Pregnane X receptor polymorphism affects CYP3A4 induction via a ligand-dependent interaction with steroid receptor coactivator-1

Pharmacogenetics and Genomics

Volumn 17, Issue 5, 2007, Pages 369-382

  Lim, Yun Ping ^a   Huang, Jin Ding ^a  

^a NATIONAL CHENG KUNG UNIVERSITY   (Taiwan)

Author keywords

Pregnane X receptor; Silencing mediator of retinoid and thyroid hormone receptor; Steroid receptor coactivator 1

Indexed keywords

CLOTRIMAZOLE; CYTOCHROME P450 3A4; NIFEDIPINE; PACLITAXEL; PREGNANE X RECEPTOR; RETINOID; RIFAMPICIN; STEROID RECEPTOR COACTIVATOR 1; THYROID HORMONE RECEPTOR;

ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; F257 GENE; GEL MOBILITY SHIFT ASSAY; GENE; GENE INDUCTION; GENE ISOLATION; GENE MUTATION; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; I346 GENE; IMMUNOPRECIPITATION; L424 GENE; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROMOTER REGION; PROTEIN EXPRESSION; PROTEIN POLYMORPHISM; PROTEIN PROTEIN INTERACTION; PROTEIN VARIANT; Q158K GENE; RECEPTOR BINDING; TRANSACTIVATION; TWO HYBRID SYSTEM; W223 GENE; WILD TYPE;

ANTINEOPLASTIC AGENTS, PHYTOGENIC; CELL LINE, TUMOR; CHROMATOGRAPHY, AFFINITY; CLOTRIMAZOLE; CYTOCHROME P-450 ENZYME SYSTEM; ELECTROPHORETIC MOBILITY SHIFT ASSAY; ENZYME INHIBITORS; GROWTH INHIBITORS; HISTONE ACETYLTRANSFERASES; HUMANS; IMMUNOPRECIPITATION; LIGANDS; MUTAGENESIS, SITE-DIRECTED; MUTATION; PACLITAXEL; PLASMIDS; POLYMORPHISM, GENETIC; RECEPTORS, STEROID; RIFAMPIN; TRANS-ACTIVATION (GENETICS); TRANSCRIPTION FACTORS; TWO-HYBRID SYSTEM TECHNIQUES;

MAMMALIA;

EID: 34247265349     PISSN: 17446872     EISSN: 17446880     Source Type: Journal    
DOI: 10.1097/FPC.0b013e32803e40d7     Document Type: Article

References (21)

1. Bertilsson G, Heidrich J, Svensson K, Asman M, Jendeberg L, Sydow-Backman M, et al. Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction. Proc Natl Acad Sci U S A 1998; 95:12208-12213.
2. Blumberg B, Sabbagh W Jr, Juguilon H, Bolado J Jr, van Meter CM, Ong ES, Evans RM. SXR, a novel steroid and xenobiotic-sensing nuclear receptor. Genes Dev 1998; 12:3195-3205.
3. Kliewer SA, Moore JT, Wade L, Staudinger JL, Watson MA, Jones SA, et al. An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway. Cell 1998; 92:73-82.
4. Lehmann JM, Mckee DD, Watson MA, Willson TM, Moore JT, Kliewer SA. The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. J Clin Invest 1998; 102:1016-1023.
5. Synold TW, Dussault I, Forman BM. The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux. Nat Med 2001; 7: 584-590.
6. Yao TP, Ku G, Zhou N, Scully R, Livingston DM. The nuclear hormone receptor coactivator SRC-1 is a specific target of p300. Proc Natl Acad Sci U S A 1996; 93:10626-10631.
7. Nolte RT, Wisely GB, Westin S, Cobb JE, Lambert MH, Kurokawa R. Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma. Nature 1998; 395:137-143.
8. Chen JD, Evans RM. A transcriptional co-repressor that interacts with nuclear hormone receptors. Nature 1995; 377:454-457.
9. Takeshita A, Taguchi M, Koibuchi N, 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 2002; 277:32453- 32458.
10. Johnson DR, Li CW, Chen LY, Ghosh JC, Chen JD. Regulation and binding of pregnane X receptor by nuclear receptor corepressor SMRT. Mol Pharm 2006; 69:99-108.
11. Wang CY, Li CW, Chen JD, Welsh WJ. Structural model reveals key interactions in the assembly of the pregnane X receptor/corepressor complex. Mol Pharm 2006; 69:1513-1517.
12. Watkins RE, Wisely GB, Moore LB, Collins JL, Lambert MH, Williams SP, et al. The human nuclear xenobiotic receptor PXR: structural determinants of directed promiscuity. Science (Washington DC) 2001; 292:2329-2333.
13. Watkins RE, Davis PR, Lambert MH, Redinbo MR. Coactivator binding promotes the specific interaction between ligand and the pregnane X receptor. J Mol Biol 2003; 331:815-828.
14. Chrencik JE, Orans J, Moore LB, Xue Y, Peng L, Collins JL, et al. Structural disorder in the complex of human pregnane X receptor and the macrolide antibiotic rifampicin. Mol Endocrinol 2005; 19:1125-1134.
15. Koyano S, Kurose K, Saito Y, Ozawa S, Hasegawa R, Komamura K, et al. Functional characterization of four naturally occurring variants of human pregnane X receptor (PXR): one variant causes dramatic loss of both DNA binding activity and the transactivation of the CYP3A4 promoter/enhancer region. Drug Metab Disp 2004; 32:149-154.
16. Hustert E, Zibat A, Presecan-Siedel E, Eiselt R, Mueller R, Fuss C, et al. Natural protein variants of pregnane X receptor with altered transactivation activity toward CYP3A4. Drug Metab Dispos 2001; 29:1454-1459.
17. Lim YP, Liu CH, Shyu LJ, Huang JD. Functional characterization of a novel polymorphism of pregnane X receptor, Q158K, in Chinese subjects. Pharmacogenet and Genom 2005; 15:337-341.
18. Bertilsson G, Jendeberg L, Berkenstam A, Uppenberg J. Identification of residues in the PXR ligand binding domain critical for species specific and constitutive activation. Eur J Biochem 2002; 269:4896-4904.
19. Pfrunder A, Gutmann H, Beglinger C, Drewe J. Gene expression of CYP3A4, ABC-transporters (MDR1 and MRP1-MRP5) and hPXR in three different human colon carcinoma cell lines. J Pharm Pharm 2003; 55: 59-66.
20. Glass CK, Rosenfeld MG. The coregulator exchange in transcriptional functions of nuclear receptors. Genes Dev 2000; 14:121-141.
21. Takeshita A, Taguchi M, Koibuchi N, Ozawa Y. Putative role of the orphan nuclear receptor SXR (steroid and xenobiotic receptor) in the mechanism of CYP3A4 inhibition by xenobiotics. J Bio Chem 2002; 277:32453- 32458.