Rifampicin induction of CYP3A4 requires pregnane X receptor cross talk with hepatocyte nuclear factor 4α and coactivators, and suppression of small heterodimer partner gene expression

Drug Metabolism and Disposition

Volumn 34, Issue 5, 2006, Pages 756-764

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

^a NORTHEAST OHIO MEDICAL UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BILE ACID; CYTOCHROME P450 3A4; HEPATOCYTE NUCLEAR FACTOR 4ALPHA; MESSENGER RNA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA; PREGNANE X RECEPTOR; RIFAMPICIN; STEROID RECEPTOR COACTIVATOR 1; XENOBIOTIC AGENT;

ADULT; ARTICLE; BINDING SITE; CHOLESTASIS; CHROMATIN; CONCENTRATION RESPONSE; ENZYME INDUCTION; FEMALE; GENE ACTIVITY; GENE EXPRESSION REGULATION; GENE MUTATION; GENETIC TRANSCRIPTION; HUMAN; HUMAN CELL; IMMUNOPRECIPITATION; LIVER CELL; LIVER DISEASE; MALE; MOLECULAR INTERACTION; PRIORITY JOURNAL; PROMOTER REGION; PROTEIN EXPRESSION; PROTEIN PROTEIN INTERACTION; TRANSCRIPTION REGULATION;

ANTIBIOTICS, ANTITUBERCULAR; BLOTTING, WESTERN; CELL LINE, TUMOR; CHROMATIN; CYTOCHROME P-450 ENZYME SYSTEM; ELECTROPHORETIC MOBILITY SHIFT ASSAY; ENZYME INDUCTION; GLUTATHIONE TRANSFERASE; HEPATOCYTE NUCLEAR FACTOR 4; HEPATOCYTES; HUMANS; IMMUNOPRECIPITATION; PLASMIDS; RECEPTOR CROSS-TALK; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, STEROID; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION; RIFAMPIN; RNA, MESSENGER; TRANSFECTION;

EID: 33645808917     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.105.007575     Document Type: Article

References (32)

1. Bachs L, Pares A, Elena M, Piera C, and Rodes J (1989) Comparison of rifampicin with phenobarbitone for treatment of pruritus in biliary cirrhosis. Lancet 1:574-576.
2. Bertilsson G, Heidrich J, Svensson K, Asman M, Jendeberg L, Sydow-Backman M, Ohlsson R, Postlind H, Blomquist P, and 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.
3. Bhalla S, Ozalp C, Fang S, Xiang L, and Kemper JK (2004) Ligand-activated PXR interferes with HNF-4 signaling by targeting a common coactivator PGC-1α: functional implications in hepatic cholesterol and glucose metabolism. J Biol Chem 279:45139-45147.
4. Boyer JL (2005) Nuclear receptor ligands: rational and effective therapy for chronic cholestatic liver disease? Gastroenterology 129:735-740.
5. Chen Y, Kissling G, Negishi M, and Goldstein JA (2005) The nuclear receptors constitutive androstane receptor and pregnane X receptor cross-talk with hepatic nuclear factor 4α to synergistically activate the human CYP2C9 promoter. J Pharmacol Exp Ther 314:1125-1133.
6. De Fabiani E, Mitro N, Gilardi F, Caruso D, Galli G, and Crestani M (2003) Coordinated control of cholesterol catabolism to bile acids and of gluconeogenesis via a novel mechanism of transcription regulation linked to the fasted-to-fed cycle. J Biol Chem 278:39124-39132.
7. Drocourt L, Ourlin JC, Pascussi JM, Maurel P, and Vilarem MJ (2002) Expression of CYP3A4, CYP2B6 and CYP2C9 is regulated by the vitamin D receptor pathway in primary human hepatocytes. J Biol Chem 277:25125-25132.
8. Ferguson SS, Chen Y, LeCluyse EL, Negishi M, and Goldstein JA (2005) Human CYP2C8 is transcriptionally regulated by the nuclear receptors constitutive androstane receptor, pregnane X receptor, glucocorticoid receptor and hepatic nuclear factor 4alpha. Mol Pharmacol 68: 747-757.
9. Gnerre C, Blattler S, Kaufmann MR, Looser R, and Meyer UA (2004) Regulation of CYP3A4 by the bile acid receptor FXR: evidence for functional binding sites in the CYP3A4 gene. Pharmacogenetics 14:635-645.
10. Goodwin B, Hodgson E, and 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.
11. Goodwin B, Jones SA, Price RR, Watson MA, McKee DD, Moore LB, Galardi C, Wilson JG, Lewis MC, Roth ME, et al. (2000) A regulatory cascade of the nuclear receptors FXR, SHP-1 and LRH-1 represses bile acid biosynthesis. Mol Cell 6:517-526.
12. Goodwin B, Redinbo MR, and Kliewer SA (2002) Regulation of CYP3A gene transcription by the pregnane X receptor. Annu Rev Pharmacol Toxicol 42:1-23.
13. Guengerich FP (1999) Cytochrome P-450 3A4: regulation and role in drug metabolism. Annu Rev Pharmacol Toxicol 39:1-17.
14. Hayhurst GP, Lee YH, Lambert G, Ward JM, and Gonzalez FJ (2001) Hepatocyte nuclear factor 4α (nuclear receptor 2A1) is essential for maintenance of hepatic gene expression and lipid homeostasis. Mol Cell Biol 21:1393-1403.
15. Hofmann AF (2002) Rifampicin and treatment of cholestatic pruritus. Gut 51:756-757.
16. Jahan A and Chiang JY (2005) Cytokine regulation of human sterol 12α-hydroxylase (CYP8B1) gene. Am J Physiol 288:G685-G695.
17. Jung D and Kullak-Ublick GA (2003) Hepatocyte nuclear factor 1 alpha: a key mediator of the effect of bile acids on gene expression. Hepatology 37:622-631.
18. Kamiya A, Inoue Y, and Gonzalez FJ (2003) Role of the hepatocyte nuclear factor 4α in control of the pregnane X receptor during fetal liver development. Hepatology 37:1375-1384.
19. Kliewer SA, Goodwin B, and Willson TM (2002) The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism. Endocr Rev 23:687-702.
20. Kliewer SA, Moore JT, Wade L, Staudinger JL, Watson MA, Jones SA, McKee DD, Oliver BB, Willson TM, Zetterstrom RH, et al. (1998) An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway. Cell 92:73-82.
21. Lehmann JM, McKee DD, Watson MA, Willson TM, Moore JT, and Kliewer SA (1998) The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. J Clin Investig 102:1016-1023.
22. Li T and Chiang JY (2004) Mechanism of rifampicin and pregnane X receptor inhibition of human cholesterol 7alpha-hydroxylase gene transcription. Am J Physiol 288:G74-G84.
23. Lu TT, Makishima M, Repa JJ, Schoonjans K, Kerr TA, Auwerx J, and Mangelsdorf DJ (2000) Molecular basis for feedback regulation of bile acid synthesis by nuclear receptors. Mol Cell 6:507-515.
24. Marschall HU, Wagner M, Zollner G, Fickert P, Diczfalusy U, Gumhold J, Silbert D, Fuchsbichler A, Benthin L, Grundstrom R, et al. (2005) Complementary stimulation of hepatobiliary transport and detoxification systems by rifampicin and ursodeoxycholic acid in humans. Gastroenterology 129:476-485.
25. Ourlin JC, Lasserre F, Pineau T, Fabre JM, Sa-Cunha A, Maurel P, Vilarem MJ, and Pascussi JM (2003) The small heterodimer partner interacts with the pregnane X receptor and represses its transcriptional activity. Mol Endocrinol 17:1693-1703.
26. Puigserver P, Rhee J, Donovan J, Walkey CJ, Yoon JC, Oriente F, Kitamura Y, Altomonte J, Dong H, Accili D, et al. (2003) Insulin-regulated hepatic gluconeogenesis through FOXO1-PGC-1α interaction. Nature (Lond) 423:550-555.
27. Schuetz EG, Strom S, Yasuda K, Lecureur V, Assem M, Brimer C, Lamba J, Kim RB, Ramachandran V, Komoroski BJ, et al. (2001) Disrupted bile acid homeostasis reveals an unexpected interaction among nuclear hormone receptors, transporters and cytochrome P450. J Biol Chem 276:39411-39418.
28. Shin DJ, Campos JA, Gil G, and Osborne TF (2003) PGC-1α activates CYP7A1 and bile acid biosynthesis. J Biol Chem 278:50047-50052.
29. Staudinger JL, Goodwin B, Jones SA, Hawkins-Brown D, MacKenzie KI, LaTour A, Liu Y, Klaassen CD, Brown KK, Reinhard J, et al. (2001) The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proc Natl Acad Sci USA 98:3369-3374.
30. Stroup D and Chiang JY (2000) HNF4 and COUP-TFII interact to modulate transcription of the cholesterol 7α-hydroxylase gene (CYP7A1). J Lipid Res 41:1-11.
31. Tirona RG, Lee W, Leake BF, Lan LB, Cline CB, Lamba V, Parviz F, Duncan SA, Inoue Y, Gonzalez FJ, et al. (2003) The orphan nuclear receptor HNF4α determines PXR- and CAR-mediated xenobiotic induction of CYP3A4. Nat Med 9:220-224.
32. Xie W, Radominska-Pandya A, Shi Y, Simon CM, Nelson MC, Ong ES, Waxman DJ, and 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.