic-metabolizing cytochrome P450s in human bronchoalveolar macrophages and peripheral blood lymphocytes. Mol Carcinog 20:224-230
61. Hukkanen J, Lassila A, Paivarinta K, Valanne S, Sarpo S, Hakkola J, Pelkonen O, Raunio H (2000) Induction and regulation of xenobiotic-metabolizing cytochrome P450s in the human A549 lung adenocarcinoma cell line. Am J Respir Cell Mol Biol 22:360-366
62. Hukkanen J, Vaisanen T, Lassila A, Piipari R, Anttila S, Pelkonen O, Raunio H, Hakkola J (2003) Regulation of CYP3A5 by glucocorticoids and cigarette smoke in human lung-derived cells. J Pharmacol Exp Ther 304:745-752
63. Hunt CM, Watkins PB, Saenger P, Stave GM, Barlascini N, Watlington CO, Wright Jr JT, Guzelian PS (1992) Heterogeneity of CYP3A isoforms metabolizing erythromycin and cortisol. Clin Pharmacol Ther 51:18-23
64. Hustert E, Zibat A, Presecan-Siedel E, Eiselt R, Mueller R, Fuss C, Brehm I, Brinkmann U, Eichelbaum M, Wojnowski L, Burk O (2001a) Natural protein variants of pregnane x receptor with altered transactivation activity toward cyp3a4. Drug Metab Dispos 29:1454-1459
65. Hustert E, Haberl M, Burk O, Wolbold R, He YQ, Klein K, Nuessler AC, Neuhaus P, Klattig J, Eiselt R, Koch I, Zibat A, Brockmoller J, Halpert JR, Zanger UM, Wojnowski L (2001b) The genetic determinants of the CYP3A5 polymorphism. Pharmacogenetics 11:773-779
66. Janardan SK, Lown KS, Schmiedlin-Ren P, Thummel KE, Watkins PB (1996) Selective expression of CYP3A5 and not CYP3A4 in human blood. Pharmacogenetics 6:379-385
67. Jones SA, Moore LB, Shenk JL, Wisely GB, Hamilton GA, McKee DD, Tomkinson NC, LeCluyse EL, Lambert MH, Willson TM, Kliewer SA, Moore JT (2000) The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution. Mol Endocrinol 14:27-39
68. Jounaidi Y, Guzelian PS, Maurel P, Vilarem MJ (1994) Sequence of the 5′-flanking region of CYP3A5: comparative analysis with CYP3A4 and CYP3A7. Biochem Biophys Res Commun 205:1741-1747
69. Jounaidi Y, Hyrailles V, Gervot L, Maurel P (1996) Detection of CYP3A5 allelic variant: a candidate for the polymorphic expression of the protein? Biochem Biophys Res Commun 221:466-470
70. Jover R, Bort R, Gomez-Lechon MJ, Castell JV (2001) Cytochrome P450 regulation by hepatocyte nuclear factor 4 in human hepatocytes: a study using adenovirus-mediated antisense targeting. Hepatology 33:668-675
71. Kinirons MT, O'Shea D, Downing TE, Fitzwilliam AT, Joellenbeck L, Groopman JD, Wilkinson GR, Wood AJ (1993) Absence of correlations among three putative in vivo probes of human cytochrome P4503A activity in young healthy men. Clin Pharmacol Ther 54:621-629
72. Kinirons MT, O'Shea D, Kim RB, Groopman JD, Thummel KE, Wood AJ, Wilkinson GR (1999) Failure of erythromycin breath test to correlate with midazolam clearance as a probe of cytochrome P4503A. Clin Pharmacol Ther 66:224-231
73. Kivisto KT, Fritz P, Linder A, Friedel G, Beaune P, Kroemer HK (1995) Immunohistochemical localization of cytochrome P450 3A in human pulmonary carcinomas and normal bronchial tissue. Histochem Cell Biol 103:25-29
74. Kivisto KT, Bookjans G, Fromm MF, Griese EU, Munzel P, Kroemer HK (1996a) Expression of CYP3A4, CYP3A5 and CYP3A7 in human duodenal tissue. Br J Clin Pharmacol 42:387-389
75. Kivisto KT, Griese EU, Fritz P, Linder A, Hakkola J, Raunio H, Beaune P, Kroemer HK (1996b) Expression of cytochrome P 450 3A enzymes in human lung: a combined RT-PCR and immunohistochemical analysis of normal tissue and lung tumours. Naunyn-Schmiedebergs Arch Pharmacol 353:207-212
76. Kliewer SA, Moore JT, Wade L, Staudinger JL, Watson MA, Jones SA, McKee DD, Oliver BB, Willson TM, Zetterstrom RH, Perlmann T, Lehmann JM (1998) An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway. Cell 92:73-82
77. Kocarek TA, Schuetz EG, Strom SC, Fisher RA, Guzelian PS (1995) Comparative analysis of cytochrome P4503A induction in primary cultures of rat, rabbit, and human hepatocytes. Drug Metab Dispos 23:415-421
78. Koch I, Weil R, Wolbold R, Brockmoller J, Hustert E, Burk O, Nuessler A, Neuhaus P, Eichelbaum M, Zanger U, Wojnowski L (2002) Interindividual variability and tissue-specificity in the expression of cytochrome P450 3A mRNA. Drug Metab Dispos 30:1108-1114
79. Kolars JC, Schmiedlin-Ren P, Schuetz JD, Fang C, Watkins PB (1992) Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes. J Clin Invest 90:1871-1878
80. Kolars JC, Lown KS, Schmiedlin-Ren P, Ghosh M, Fang C, Wrighton SA, Merion RM, Watkins PB (1994) CYP3A gene expression in human gut epithelium. Pharmacogenetics 4:247-259
81. Kostrubsky VE, Lewis LD, Strom SC, Wood SG, Schuetz EG, Schuetz JD, Sinclair PR, Wrighton SA, Sinclair JF (1998) Induction of cytochrome P4503A by taxol in primary cultures of human hepatocytes. Arch Biochem Biophys 355:131-136
82. Krivoruk Y, Kinirons MT, Wood AJ, Wood M (1994) Metabolism of cytochrome P4503A substrates in vivo administered by the same route: lack of correlation between alfentanil clearance and erythromycin breath test. Clin Pharmacol Ther 56:608-614
83. Krovat BC, Tracy JH, Omiecinski CJ (2000) Fingerprinting of cytochrome P450 and microsomal epoxide hydrolase gene expression in human blood cells. Toxicol Sci 55:352-360
84. Kuehl P, Zhang J, Lin Y, Lamba J, Assem M, Schuetz J, Watkins PB, Daly A, Wrighton SA, Hall SD, Maurel P, Relling M, Brimer C, Yasuda K, Venkataramanan R, Strom S, Thummel K, Boguski MS, Schuetz E (2001) Sequence diversity in CYP3A promoters and characterization of the genetic basis of polymorphic CYP3A5 expression. Nat Genet 27:383-391
85. Lakehal F, Wendum D, Barbu V, Becquemont L, Poupon R, Balladur P, Hannoun L, Ballet F, Beaune PH, Housset C (1999) Phase I and phase II drug-metabolizing enzymes are expressed and heterogeneously distributed in the biliary epithelium. Hepatology 30:1498-506
86. Lamba JK, Lin YS, Schuetz EG, Thummel KE (2002a) Genetic contribution to variable human CYP3A-mediated metabolism. Adv Drug Deliv Rev 54:1271-1294
87. Lamba JK, Lin YS, Thummel K, Daly A, Watkins PB, Strom S, Zhang J, Schuetz EG (2002b) Common allelic variants of cytochrome P4503A4 and their prevalence in different populations. Pharmacogenetics 12:121-132
88. Landes N, Pfluger P, Kluth D, Birringer M, Ruhl R, Bol GF, Glatt H, Brigelius-Flohe R (2003) Vitamin E activates gene expression via the pregnane X receptor. Biochem Pharmacol 65:269-273
89. Lechevrel M, Casson AG, Wolf CR, Hardie LJ, Flinterman MB, Montesano R, Wild CP (1999) Characterization of cytochrome P450 expression in human oesophageal mucosa. Carcinogenesis 20:243-248
90. Lehmann JM, McKee DD, Watson MA, Willson TM, Moore JT, Kliewer SA (1998) The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. J Clin Invest 102:1016-1023
91. Li AP, Kaminski DL, Rasmussen A (1995) Substrates of human hepatic cytochrome P450 3A4. Toxicology 104:1-8
92. Li J, Ning G, Duncan SA (2000) Mammalian hepatocyte differentiation requires the transcription factor HNF-4alpha. Genes Dev 14:464-474
93. Liddle C, Goodwin BJ, George J, Tapner M, Farrell GC (1998) Separate and interactive regulation of cytochrome P450 3A4 by triiodothyronine, dexamethasone, and growth hormone in cultured hepatocytes. J Clin Endocrinol Metab 83:2411-2416
94. Lin YS, Lockwood GF, Graham MA, Brian WR, Loi CM, Dobrinska MR, Shen DD, Watkins PB, Wilkinson GR, Kharasch ED, Thummel KE (2001) In-vivo phenotyping for CYP3A by a single-point determination of midazolam plasma concentration. Pharmacogenetics 11:781-791
95. Lin YS, Dowling AL, Quigley SD, Farin FM, Zhang J, Lamba J, Schuetz EG, Thummel KE (2002) Co-regulation of CYP3A4 and CYP3A5 and contribution to hepatic and intestinal midazolam metabolism. Mol Pharmacol 62:162-172
96. Lown KS, Kolars JC, Thummel KE, Barnett JL, Kunze KL, Wrighton SA, Watkins PB (1994) Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel. Lack of prediction by the erythromycin breath test [published erratum appears in Drug Metab Dispos 1995 Mar;23(3):following table of contents]. Drug Metab Dispos 22:947-955
97. Lucey MR, Kolars JC, Merion RM, Campbell DA, Aldrich M, Watkins PB (1990) Cyclosporin toxicity at therapeutic blood levels and cytochrome P-450 IIIA. Lancet 335:11-15
98. Macphee IA, Fredericks S, Tai T, Syrris P, Carter ND, Johnston A, Goldberg L, Holt DW (2002) Tacrolimus pharmacogenetics: polymorphisms associated with expression of cytochrome p4503A5 and P-glycoprotein correlate with dose requirement. Transplantation 74:1486-1489
99. Marill J, Cresteil T, Lanotte M, Chabot GG (2000) Identification of human cytochrome P450s involved in the formation of all-trans-retinoic acid principal metabolites. Mol Pharmacol 58:1341-1348
100. Martin JE, Daoud AJ, Schroeder TJ, First MR (1999) The clinical and economic potential of cyclosporin drug interactions. Pharmacoeconomics 15:317-337
101. Masubuchi N, Li AP, Okazaki O (1998) An evaluation of the cytochrome P450 induction potential of pantoprazole in primary human hepatocytes. Chem Biol Interact 114:1-13
102. McCune JS, Hawke RL, LeCluyse EL, Gillenwater HH, Hamilton G, Ritchie J, Lindley C (2000) In vivo and in vitro induction of human cytochrome P4503A4 by dexamethasone. Clin Pharmacol Ther 68:356-366
103. McKinnon RA, Burgess WM, Hall PM, Roberts-Thomson SJ, Gonzalez FJ, McManus ME (1995) Characterisation of CYP3A gene subfamily expression in human gastrointestinal tissues. Gut 36:259-267
104. Molowa DT, Schuetz EG, Wrighton SA, Watkins PB, Kremers P, Mendez-Picon G, Parker GA, Guzelian PS (1986) Complete cDNA sequence of a cytochrome P-450 inducible by glucocorticoids in human liver. Proc Natl Acad Sci USA 83:5311-5315
105. Moore LB, Goodwin B, Jones SA, Wisely GB, Serabjit-Singh CJ, Willson TM, Collins JL, Kliewer SA (2000a) St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor. Proc Natl Acad Sci USA 97:7500-7502
106. Moore LB, Parks DJ, Jones SA, Bledsoe RK, Consler TG, Stimmel JB, Goodwin B, Liddle C, Blanchard SG, Willson TM, Collins JL, Kliewer SA (2000b) Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands [in process citation]. J Biol Chem 275:15122-15127
107. Murray GI, Barnes TS, Sewell HF, Ewen SW, Melvin WT, Burke MD (1988) The immunocytochemical localisation and distribution of cytochrome P-450 in normal human hepatic and extra-hepatic tissues with a monoclonal antibody to human cytochrome P-450. Br J Clin Pharmacol 25:465-475
108. Murray GI, Pritchard S, Melvin WT, Burke MD (1995) Cytochrome P450 CYP3A5 in the human anterior pituitary gland. FEBS Lett 364:79-82
109. Murray GI, McFadyen MC, Mitchell RT, Cheung YL, Kerr AC, Melvin WT (1999) Cytochrome P450 CYP3A in human renal cell cancer. Br J Cancer 79:1836-1842
110. Nakamoto T, Hase I, Imaoka S, Hiroi T, Oda Y, Asada A, Funae Y (2000) Quantitative RT-PCR for CYP3A4 mRNA in human peripheral lymphocytes: induction of CYP3A4 in lymphocytes and in liver by rifampicin. Pharmacogenetics 10:571-575
111. Nowakowski-Gashaw I, Mrozikiewicz PM, Roots I, Brockmoller J (2002) Rapid quantification of CYP3A4 expression in human leukocytes by real-time reverse transcription-PCR. Clin Chem 48:366-370
112. Ohmori S, Fujiki N, Nakasa H, Nakamura H, Ishii I, Itahashi K, Kitada M (1998a) Steroid hydroxylation by human fetal CYP3A7 and human NADPH-cytochrome P450 reductase co-expressed in insect cells using baculovirus. Res Commun Mol Pathol Pharmacol 100:15-28
113. Ohmori S, Nakasa H, Asanome K, Kurose Y, Ishii I, Hosokawa M, Kitada M (1998b) Differential catalytic properties in metabolism of endogenous and exogenous substrates among CYP3A enzymes expressed in COS-7 cells. Biochim Biophys Acta 1380:297-304
114. Ourlin JC, Jounaidi Y, Maurel P, Vilarem MJ (1997) Role of the liver-enriched transcription factors C/EBP alpha and DBP in the expression of human CYP3A4 and CYP3A7. J Hepatol 2:54-62
115. Ozdemir V, Kalowa W, Tang BK, Paterson AD, Walker SE, Endrenyi L, Kashuba AD (2000) Evaluation of the genetic component of variability in CYP3A4 activity: a repeated drug administration method. Pharmacogenetics 10:373-388
116. Paine MF, Khalighi M, Fisher JM, Shen DD, Kunze KL, Marsh CL, Perkins JD, Thummel KE (1997) Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. J Pharmacol Exp Ther 283:1552-1562
117. Paris PL, Kupelian PA, Hall JM, Williams TL, Levin H, Klein EA, Casey G, Witte JS (1999) Association between a CYP3A4 genetic variant and clinical presentation in African-American prostate cancer patients. Cancer Epidemiol Biomarkers Prev 8:901-905
118. Pascussi JM, Drocourt L, Fabre JM, Maurel P, Vilarem MJ (2000a) Dexamethasone induces pregnane X receptor and retinoid X receptor-alpha expression in human hepatocytes: synergistic increase of CYP3A4 induction by pregnane X receptor activators. Mol Pharmacol 58:361-372
119. Pascussi JM, Gerbal-Chaloin S, Fabre JM, Maurel P, Vilarem MJ (2000b) Dexamethasone enhances constitutive androstane receptor expression in human hepatocytes: consequences on cytochrome P450 gene regulation. Mol Pharmacol 58:1441-1450
120. Pascussi JM, Drocourt L, Gerbal-Chaloin S, Fabre JM, Maurel P, Vilarem MJ (2001) Dual effect of dexamethasone on CYP3A4 gene expression in human hepatocytes. Sequential role of glucocorticoid receptor and pregnane X receptor. Eur J Biochem 268:6346-6358
121. Paulussen A, Lavrijsen K, Bohets H, Hendrickx J, Verhasselt P, Luyten W, Konings F, Armstrong M (2000) Two linked mutations in transcriptional regulatory elements of the CYP3A5 gene constitute the major genetic determinant of polymorphic activity in humans [in process citation]. Pharmacogenetics 10:415-04
122. Pichard L, Fabre I, Fabre G, Domergue J, Saint Aubert B, Mourad G, 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 Metab Dispos 18:595-606
123. Piipari R, Savela K, Nurminen T, Hukkanen J, Raunio H, Hakkola J, Mantyla T, Beaune P, Edwards RJ, Boobis AR, Anttila S (2000) Expression of CYP1A1, CYP1B1 and CYP3A, and polycyclic aromatic hydrocarbon-DNA adduct formation in bronchoalveolar macrophages of smokers and non-smokers. Int J Cancer 86:610-616
124. Ratanasavanh D, Beaune P, Morel F, Flinois JP, Guengerich FP, Guillouzo A (1991) Intralobular distribution and quantitation of cytochrome P-450 enzymes in human liver as a function of age. Hepatology 13:1142-1151
125. Rebbeck TR, Jaffe JM, Walker AH, Wein AJ, Malkowicz SB (1998) Modification of clinical presentation of prostate tumors by a novel genetic variant in CYP3A4 [published erratum appears in J Natl Cancer Inst 1999 91:1082]. J Natl Cancer Inst 90:1225-1229
126. Rodriguez-Antona C, Bort R, Jover R, Tindberg N, Ingelman-Sundberg M, Gomez-Lechon MJ, Castell JV (2003) Transcriptional regulation of human CYP3A4 basal expression by CCAAT enhancer-binding protein alpha and hepatocyte nuclear factor-3gamma. Mol Pharmacol 63:1180-1189
127. Romani A, Guerra E, Trerotola M, Alberti S (2003) Detection and analysis of spliced chimeric mRNAs in sequence databanks. Nucleic Acids Res 31:e17
128. Sakaeda T, Nakamura T, Okumura K (2003) Pharmacogenetics of MDR1 and its impact on the pharmacokinetics and pharmacodynamics of drugs. Pharmacogenomics 4:397-410
129. Santos A, Zanetta S, Cresteil T, Deroussent A, Pein F, Raymond E, Vernillet L, Risse ML, Boige V, Gouyette A, Vassal G (2000) Metabolism of irinotecan (CPT-11) by CYP3A4 and CYP3A5 in humans. Clin Cancer Res 6:2012-2020
130. Sata F, Sapone A, Elizondo G, Stocker P, Miller VP, Zheng W, Raunio H, Crespi CL, Gonzalez FJ (2000) CYP3A4 allelic variants with amino acid substitutions in exons 7 and 12: evidence for an allelic variant with altered catalytic activity. Clin Pharmacol Ther 67:48-56
131. Schellens JH, Soons PA, Breimer DD (1988) Lack of bimodality in nifedipine plasma kinetics in a large population of healthy subjects. Biochem Pharmacol 37:2507-2510
132. Schmiedlin-Ren P, Thummel KE, Fisher JM, Paine MF, Lown KS, Watkins PB (1997) Expression of enzymatically active CYP3A4 by Caco-2 cells grown on extracellular matrix-coated permeable supports in the presence of 1alpha,25-dihydroxyvitamin D3. Mol Pharmacol 51:741-754
133. Schmiedlin-Ren P, Thummel KE, Fisher JM, Paine MF, Watkins PB (2001) Induction of cyp3a4 by 1alpha,25-dihydroxyvitamin d(3) is human cell line-specific and is unlikely to involve pregnane x receptor. Drug Metab Dispos 29:1446-1453
134. Schuetz EG (2001) Induction of cytochromes P450. Curr Drug Metab 2:139-147
135. Schuetz EG, Guzelian PS (1984) Induction of cytochrome P-450 by glucocorticoids in rat liver. II. Evidence that glucocorticoids regulate induction of cytochrome P-450 by a nonclassical receptor mechanism. J Biol Chem 259:2007-2012
136. Schuetz JD, Beach DL, Guzelian PS (1994) Selective expression of cytochrome P450 CYP3A mRNAs in embryonic and adult human liver. Pharmacogenetics 4:11-20
137. Schuetz JD, Schuetz EG, Thottassery JV, Guzelian PS, Strom S, Sun D (1996) Identification of a novel dexamethasone responsive enhancer in the human CYP3A5 gene and its activation in human and rat liver cells. Mol Pharmacol 49:63-72
138. Sempoux C, Starkel P, Stevens M, Van Den Berge V, Horsmans Y (1999) Cytochrome P450 3A proteins are expressed in B lymphocytes but not in T lymphocytes. Pharmacogenetics 9:263-265
139. Shih PS, Huang JD (2002) Pharmacokinetics of midazolam and 1′-hydroxymidazolam in Chinese with different CYP3A5 genotypes. Drug Metab Dispos 30:1491-1496
140. Shimada T, Yamazaki H, Mimura M, Inui Y, Guengerich FP (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. J Pharmacol Exp Ther 270:414-423
141. Smirlis D, Muangmoonchai R, Edwards M, Phillips IR, Shephard EA (2001) Orphan receptor promiscuity in the induction of cytochromes p450 by xenobiotics. J Biol Chem 276:12822-12826
142. Spurdle AB, Goodwin B, Hodgson E, Hopper JL, Chen X, Purdie DM, McCredie MR, Giles GG, Chenevix-Trench G, Liddle C (2002) The CYP3A4*1B polymorphism has no functional significance and is not associated with risk of breast or ovarian cancer. Pharmacogenetics 12:355-366
143. Standop J, Schneider MB, Ulrich A, Chauhan S, Moniaux N, Buchler MW, Batra SK, Pour PM (2002) The pattern of xenobiotic-metabolizing enzymes in the human pancreas. J Toxicol Environ Health A 65:1379-1400
144. Staudinger JL, Goodwin B, Jones SA, Hawkins-Brown D, MacKenzie KI, LaTour A, Liu Y, Klaassen CD, Brown KK, Reinhard J, Willson TM, Koller BH, Kliewer SA (2001) The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proc Natl Acad Sci USA 98:3369-3374
145. Stein CM, Kinirons MT, Pincus T, Wilkinson GR, Wood AJ (1996) Comparison of the dapsone recovery ratio and the erythromycin breath test as in vivo probes of CYP3A activity in patients with rheumatoid arthritis receiving cyclosporine. Clin Pharmacol Ther 59:47-51
146. Sumida A, Kinoshita K, Fukuda T, Matsuda H, Yamamoto I, Inaba T, Azuma J (1999) Relationship between mRNA levels quantified by reverse transcription-competitive PCR and metabolic activity of CYP3A4 and CYP2E1 in human liver. Biochem Biophys Res Commun 262:499-503
147. Sy SK, Ciaccia A, Li W, Roberts EA, Okey A, Kalow W, Tang BK (2002) Modeling of human hepatic CYP3A4 enzyme kinetics, protein, and mRNA indicates deviation from log-normal distribution in CYP3A4 gene expression. Eur J Clin Pharmacol 58:357-365
148. Synold TW, Dussault I, Forman BM (2001) The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux. Nat Med 7:584-590
149. Takeshita A, Koibuchi N, Oka J, Taguchi M, Shishiba Y, Ozawa Y (2001) Bisphenol-A, an environmental estrogen, activates the human orphan nuclear receptor, steroid and xenobiotic receptor-mediated transcription. Eur J Endocrinol 145:513-517
150. Tateishi T, Watanabe M, Moriya H, Yamaguchi S, Sato T, Kobayashi S (1999) No ethnic difference between Caucasian and Japanese hepatic samples in the expression frequency of CYP3A5 and CYP3A7 proteins. Biochem Pharmacol 57:935-939
151. Tayeb MT, Clark C, Sharp L, Haites NE, Rooney PH, Murray GI, Payne SN, McLeod HL (2002) CYP3A4 promoter variant is associated with prostate cancer risk in men with benign prostate hyperplasia. Oncol Rep 9:653-655
152. Thompson PD, Jurutka PW, Whitfield GK, Myskowski SM, Eichhorst KR, Dominguez CE, Haussler CA, Haussler MR (2002) Liganded VDR induces CYP3A4 in small intestinal and colon cancer cells via DR3 and ER6 vitamin D responsive elements. Biochem Biophys Res Commun 299:730-738
153. Thummel KE, Wilkinson GR (1998) In vitro and in vivo drug interactions involving human CYP3A. Annu Rev Pharmacol Toxicol 38:389-430
154. Thummel KE, Brimer C, Yasuda K, Thottassery J, Senn T, Lin Y, Ishizuka H, Kharasch E, Schuetz J, Schuetz (2001) Transcriptional control of intestinal cytochrome P-4503A by 1alpha,25-dihydroxy vitamin D3. Mol Pharmacol 60:1399-1406
155. Tirona RG, Lee W, Leake BF, Lan LB, Cline CB, Lamba V, Parviz F, Duncan SA, Inoue Y, Gonzalez FJ, Schuetz EG, Kim RB (2003) The orphan nuclear receptor HNF4alpha determines PXR-and CAR-mediated xenobiotic induction of CYP3A4. Nat Med 9:220-224
156. Van Schaik RH, van der Heiden IP, van den Anker JN, Lindemans J (2002) CYP3A5 variant allele frequencies in Dutch Caucasians. Clin Chem 48:1668-1671
157. Von Ahsen N, Richter M, Grupp C, Ringe B, Oellerich M, Armstrong VW (2001) No influence of the MDR-1 C3435T polymorphism or a CYP3A4 promoter polymorphism (CYP3A4-V allele) on dose-adjusted cyclosporin A trough concentrations or rejection incidence in stable renal transplant recipients. Clin Chem 47:1048-1052
158. Walker AH, Jaffe JM, Gunasegaram S, Cummings SA, Huang CS, Chern HD, Olopade OI, Weber BL, Rebbeck TR (1998) Characterization of an allelic variant in the nifedipine-specific element of CYP3A4: ethnic distribution and implications for prostate cancer risk. Mutations in brief no. 191. Online. Hum Mutat 12:289
159. Wall JD, Pritchard JK (2003) Haplotype blocks and linkage disequilibrium in the human genome. Nat Rev Genet 4:587-597
160. Wandel C, Witte JS, Hall JM, Stein CM, Wood AJ, Wilkinson GR (2000) CYP3A activity in African American and European American men: population differences and functional effect of the CYP3A4*1B5′-promoter region polymorphism. Clin Pharmacol Ther 68:82-91
161. Wang H, Dick R, Yin H, Licad-Coles E, Kroetz DL, Szklarz G, Harlow G, Halpert JR, Correia MA (1998) Structure-function relationships of human liver cytochromes P450 3A: aflatoxin B1 metabolism as a probe. Biochemistry 37:12536-12545
162. Watkins PB, Wrighton SA, Schuetz EG, Molowa DT, Guzelian PS (1987) Identification of glucocorticoid-inducible cytochromes P-450 in the intestinal mucosa of rats and man. J Clin Invest 80:1029-1036
163. Watkins PB, Murray SA, Winkelman LG, Heuman DM, Wrighton SA, Guzelian PS (1989) Erythromycin breath test as an assay of glucocorticoid-inducible liver cytochromes P-450. Studies in rats and patients. J Clin Invest 83:688-697
164. Watkins RE, Wisely GB, Moore LB, Collins JL, Lambert MH, Williams SP, Willson TM, Kliewer SA, Redinbo MR (2001) The human nuclear xenobiotic receptor PXR: structural determinants of directed promiscuity. Science 292:2329-2333
165. Watkins RE, Maglich JM, Moore LB, Wisely GB, Noble SM, Davis-Searles PR, Lambert MH, Kliewer SA, Redinbo MR (2003) 2.1 A crystal structure of human PXR in complex with the St. John's wort compound hyperforin. Biochemistry 42:1430-1438
166. Westlind A, Lofberg L, Tindberg N, Andersson TB, Ingelman-Sundberg M (1999) Interindividual differences in hepatic expression of CYP3A4: relationship to genetic polymorphism in the 5′-upstream regulatory region. Biochem Biophys Res Commun 259:201-205
167. Westlind A, Malmebo S, Johansson I, Otter C, Andersson TB, Ingelman-Sundberg M, Oscarson M (2001) Cloning and tissue distribution of a novel human cytochrome p450 of the CYP3A subfamily, CYP3A43. Biochem Biophys Res Commun 281:1349-1355
168. Westlind-Johnsson A, Malembo S, Johansson A, Otter C, Andersson TB, Johansson I, Erwards RJ, Boobis AR, Ingelman-Sundberg M (2003) Comparative analysis of CYP3A expression in human liver suggests only a minor role for CYP3A5 in drug metabolism. Drug Metab Dispos 31:1-8
169. Wilkinson GR (1996) Cytochrome P4503A (CYP3A) metabolism: prediction of in vivo activity in humans. J Pharmacokinet Biopharm 24:475-490
170. Williams JA, Ring BJ, Cantrell VE, Jones DR, Eckstein J, Ruterbories K, Hamman MA, Hall SD, Wrighton SA (2002) Comparative metabolic capabilities of CYP3A4, CYP3A5, and CYP3A7. Drug Metab Dispos 30:883-891
171. Wojnowski L, Hustert E, Klein K, Goldammer M, Haberl M, Kirchheiner J, Koch I, Klattig J, Zanger U, Brockmoller J (2002) Re: modification of clinical presentation of prostate tumors by a novel genetic variant in CYP3A4. J Natl Cancer Inst 94:630-631
172. Wright MC (1999) The cytochrome P450 3A4 inducer metyrapone is an activator of the human pregnane X receptor. Biochem Soc Trans 27:387-391
173. Wrighton SA, Brian WR, Sari MA, Iwasaki M, Guengerich FP, Raucy JL, Molowa DT, Vandenbranden M (1990) Studies on the expression and metabolic capabilities of human liver cytochrome P450IIIA5 (HLp3). Mol Pharmacol 38:207-213
174. Xie W, Barwick JL, Downes M, Blumberg B, Simon CM, Nelson MC, Neuschwander-Tetri BA, Brunt EM, Guzelian PS, Evans RM (2000a) Humanized xenobiotic response in mice expressing nuclear receptor SXR." Nature 406:435-439
175. Xie W, Barwick JL, Simon CM, Pierce AM, Safe S, Blumberg B, Guzelian PS, Evans (2000b) Reciprocal activation of xenobiotic response genes by nuclear receptors SXR/PXR and CAR. Genes Dev 14:3014-3023
176. Xie W, Radominska-Pandya A, Shi Y, Simon CM, Nelson MC, Ong ES, Waxman DJ, Evans RM (2001) An essential role for nuclear receptors SXR/PXR in detoxification of cholestatic bile acids. Proc Natl Acad Sci USA 98:3375-3380
177. Yokose T, Doy M, Taniguchi T, Shimada T, Kakiki M, Horie T, Matsuzaki Y, Mukai K (1999) Immunohistochemical study of cytochrome P450 2C and 3A in human non-neoplastic and neoplastic tissues. Virchows Arch 434:401-411
178. Zhang J, Kuehl P, Green ED, Touchman JW, Watkins PB, Daly A, Hall SD, Maurel P, Relling M, Brimer C, Yasuda K, Wrighton SA, Hancock M, Kim RB, Strom S, Thummel K, Russell CG, Hudson Jr JR, Schuetz EG, Boguski MS (2001) The human pregnane X receptor: genomic structure and identification and functional characterization of natural allelic variants. Pharmacogenetics 11:555-572
179. Zheng H, Webber S, Zeevi A, Schuetz E, Zhang J, Bowman P, Boyle G, Law Y, Miller S, Lamba J, Burckart GJ (2003) Tacrolimus dosing in pediatric heart transplant patients is related to CYP3A5 and MDR1 gene polymorphisms. Am J Transplant 3:477-483
180. Zhu B, Liu ZQ, Chen GL, Chen XP, Ou-Yang DS, Wang LS, Huang SL, Tan ZR, Zhou HH (2003) The distribution and gender difference of CYP3A activity in Chinese subjects. Br J Clin Pharmacol 55:264-269