Regulation of the human bile acid UDP-glucuronosyltransferase 1A3 by the farnesoid X receptor and bile acids

Journal of Hepatology

Volumn 52, Issue 4, 2010, Pages 570-578

  Erichsen, Thomas J ^a   Aehlen, André ^a   Ehmer, Ursula ^a   Kalthoff, Sandra ^a   Manns, Michael P ^a   Strassburg, Christian P ^a  

^a HANNOVER MEDICAL SCHOOL   (Germany)

Author keywords

Bile acid regulation; Cholestasis; Farnesoid X receptor; Glucuronidation; Nuclear receptor; UGT1A3; Xenobiotic metabolism

Indexed keywords

BILE ACID; CHENODEOXYCHOLIC ACID; FARNESOID X RECEPTOR; GENOMIC DNA; GLUCURONOSYLTRANSFERASE 1A3; GLUCURONOSYLTRANSFERASE 1A4; URSODEOXYCHOLIC ACID;

ARTICLE; BILE ACID BLOOD LEVEL; BLOOD SAMPLING; CASE REPORT; CHOLESTASIS; GEL MOBILITY SHIFT ASSAY; GENE TARGETING; GENETIC VARIABILITY; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; PRIORITY JOURNAL; PROTEIN EXPRESSION; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; SITE DIRECTED MUTAGENESIS; TRANSCRIPTION REGULATION;

BILE ACIDS AND SALTS; CHENODEOXYCHOLIC ACID; CHOLESTASIS; GENE EXPRESSION; GENES, REPORTER; GENETIC VARIATION; GLUCURONOSYLTRANSFERASE; HEP G2 CELLS; HUMANS; LITHOCHOLIC ACID; LUCIFERASES; MUTAGENESIS, SITE-DIRECTED; PROMOTER REGIONS, GENETIC; RECEPTORS, CYTOPLASMIC AND NUCLEAR; TRANSCRIPTIONAL ACTIVATION; URSODEOXYCHOLIC ACID; XENOBIOTICS;

EID: 77949654677     PISSN: 01688278     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jhep.2010.01.010     Document Type: Article

References (39)

1. Takikawa H., Otsuka H., Beppu T., Seyama Y., and Yamakawa T. Serum concentrations of bile acid glucuronides in hepatobiliary diseases. Digestion 27 (1983) 189-195
2. Marschall H.U., Matern H., Wietholtz H., Egestad B., Matern S., and Sjovall J. Bile acid N-acetylglucosaminidation. In vivo and in vitro evidence for a selective conjugation reaction of 7 beta-hydroxylated bile acids in humans. J Clin Invest 89 (1992) 1981-1987
3. Russell D.W. The enzymes, regulation, and genetics of bile acid synthesis. Annu Rev Biochem 72 (2003) 137-174
4. Kullak-Ublick G.A., Beuers U., and Paumgartner G. Hepatobiliary transport. J Hepatol 32 (2000) 3-18
5. Lee F.Y., Lee H., Hubbert M.L., Edwards P.A., and Zhang Y. FXR, a multipurpose nuclear receptor. Trends Biochem Sci 31 (2006) 572-580
6. Parks D.J., Blanchard S.G., Bledsoe R.K., Chandra G., Consler T.G., Kliewer S.A., et al. Bile acids: natural ligands for an orphan nuclear receptor. Science 284 (1999) 1365-1368
7. Wang H., Chen J., Hollister K., Sowers L.C., and Forman B.M. Endogenous bile acids are ligands for the nuclear receptor FXR/BAR. Mol Cell 3 (1999) 543-553
8. Wang S., Lai K., Moy F.J., Bhat A., Hartman H.B., and Evans M.J. The nuclear hormone receptor farnesoid X receptor (FXR) is activated by androsterone. Endocrinology 147 (2006) 4025-4033
9. Watanabe M., Houten S.M., Mataki C., Christoffolete M.A., Kim B.W., Sato H., et al. Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation. Nature 439 (2006) 484-489
10. Downes M., Verdecia M.A., Roecker A.J., Hughes R., Hogenesch J.B., Kast-Woelbern H.R., et al. A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. Mol Cell 11 (2003) 1079-1092
11. Maloney P.R., Parks D.J., Haffner C.D., Fivush A.M., Chandra G., Plunket K.D., et al. Identification of a chemical tool for the orphan nuclear receptor FXR. J Med Chem 43 (2000) 2971-2974
12. Pellicciari R., Fiorucci S., Camaioni E., Clerici C., Costantino G., Maloney P.R., et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J Med Chem 45 (2002) 3569-3572
13. Dussault I., Beard R., Lin M., Hollister K., Chen J., Xiao J.H., et al. Identification of gene-selective modulators of the bile acid receptor FXR. J Biol Chem 278 (2003) 7027-7033
14. Matern H., Matern S., Schelzig C., and Gerok W. Bile acid UDP-glucoronyltransferase from human liver. Properties and studies on aglycone substrate specificity. FEBS Lett 118 (1980) 251-254
15. Parquet M., Pessah M., Sacquet E., Salvat C., Raizman A., and Infante R. Glucuronidation of bile acids in human liver, intestine and kidney. An in vitro study on hyodeoxycholic acid. FEBS Lett 189 (1985) 183-187
16. Trottier J., Verreault M., Grepper S., Monte D., Belanger J., Kaeding J., et al. Human UDP-glucuronosyltransferase (UGT)1A3 enzyme conjugates chenodeoxycholic acid in the liver. Hepatology 44 (2006) 1158-1170
17. Barbier O., Torra I.P., Sirvent A., Claudel T., Blanquart C., Duran-Sandoval D., et al. FXR induces the UGT2B4 enzyme in hepatocytes: a potential mechanism of negative feedback control of FXR activity. Gastroenterology 124 (2003) 1926-1940
18. Belanger A., Pelletier G., Labrie F., Barbier O., and Chouinard S. Inactivation of androgens by UDP-glucuronosyltransferase enzymes in humans. Trends Endocrinol Metab 14 (2003) 473-479
19. Kauffman F.C. Sulfonation in pharmacology and toxicology. Drug Metab Rev 36 (2004) 823-843
20. Podesta M.R., Murphy G.M., and Dowling R.H. Measurement of faecal bile acid sulphates. J Chromatogr 182 (1980) 293-300
21. Pillot T., Ouzzine M., Fournel-Gigleux S., Lafaurie C., Radominska A., Burchell B., et al. Glucuronidation of hyodeoxycholic acid in human liver. Evidence for a selective role of UDP-glucuronosyltransferase 2B4. J Biol Chem 268 (1993) 25636-25642
22. Gall W.E., Zawada G., Mojarrabi B., Tephly T.R., Green M.D., Coffman B.L., et al. Differential glucuronidation of bile acids, androgens and estrogens by human UGT1A3 and 2B7. J Steroid Biochem Mol Biol 70 (1999) 101-108
23. Strassburg C.P., Lankisch T.O., Manns M.P., and Ehmer U. Family 1 uridine-5′-diphosphate glucuronosyltransferases (UGT1A): from Gilbert's syndrome to genetic organization and variability. Arch Toxicol 82 (2008) 415-433
24. Mojarrabi B., Butler R., and Mackenzie P.I. CDNA cloning and characterization of the human UDP glucuronosyltransferase, UGT1A3. Biochem Biophys Res Commun 225 (1996) 785-790
25. Green M.D., King C.D., Mojarrabi B., Mackenzie P.I., and Tephly T.R. Glucuronidation of amines and other xenobiotics catalyzed by expressed human UDP-glucuronosyltransferase 1A3. Drug Metab Dispos 26 (1998) 507-512
26. Kuehl G.E., Lampe J.W., Potter J.D., and Bigler J. Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos 33 (2005) 1027-1035
27. Prueksaritanont T., Subramanian R., Fang X., Ma B., Qiu Y., Lin J.H., et al. Glucuronidation of statins in animals and humans: a novel mechanism of statin lactonization. Drug Metab Dispos 30 (2002) 505-512
28. Iwai M., Maruo Y., Ito M., Yamamoto K., Sato H., and Takeuchi Y. Six novel UDP-glucuronosyltransferase (UGT1A3) polymorphisms with varying activity. J Hum Genet 49 (2004) 123-128
29. Kasai N., Sakaki T., Shinkyo R., Ikushiro S., Iyanagi T., Ohta M., et al. Metabolism of 26, 26, 26, 27, 27, 27-F6-1 alpha, 23S, 25-trihydroxyvitamin D3 by human UDP-glucuronosyltransferase 1A3. Drug Metab Dispos 33 (2005) 102-107
30. Lankisch T.O., Gillman T.C., Erichsen T.J., Ehmer U., Kalthoff S., Freiberg N., et al. Aryl hydrocarbon receptor (AhR)-mediated regulation of the human estrogen and bile acid UDP-glucuronosyltransferase 1A3 gene. Arch Toxicol 82 (2008) 573-582
31. Strassburg C.P., Manns M.P., and Tukey R.H. Expression of the UDP-glucuronosyltransferase 1A locus in human colon. Identification and characterization of the novel extrahepatic UGT1A8. J Biol Chem 273 (1998) 8719-8726
32. Rust C., Bauchmuller K., Bernt C., Vennegeerts T., Fickert P., Fuchsbichler A., et al. Sulfasalazine reduces bile acid induced apoptosis in human hepatoma cells and perfused rat livers. Gut 55 (2006) 719-727
33. Chen S., Beaton D., Nguyen N., Senekeo-Effenberger K., Brace-Sinnokrak E., Argikar U., et al. Tissue-specific, inducible, and hormonal control of the human UDP-glucuronosyltransferase-1 (UGT1) locus. J Biol Chem 280 (2005) 37547-37557
34. Forman B.M., Goode E., Chen J., Oro A.E., Bradley D.J., Perlmann T., et al. Identification of a nuclear receptor that is activated by farnesol metabolites. Cell 81 (1995) 687-693
35. Seol W., Choi H.S., and Moore D.D. An orphan nuclear hormone receptor that lacks a DNA binding domain and heterodimerizes with other receptors. Science 272 (1996) 1336-1339
36. Strassburg C.P., Kneip S., Topp J., Obermayer-Straub P., Barut A., Tukey R.H., et al. Polymorphic gene expression and interindividual variation of UDP-glucuronosyltransferase activity in human small intestine. J Biol Chem 275 (2000) 36164-36171
37. Strassburg C.P., Oldhafer K., Manns M.P., and Tukey R.H. Differential expression of the UGT1A locus in human liver, biliary, and gastric tissue: identification of UGT1A7 and UGT1A10 transcripts in extrahepatic tissue. Mol Pharmacol 52 (1997) 212-220
38. Glass C.K. Differential recognition of target genes by nuclear receptor monomers, dimers, and heterodimers. Endocr Rev 15 (1994) 391-407
39. Stedman C., Liddle C., Coulter S., Sonoda J., Alvarez J.G., Evans R.M., et al. Benefit of farnesoid X receptor inhibition in obstructive cholestasis. Proc Natl Acad Sci USA 103 (2006) 11323-11328