Retinoid X receptor-α-dependent transactivation by a naturally occurring structural variant of human constitutive androstane receptor (NR1I3)

Molecular Pharmacology

Volumn 68, Issue 5, 2005, Pages 1239-1253

  Auerbach, Scott S ^a   Stoner, Matthew A ^b   Su, Shengzhong ^b   Omiecinski, Curtis J ^b  

^a UNIVERSITY OF WASHINGTON SCHOOL OF MEDICINE   (United States)

^b PENNSYLVANIA STATE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6 (4 CHLOROPHENYL)IMIDAZO[2,1 B]THIAZOLE 5 CARBALDEHYDE O (3,4 DICHLOROBENZYL)OXIME; CLOTRIMAZOLE; CONSTITUTIVE ANDROSTANE RECEPTOR; CONSTITUTIVE ANDROSTANE RECEPTOR 3; CYTOCHROME P450 2B6; CYTOCHROME P450 3A4; LIGAND; RETINOID X RECEPTOR ALPHA; STEROID RECEPTOR COACTIVATOR 1; UNCLASSIFIED DRUG;

AGONIST; ANIMAL CELL; ARTICLE; ASSAY; CONTROLLED STUDY; DIMERIZATION; DNA BINDING MOTIF; ENHANCER REGION; GENE EXPRESSION; GENETIC TRANSCRIPTION; HUMAN; HUMAN CELL; MAMMAL; NONHUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN FUNCTION; PROTEIN INTERACTION; PROTEIN MOTIF; PROTEIN STRUCTURE; TRANSACTIVATION; TWO HYBRID SYSTEM;

ANIMALS; ARYL HYDROCARBON HYDROXYLASES; BASE SEQUENCE; BINDING SITES; CELLS, CULTURED; CLOTRIMAZOLE; DIMERIZATION; DNA; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTROPHORETIC MOBILITY SHIFT ASSAY; HUMANS; LIGANDS; MOLECULAR SEQUENCE DATA; OXIDOREDUCTASES, N-DEMETHYLATING; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RETINOID X RECEPTOR ALPHA; TRANS-ACTIVATION (GENETICS); TRANSCRIPTION FACTORS; TWO-HYBRID SYSTEM TECHNIQUES;

EID: 27544477927     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.105.013417     Document Type: Article

References (52)

1. Arnold KA, Eichelbaum M, and Burk O (2004) Alternative splicing affects the function and tissue-specific expression of the human constitutive androstane receptor. Nucl Recept 2:1.
2. Assem M, Schuetz EG, Leggas M, Sun D, Yasuda K, Reid G, Zelcer N, Adachi M, Strom S, Evans RM, et al. (2004) Interactions between hepatic Mrp4 and Sult2a as revealed by the constitutive androstane receptor and Mrp4 knockout mice. J Biol Chem 279:22250-22257.
3. Auerbach SS, Ramsden R, Stoner MA, Verlinde C, Hassett C, and Omiecinski CJ (2003) Alternatively spliced isoforms of the human constitutive androstane receptor. Nucleic Acids Res 31:3194-3207.
4. Baes M, Gulick T, Choi HS, Martinoli MG, Simha D, and Moore DD (1994) A new orphan member of the nuclear hormone receptor superfamily that interacts with a subset of retinoic acid response elements. Mol Cell Biol 14:1544-1551.
5. Barwick JL, Quattrochi LC, Mills AS, Potenza C, Tukey RH, and 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.
6. Chen Y, Ferguson SS, Negishi M, and Goldstein JA (2003) Identification of constitutive androstane receptor and glucocorticoid receptor binding sites in the CYP2C19 promoter. Mol Pharmacol 64:316-324.
7. Dussault I, Lin M, Hollister K, Fan M, Termini J, Sherman MA, and Forman BM (2002) A structural model of the constitutive androstane receptor defines novel interactions that mediate ligand-independent activity. Mol Cell Biol 22:5270-5280.
8. Egea PF, Rochel N, Birck C, Vachette P, Timmins PA, and Moras D (2001) Effects of ligand binding on the association properties and conformation in solution of retinoic acid receptors RXR and RAR. J Mol Biol 307:557-576.
9. Faucette SR, Wang H, Hamilton GA, Jolley SL, Gilbert D, Lindley C, Yan B, Negishi M, and LeCluyse EL (2004) Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers. Drug Metab Dispos 32:348-358.
10. Ferguson SS, LeCluyse EL, Negishi M, and Goldstein JA (2002) Regulation of human CYP2C9 by the constitutive androstane receptor: discovery of a new distal binding site. Mol Pharmacol 62:737-746.
11. Forman BM, Tzameli I, Choi HS, Chen J, Simha D, Seol W, Evans RM, and Moore DD (1998) Androstane metabolites bind to and deactivate the nuclear receptor CAR-beta. Nature (Lond) 395:612-615.
12. Frank C, Gonzalez MM, Oinonen C, Dunlop TW, and Carlberg C (2003) Characterization of DNA complexes formed by the nuclear receptor constitutive androstane receptor. J Biol Chem 278:43299-43310.
13. Geick A, Eichelbaum M, and Burk O (2001) Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem 276:14581-14587.
14. Gerbal-Chaloin S, Daujat M, Pascussi JM, Pichard-Garcia L, Vilarem MJ, and Maurel P (2002) Transcriptional regulation of CYP2C9 gene. Role of glucocorticoid receptor and constitutive androstane receptor. J Biol Chem 277:209-217.
15. Goodwin B, Hodgson E, D'Costa DJ, Robertson GR, and Liddle C (2002) Transcriptional regulation of the human CYP3A4 gene by the constitutive androstane receptor. Mol Pharmacol 62:359-365.
16. 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.
17. Guo GL, Lambert G, Negishi M, Ward JM, Brewer HB Jr, Kliewer SA, Gonzalez FJ, and Sinal CJ (2003) Complementary roles of farnesoid X receptor, pregnane X receptor and constitutive androstane receptor in protection against bile acid toxicity. J Biol Chem 278:45062-45071.
18. Handschin C and Meyer UA (2003) Induction of drug metabolism: the role of nuclear receptors. Pharmacol Rev 55:649-673.
19. Honkakoski P, Zelko I, Sueyoshi T, and 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.
20. Huang W, Zhang J, Chua SS, Qatanani M, Han Y, Granata R, and Moore DD (2003) Induction of bilirubin clearance by the constitutive androstane receptor (CAR). Proc Natl Acad Sci USA 100:4156-4161.
21. IJpenberg A, Tan NS, Gelman L, Kersten S, Seydoux J, Xu J, Metzger D, Canaple L, Chambon P, Wahli W, et al. (2004) In vivo activation of PPAR target genes by RXR homodimers. EMBO (Eur Mol Biol Organ) J 23:2083-2091.
22. Jinno H, Tanaka-Kagawa T, Hanioka N, Ishida S, Saeki M, Soyama A, Itoda M, Nishimura T, Saito Y, Ozawa S, et al. (2004) Identification of novel alternative splice variants of human constitutive androstane receptor and characterization of their expression in the liver. Mol Pharmacol 65:496-502.
23. Kawamoto T, Sueyoshi T, Zelko I, Moore R, Washburn K, and Negishi M (1999) Phenobarbital-responsive nuclear translocation of the receptor CAR in induction of the CYP2B gene. Mol Cell Biol 19:6318-6322.
24. Khorasanizadeh S and Rastinejad F (2001) Nuclear-receptor interactions on DNA-response elements. Trends Biochem Sci 26:384-390.
25. Kocarek TA and Mercer-Haines NA (2002) Squalestatin 1-inducible expression of rat CYP2B: evidence that an endogenous isoprenoid is an activator of the constitutive androstane receptor. Mol Pharmacol 62:1177-1186.
26. Kozak M (1987) An analysis of 5′-noncoding sequences from 699 vertebrate messenger RNAs. Nucleic Acids Res 15:8125-8148.
27. Lamba JK, Lamba V, Yasuda K, Lin YS, Assem M, Thompson E, Strom S, and Schuetz EG (2004) Expression of CAR splice variants in human tissues and their functional consequences. J Pharmacol Exp Ther 311:811-821.
28. Maglich JM, Parks DJ, Moore LB, Collins JL, Goodwin B, Billin AN, Stoltz CA, Kliewer SA, Lambert MH, Willson TM, et al. (2003) Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of car target genes. J Biol Chem 278:17277-17283.
29. Maglich JM, Stoltz CM, Goodwin B, Hawkins-Brown D, Moore JT, and Kliewer SA (2002) Nuclear pregnane X receptor and constitutive androstane receptor regulate overlapping but distinct sets of genes involved in xenobiotic detoxification. Mol Pharmacol 62:638-646.
30. Maglich JM, Watson J, McMillen PJ, Goodwin B, Willson TM, and Moore JT (2004) The nuclear receptor CAR is a regulator of thyroid hormone metabolism during caloric restriction. J Biol Chem 279:19832-19838.
31. Min G, Kemper JK, and Kemper B (2002) Glucocorticoid receptor-interacting protein 1 mediates ligand-independent nuclear translocation and activation of constitutive androstane receptor in vivo. J Biol Chem 277:26356-26363.
32. Moore LB, Parks DJ, Jones SA, Bledsoe RK, Consler TG, Stimmel JB, Goodwin B, Liddle C, Blanchard SG, Willson TM, et al. (2000) Orphan Nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands. J Biol Chem 275:15122-15127.
33. Moraitis AN, Giguere V, and Thompson CC (2002) Novel mechanism of nuclear receptor corepressor interaction dictated by activation function 2 helix determinants. Mol Cell Biol 22:6831-6841.
34. Nuclear Receptors Nomenclature Committee (1999) A unified nomenclature system for the nuclear receptor superfamily. Cell 97:161-163.
35. Saini SP, Sonoda J, Xu L, Toma D, Uppal H, Mu Y, Ren S, Moore DD, Evans RM, and Xie W (2004) A novel constitutive androstane receptor-mediated and CYP3A-independent pathway of bile acid detoxification. Mol Pharmacol 65:292-300.
36. Savkur RS, Wu Y, Bramlett KS, Wang M, Yao S, Perkins D, Totten M, Searfoss G 3rd, Ryan TP, Su EW, et al. (2003) Alternative splicing within the ligand binding domain of the human constitutive androstane receptor. Mol Genet Metab 80:216-226.
37. Steinmetz AC, Renaud JP, and Moras D (2001) Binding of ligands and activation of transcription by nuclear receptors. Annu Rev Biophys Biomol Struct 30:329-359.
38. Stoner M, Saville B, Wormke M, Dean D, Burghardt R, and Safe S (2002) Hypoxia induces proteasome-dependent degradation of estrogen receptor alpha in ZR-75 breast cancer cells. Mol Endocrinol 16:2231-2242.
39. Sueyoshi T, Kawamoto T, Zelko I, Honkakoski P, and Negishi M (1999) The repressed nuclear receptor CAR responds to phenobarbital in activating the human CYP2B6 gene. J Biol Chem 274:6043-6046.
40. Sugatani J, Kojima H, Ueda A, Kakizaki S, Yoshinari K, Gong QH, Owens IS, Negishi M, and Sueyoshi T (2001) The phenobarbital response enhancer module in the human bilirubin UDP-glucuronosyltransferase UGT1A1 gene and regulation by the nuclear receptor CAR. Hepatology 33:1232-1238.
41. Treuter E, Albrektsen T, Johansson L, Leers J, and Gustafsson JA (1998) A regulatory role for RIP140 in nuclear receptor activation. Mol Endocrinol 12:864-881.
42. Tzameli I, Pissios P, Schuetz EG, and Moore DD (2000) The xenobiotic compound 1,4-Bis[2-(3,5-dichloropyridyloxy)]benzene is an agonist ligand for the nuclear receptor CAR. Mol Cell Biol 20:2951-2958.
43. Ueda A, Hamadeh HK, Webb HK, Yamamoto Y, Sueyoshi T, Afshari CA, Lehmann JM, and Negishi M (2002) Diverse roles of the nuclear orphan receptor CAR in regulating hepatic genes in response to phenobarbital. Mol Pharmacol 61:1-6.
44. Urnov FD and Wolffe AP (2001) A necessary good: nuclear hormone receptors and their chromatin templates. Mol Endocrinol 15:1-16.
45. Vivat-Hannah V, Bourguet W, Gottardis M, and Gronemeyer H (2003) Separation of retinoid X receptor homo- and heterodimerization functions. Mol Cell Biol 23:7678-7688.
46. Wang H, Faucette S, Sueyoshi T, Moore R, Ferguson S, Negishi M, and LeCluyse EL (2003a) A novel distal enhancer module regulated by pregnane X receptor/constitutive androstane receptor is essential for the maximal induction of CYP2B6 gene expression. J Biol Chem 278:14146-14152.
47. Wang H and LeCluyse EL (2003) Role of orphan nuclear receptors in the regulation of drug-metabolising enzymes. Clin Pharmacokinet 42:1331-1357.
48. Wang X, Le R, I, Nicodeme E, Li R, Wagner R, Petros C, Churchill GA, Harris S, Darvasi A, Kirilovsky J, et al. (2003b) Using advanced intercross lines for high-resolution mapping of HDL cholesterol quantitative trait loci. Genome Res 13:1654-1664.
49. Wei P, Zhang J, Egan-Hafley M, Liang S, and Moore DD (2000) The nuclear receptor CAR mediates specific xenobiotic induction of drug metabolism. Nature (Lond) 407:920-923.
50. Xie W, Yeuh MF, Radominska-Pandya A, Saini SP, Negishi Y, Bottroff BS, Cabrera GY, Tukey RH, and Evans RM (2003) Control of steroid, heme and carcinogen metabolism by nuclear pregnane x receptor and constitutive androstane receptor. Proc Natl Acad Sci USA 100:4150-4155.
51. Zelko I and Negishi M (2000) Phenobarbital-elicited activation of nuclear receptor CAR in induction of cytochrome P450 genes. Biochem Biophys Res Commun 277:1-6.
52. Zhang J, Huang W, Chua SS, Wei P, and Moore DD (2002) Modulation of acetaminophen-induced hepatotoxicity by the xenobiotic receptor CAR. Science (Wash DC) 298:422-424.