Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes

Journal of Clinical Investigation

Volumn 90, Issue 5, 1992, Pages 1871-1878

  Kolars, Joseph C ^a   Schmiedlin Ren, Phyllissa ^a   Schuetz, John D ^b   Fang, Che ^a   Watkins, Paul B ^a  

^a UNIVERSITY OF MICHIGAN HEALTH SYSTEM   (United States)

^b VIRGINIA COMMONWEALTH UNIVERSITY   (United States)

Author keywords

Cyclosporine A; Cytochrome P450; Enterocyte; Gastrointestinal tract; Immunohistochemistry; P450IIIA

Indexed keywords

COMPLEMENTARY DNA; CYTOCHROME P450 ISOENZYME; DNA FRAGMENT; ERYTHROMYCIN; FATTY ACID BINDING PROTEIN; MESSENGER RNA; OLIGO 1,6 GLUCOSIDASE; RIFAMPICIN; SUCRASE; XENOBIOTIC AGENT;

ADULT; ARTICLE; CONTROLLED STUDY; DEMETHYLATION; DNA SEQUENCE; DRUG METABOLISM; ENZYME ANALYSIS; GENE AMPLIFICATION; HUMAN; HUMAN CELL; HUMAN TISSUE; IMMUNOHISTOCHEMISTRY; IMMUNOREACTIVITY; INTESTINE BIOPSY; INTESTINE CELL; POLYMERASE CHAIN REACTION; PRIORITY JOURNAL; SMALL INTESTINE;

ADULT; BASE SEQUENCE; CYCLOSPORINE; CYTOCHROME P-450 ENZYME SYSTEM; ENZYME INDUCTION; FEMALE; HUMAN; INTESTINE, SMALL; MALE; MOLECULAR SEQUENCE DATA; RIFAMPIN; RNA, MESSENGER; SUPPORT, U.S. GOV'T, NON-P.H.S.; SUPPORT, U.S. GOV'T, P.H.S.;

EID: 0026464616     PISSN: 00219738     EISSN: None     Source Type: Journal    
DOI: 10.1172/JCI116064     Document Type: Article

References (45)

1. Watkins, P. B., S. A. Wrighton, P. Maurel, E. G. Schuetz., G. Mendez-Picon, G. A. Parker, and P. S. Guzelian. 1985. Identification of an inducible form of eylochrome P-450 in human liver. Proc. Natl. Acad Sci. USA. 82:6310-6314.
2. Shimada, T., and F. P. Guengerich. 1989. Evidence for cytochrome P-450NF, the nifedipine oxidase, being the principal enzyme involved in the bioactivation of aflatoxins in human liver. Proc. Natl. Acad. Sci. USA. 86:462-465.
3. Kronbach, T., V. Fischer, and U. A. Meyer. 1988. Cyclosporine metabolism in human liver: identification of a cytochrome P-450III gene family as the major cyclosporine-metabolizing enzyme explains interactions of cyclosporine with other drugs. Clin. Pharmacol. Ther. 43:630-635.
4. Combalbert, J., I. Fabre, G. Fabre, I. Dalet, J. Derancourt, J. P. Cano, and P. Maurel. 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 Metab. Dispos. 17:197-207.
5. Gonzalez, F. J., B. J. Schmid, M. Umeno, O. W. McBride, J. P. Hardwick, U. A. Meyer, H. V. Gelboin, and J. R. Idle. 1988. Human P450PCN1: sequence, chromosome localization, and evidence through cDNA expression that P450PCN1 is nifedipine oxidase. DNA (NY). 7:79-86.
6. Guengerich, F. P., M. V. Martin, P. H. Beaune, P. Kremers, T. Wolff, and D. J. Waxman. 1986. Characterization of rat and human liver microsomal cytochrome P-450 forms involved in nifedipine oxidation, a prototype for genetic polymorphism in oxidative drug metabolism. J. Biol. Chem. 261:5051-5060.
7. Bargetzi, M. J., T. Aoyama, F. J. Gonzalez, and U. A. Meyer. 1989. Lidocaine metabolism in human liver microsomes by cytochrome P450IIIA4. Clin. Pharmacol. Ther. 46:521-527.
8. Guengerich, F. P., D. Meuller-Enoch, and I. A. Blair. 1986. Oxidation of quinidine by human liver cytochrome P-450. Mol. Pharmacol. 30:287-295.
9. Kronbach, T., D. Mathys, M. Umeno, F. J. Gonzalez, and U. A. Meyer. 1989. Oxidation of midazolam and triazolam by human liver cytochrome P450IIIA4. Mol. Pharmacol. 36:89-96.
10. Regina, R. W., P. H. Kari, A. Y. H. Lu, P. E. Thomas, F. P. Guengerich, and K. P. Vyas. 1991. Biotransformation of Lovastatin. Arch. Biochem. Biophys. 290:355-361.
11. Jacolot, F., I. Simon, Y. Dreano, P. Beaune, C. Riche, and F. Berthou. 1991. Identification of the cytochrome P450IIIA family as the enzymes involved in the N-demethylation of tamoxifen in human liver microsomes. Biochem. Pharmacol. 41:1911-1919.
12. Nebert, D. W., D. R. Nelson, M. J. Coon, R. W. Estabrook, R. Feyereisen, Y. Fujii-Kuriyama, F. J. Gonzalez, F. P. Guengerich, I. C. Gunsalus, E. F. Johnson, et al. 1991. The P450 superfamily: Update on new sequences, gene mapping, and recommended nomenclature. DNA Cell Biol. 10:1-14.
13. Molowa, D. T., E. G. Schuetz, S. A. Wrighton, P. B. Watkins, P. Kremers, G. Mendez-Picon, G. A. Parker, and P. S. Guzelian. 1986. Complete cDNA sequence of a cytochrome P-450 inducible by glucocorticoids in human liver. Proc. Natl. Acad. Sci. USA. 83:5311-5315.
14. Aoyama, T., S. Yamano, D. J. Waxman, D. P. Lapenson, U. A. Meyer, V. Fischer, R. Tyndale, T. Inaba, W. Kalow, H. V. Gelboin, F. J. Gonzalez. 1989. Cytochrome P-450 hPCN3, a novel cytochrome P-450IIIA gene product that is differentially expressed in adull 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.
15. Wrighton, S. A., W. R. Brian, M. A. Sari, M. Iwasaki, F. P. Guengerich, J. L. Raucy, D. T. Molowa, and M. Vandenbranden. 1990. Studies on the expression and metabolic capabilities of human liver cytochrome P450IIIA5 (HLp3). Mol. Pharmacol. 38:207-213.
16. Bork, R. W., T. Muto, P. H. Beaune, P. K. Srivastava, R. S. Lloyd, and F. P. Guengerich. 1989. Characterization of mRNA species related to human liver cytochrome P-450 nifedipine oxidase and the regulation of catalytic activity. J. Biol. Chem. 264:910-919.
17. Guengerich, F. P. 1989. Characterization of human microsomal cytochrome P-450 enzymes. Annu. Rev. Pharmacol. Toxicol. 29:241-264.
18. Watkins, P. B. 1990. Role of cytochromes P450 in drug metabolism and hepatotoxicity. Semin. Liver Dis. 10:235-250.
19. Watkins, P. B., S. A. Murray, L. G. Winkelman, D. M. Heuman, S. A. Wrighton, and P. S. Guzelian. 1989. Erythromycin breath test as an assay of glucocorticoid-inducible liver cytochromes P-450. J. Clin. Invest. 83:688-697.
20. Pichard, P., I. Fabre, G. Fabre, J. Domergue, B. Saint Aubert, G. Mourad, and P. Maurel. 1990. Cyclosporin A drug interactions: screening for inducers and inhibitors of cytochrome P450 (Cyclosporin A Oxidase) in primary cultures of human hepatocytes. Drug Metab. Dispos. 18:595-606.
21. Ged, C., J. M. Rouillon, L. Pichard, J. Combalbert, N. Bressot, P. Bories, H. Michel, P. Beaune, and P. Maurel. 1989. The increase in urinary excretion of 6β-hydroxycortisol as a marker of human hepatic cytochrome P450IIIA induction. Br J. Clin. Pharmacol. 28:373-387.
22. Wrighton, S. A., B. J. Ring, P. B. Watkins, and M. Vandenbranden. 1989. Identification of a polymorphically expressed member of the human cytochrome P-450III family. Mol. Pharmacol 36:97-105.
23. Gupta. S. K., A. Bakran, R. W. Johnson, and M. Rowland. 1989. Cyclosporin-erythromycin interaction in renal transplant patients. Br. J. Clin. Pharmacol. 27:475-481.
24. First, M. R., T. J. Schroeder, P. Weiskittel, S. A. Myre, J. W. Alexander, and A. J. Pesce. 1989. Combinant administration of cyclosporin and ketoconazole in renal transplant recipients. Lancet. ii:1198-1201.
25. Daniels, N. J., J. S. Dover, and R. K. Schachter. 1984. Interaction between cyclosporin and rifampicin. Lancet. ii:639.
26. Watkins, P. B., T. A. Hamilton, T. M. Annesley, C. N. Ellis, J. C. Kotars, and J. J. Voorhees. 1990. The erythromycin breath test as a predictor of cyclosporine A blood levels, Clin. Pharmacol. & Ther. 48:120-129.
27. Kolars, J. C., W. M. Awni, R. M. Merion, and P. B. Watkins. 1991. First-pass metabolism of cyclosporin by the gut. Lancet. 338:1488-1490.
28. Kolars, J. C., P. L. Stetson, B. D. Rush, M. J. Ruwart, P. Schmiedlin-Ren, E. A. Duell, J. J. Voorhees, and P. B. Watkins. 1992. Cyclosporin metabolism by P450IIIA in rat enterocytes - another determinant of oral bioavailability? Transplantation (Baltimore). 53:596-602.
29. Watkins, P. B., S. A. Wrighton, E. G. Schuetz, D. T. Molowa, and P. S. Guzelian. 1987. Identification of glucocorticoid-inducible cytochromes P-450 in the intestinal mucosa of rats and man. J. Clin. Invest. 80:1029-1036.
30. Chomczynski, P., and N. Sacchi. 1987. Single-step method of RNA isolation by acid guanidinium thiocyanate-phenol-chloroform extraction. Anal. Biochem. 162:156-159.
31. Traber, P. G., L. Yu, G. D. Wu, and T. A. Judge. 1992. Sucrase-isomaltase gene expression along crypt-villus axis of human small intestine is regulated at level of mRNA abundance. Am. J. Physiol. 262:G123-G130.
32. Komori, M., K. Nishio, H. Ohi, M. Kitada, and T. Kamataki. 1989. Molecular cloning and sequence analysis of cDNA containing the entire coding region for human fetal liver cytochrome P-450. J. Biochem. (Tokyo). 105:161-163.
33. Sweetser, D. A., E. H. Birkenmeier, I. J. Klisak, S. Zollman, R. S. Sparkes, T. Mohandas, A. J. Lusis, and J. I. Gordon. 1987. The human and rodent intestinal fatty acid binding protein genes. J. Biol. Chem. 262:16060-16071.
34. Sanger, F., S. Nicklen, and A. R. Coulson. 1977. DNA sequencing with chain-terminating inhibitors. Proc. Natl. Acad. Sci. USA. 74:5463-5467.
35. Dahlqvist, A. 1984. Assay of intestinal disaccharidases. Scand. J. Clin Lab. Invest. 44:169-172.
36. Nash, T. 1953. The colorimetric estimation of formaldehyde by means of the Hantzsch reaction. Biochem. J. 55:416-421.
37. Wrighton, S. A., P. Maurel, E. G. Schuetz, P. B. Watkins, B. Young, and P. S. Guzelian. 1985. Identification of the cytochrome P-450 induced by macrolide antibiotics in rat liver as the glucocorticoid responsive cytochrome P-450p. Biochemistry. 24:2171-2178.
38. Poland, A. P., and D. W. Nebert. 1973. A sensitive radiometric assay of aminopyrine N-demethylation. J. Pharmacol. Exp. Ther. 184:269-277.
39. Beaune, P. H., D. R. Umbenhauer, R. W. Bork, R. S. Lloyd, and F. P. Guengerich. 1986. Isolation and sequence determination of a cDNA clone related to human cytochrome P-450 nifedipine oxidase. Proc. Natl. Acad. Sci. USA. 83:8064-8068.
40. Schuetz, J. D., D. T. Molowa, and P. S. Guzelian. 1989. Characterization of a cDNA encoding a new member of the glucocorticoid-responsive cytochromes P450 in human liver. Arch. Biochem. Biophys. 274:355-365.
41. Komori, M., K. Nishio, M. Kitada, K. Shiramatsu, K. Muroya, M. Soma, K. Nagashima, and T. Kamataki. 1990. Fetus-specific expression of a form of cytochrome P-450 in human livers. Biochemistry. 29:4430-4433.
42. Murray, G. I., T. S. Barnes, H. F. Sewell, S. W. Ewen, W. T. Melvin, and M. D. Burke. 1988. The immunocytochemical localisation and distribution of cytochrome P-450 in normal human hepatic and extrahepatic tissues with a monoclonal antibody to human cytochrome P-450. Br J. Clin. Pharmacol. 25:465-475.
43. Ptachcinski, R. J., R. Venkatatramanan, and G. J. Burckhart. 1986. Clinical pharmacokinetics of cyclosporin. Clin. Pharmacokinet. 11:107-132.
44. Lucey, M. R., J. C. Kolars, R. M. Merion, D. A. Campbell, M. Aldrich, and P. B. Watkins. 1990. Cyclosporin toxicity at therapeutic blood levels and cytochrome P-450IIIA, Lancet. 335:11-15.
45. Kolars, J. C., P. Schmiedlin-Ren, J. Schuetz, W. O. Dobbins, S. A. Wrighton, and P. B. Watkins. 1992. Heterogeneity of cytochrome P-450 III expression in rat gut epithelia. Gastroenterology. 102:1186-1198.