Mechanism of rifampicin and pregnane X receptor inhibition of human cholesterol 7α-hydroxylase gene transcription

American Journal of Physiology - Gastrointestinal and Liver Physiology

Volumn 288, Issue 1 51-1, 2005, Pages

  Li, Tiangang ^a   Chiang, John Y L ^a  

^a NORTHEAST OHIO MEDICAL UNIVERSITY   (United States)

Author keywords

Bile acid synthesis; Gene regulation; Nuclear receptors; Peroxisome proliferator activated receptor coactivator

Indexed keywords

BILE ACID; CELL NUCLEUS RECEPTOR; CHOLESTEROL 7ALPHA MONOOXYGENASE; DNA BINDING PROTEIN; MESSENGER RNA; PREGNANE X RECEPTOR; PROTEIN HEPATIC NUCLEAR FACTOR 4 ALPHA; PROTEIN PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA COACTIVATOR; PROTEIN SHORT HETERODIMER PARTNER; RECEPTOR; RIFAMPICIN; UNCLASSIFIED DRUG;

ADULT; AGED; ARTICLE; BILE ACID SYNTHESIS; BINDING SITE; CHOLESTASIS; CHROMATIN; DNA RESPONSIVE ELEMENT; DRUG RECEPTOR BINDING; FEMALE; GENETIC TRANSCRIPTION; HEPATOBLASTOMA; HUMAN; HUMAN CELL; IMMUNOPRECIPITATION; LIVER CELL; MALE; PRESCHOOL CHILD; PRIORITY JOURNAL; PROTEIN DNA BINDING; PROTEIN DNA INTERACTION; PROTEIN EXPRESSION; PROTEIN PROTEIN INTERACTION; REAL TIME POLYMERASE CHAIN REACTION; TRANSCRIPTION REGULATION;

BILE ACIDS AND SALTS; CHOLESTASIS; CHOLESTEROL 7-ALPHA-HYDROXYLASE; DNA-BINDING PROTEINS; ENZYME INHIBITORS; HEPATOBLASTOMA; HEPATOCYTE NUCLEAR FACTOR 4; HUMANS; LIVER NEOPLASMS; PHOSPHOPROTEINS; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, GLUCOCORTICOID; RECEPTORS, STEROID; RIFAMPIN; RNA, MESSENGER; TRANSCRIPTION FACTORS; TRANSCRIPTION, GENETIC; TUMOR CELLS, CULTURED; UP-REGULATION;

EID: 10844273426     PISSN: 01931857     EISSN: None     Source Type: Journal    
DOI: 10.1152/ajpgi.00258.2004     Document Type: Article

References (34)

1. Bachs L, Pares A, Elena M, Piera C, and Rodes J. Comparison of rifampicin with phenobarbitone for treatment of pruritus in biliary cirrhosis. Lancet 1: 574-576, 1989.
2. Chen W, Owsley E, Yang Y, Stroup D, and Chiang JY. Nuclear receptor-mediated repression of human cholesterol 7α-hydroxylase gene transcription by bile acids. J Lipid Res 42: 1402-1412, 2001.
3. Chiang JY. Bile Acid regulation of gene expression: roles of nuclear hormone receptors. Endocr Rev 23: 443-463, 2002.
4. Chiang JY. Regulation of bile acid synthesis: pathways, nuclear receptors, and mechanisms. J Hepatol 40: 539-551, 2004.
5. Chiang JY, Kimmel R, and Stroup D. Regulation of cholesterol 7α-hydroxylase gene (CYP7A1) transcription by the liver orphan receptor (LXRα). Gene 262: 257-265, 2001.
6. Chiang JYL, Miller WF, and Lin GM. Regulation of cholesterol 7α-hydroxylase in the liver:Purification of cholesterol 7α-hydroxylase and the immunochemical evidence for the induction of cholesterol 7α-hydroxylase by cholestyramine and circadian rhythm. J Biol Chem 265: 3889-3897, 1990.
7. Cohen RN, Putney A, Wondisford FE, and Hollenberg AN. The nuclear corepressors recognize distinct nuclear receptor complexes. Mol Endocrinol 14: 900-914, 2000.
8. Crestani M, Sadeghpour A, Stroup D, Gali G, and Chiang JYL. Transcriptional activation of the cholesterol 7α-hydroxylase gene (CYP7A) by nuclear hormone receptors. J Lipid Res 39: 2192-2200, 1998.
9. Drocourt L, Ourlin JC, Pascussi JM, Maurel P, and Vilarem MJ. Expression of CYP3A4, CYP2B6 and CYP2C9 is regulated by the vitamin D receptor pathway in primary human hepatocytes. J Biol Chem 277: 25125-25132, 2002.
10. Glass CK, Rose DW, and Rosenfeld MG. Nuclear receptor coactivators. Curr Opin Cell Biol 9: 222-232, 1997.
11. Handschin C and Meyer UA. Induction of drug metabolism: the role of nuclear receptors. Pharmacol Rev 55: 649-673, 2003.
12. Hofmann AF. Rifampicin and treatment of cholestatic pruritus. Gut 51: 756-757, 2002.
13. Ishizuka T and Lazar MA. The N-CoR/histone deacetylase 3 complex is required for repression by thyroid hormone receptor. Mol Cell Biol 23: 5122-5131, 2003.
14. Kamiya A, Inoue Y, and Gonzalez FJ. Role of the hepatocyte nuclear factor 4á in control of the pregnane X receptor during fetal liver development. Hepatology 37: 1375-1384, 2003.
15. Kerr TA, Saeki S, Schneider M, Schaefer K, Berdy S, Redder T, Shan B, Russell DW, and Schwarz M. Loss of nuclear receptor SHP impairs but does not eliminate negative feedback regulation of bile acid synthesis. Dev Cell 2: 713-720, 2002.
16. Kim S and Kim T. Selection of optimal internal controls for gene expression profiling of liver disease. Biotechniques 35: 456-458, 460, 2003.
17. Kliewer SA, Goodwin B, and Willson TM. The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism. Endocr Rev 23: 687-702, 2002.
18. Kliewer SA and Willson TM. Regulation of xenobiotic and bile acid metabolism by the nuclear pregnane X receptor. J Lipid Res 43: 359-364, 2002.
19. Lehmann JM, McKee DD, Watson MA, Willson TM, Moore JT, and Kliewer SA. 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, 1998.
20. Li YC, Wang DP, and Chiang JYL. Regulation of cholesterol 7α-hydroxylase in the liver: cDNA cloning, sequencing and regulation of cholesterol 7α-hydroxylase mRNA. J Biol Chem 265: 12012-12019, 1990.
21. Menke JG, Macnaul KL, Hayes NS, Baffic J, Chao YS, Elbrecht A, Kelly LJ, Lam MH, Schmidt A, Sahoo S, Wang J, Wright SD, Xin P, Zhou G, Moller DE, and Sparrow CP. A novel liver X receptor agonist establishes species differences in the regulation of cholesterol 7α-hydroxylase (CYP7a). Endocrinology 143: 2548-2558., 2002.
22. Ourlin JC, Lasserre F, Pineau T, Fahre JM, Sa-Cunha A, Maurel P, Vilarem MJ, and Pascussi JM. The small heterodimer partner interacts with the pregnane X receptor and represses its transcriptional activity. Mol Endocrinol 17: 1693-1703, 2003.
23. Puigserver P and Spiegelman BM. Peroxisome proliferator-activated receptor-gamma coactivator 1α (PGC-1α): transcriptional coactivator and metabolic regulator. Endocr Rev 24: 78-90, 2003.
24. Qin J, Gao DM, Jiang QF, Zhou Q, Kong YY, Wang Y, and Xie YH. Prox1 is a corepressor of human liver receptor homologue-1 and suppresses the transcription of the cholesterol 7α-hydroxylase gene. Mol Endocrinol 18: 2424-2439, 2004.
25. Schreiber SN, Knutti D, Brogli K, Uhlmann T, and Kralli A. The transcriptional coactivator PGC-1 regulates the expression and activity of the orphan nuclear receptor estrogen-related receptor α (ERRα). J Biol Chem 278: 9013-9018, 2003.
26. Sinai CJ, Tohkin M, Miyata M, Ward JM, Lambert G, and Gonzalez FJ. Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis. Cell 102: 731-744, 2000.
27. 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, and Kliewer SA. The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proc Natl Acad Sci. USA 98: 3369-3374, 2001.
28. Steffensen KR, Holter E, Bavner A, Nilsson M, Pelto-Huikko M, Tomarev S, and Treuter E. Functional conservation of interactions between a homeodomain cofactor and a mammalian FTZ-F1 homologue. EMBO Rep 5: 613-619, 2004.
29. Stroup D and Chiang JYL. HNF4 and COUP-TFII interact to modulate transcription of the cholesterol 7α-hydroxylase gene (CYP7A). J Lipid Res 41: 1-11, 2000.
30. Takeshita A, Taguchi M, Koibuchi N, and Ozawa Y. Putative role of the orphan nuclear receptor SXR (steroid and xenobiotic receptor) in the mechanism of CYP3A4 inhibition by xenobiotics. J Biol Chem 277: 32453-32458, 2002.
31. Tirona RG, Lee W, Leake BF, Lan LB, Cline CB, Lamba V, Parviz F, Duncan SA, Inoue Y, Gonzalez FJ, Schuetz EG, and Kim RB. The orphan nuclear receptor HNF4α determines PXR- and CAR-mediated xenobiotic induction of CYP3A4. Nat Med 9: 220-224, 2003.
32. Wang DP, Stroup D, Marrapodi M, Crestani M, Galli G, and Chiang JYL. Transcriptional regulation of the human cholesterol 7α-hydroxylase gene (CYP7A) in HepG2 cells. J Lipid Res 37: 1831-1841, 1996.
33. Wang L, Lee YK, Bundman D, Han Y, Thevananther S, Kim CS, Chua SS, Wei P, Heyman RA, Karin M, and Moore DD. Redundant pathways for negative feedback regulation of bile Acid production. Dev Cell 2: 721-731, 2002.
34. Xie W, Radominska-Pandya A, Shi Y, Simon CM, Nelson MC, Ong ES, Waxman DJ, and Evans RM. An essential role for nuclear receptors SXR/PXR in detoxification of cholestatic bile acids. Proc Natl Acad Sci USA 98: 3375-3380, 2001.