Transcriptional regulation of human UDP-glucuronosyltransferase genes

Drug Metabolism Reviews

Volumn 46, Issue 4, 2014, Pages 421-458

  Hu, Dong Gui ^a   Meech, Robyn ^a   McKinnon, Ross A ^a   Mackenzie, Peter I ^a  

^a FLINDERS UNIVERSITY   (Australia)

Author keywords

Enhancer; Gene regulation; Nuclear receptors; Promoter; Transcription factors; UDP glucuronosyltransferase genes

Indexed keywords

GLUCURONOSYLTRANSFERASE; GLUCURONOSYLTRANSFERASE 1A1; GLUCURONOSYLTRANSFERASE 1A10; GLUCURONOSYLTRANSFERASE 1A3; GLUCURONOSYLTRANSFERASE 1A4; GLUCURONOSYLTRANSFERASE 1A5; GLUCURONOSYLTRANSFERASE 1A6; GLUCURONOSYLTRANSFERASE 1A7; GLUCURONOSYLTRANSFERASE 1A8; GLUCURONOSYLTRANSFERASE 1A9; GLUCURONOSYLTRANSFERASE 2B10; GLUCURONOSYLTRANSFERASE 2B11; GLUCURONOSYLTRANSFERASE 2B15; GLUCURONOSYLTRANSFERASE 2B17; GLUCURONOSYLTRANSFERASE 2B28; GLUCURONOSYLTRANSFERASE 2B4; GLUCURONOSYLTRANSFERASE 2B7; LIGAND; MESSENGER RNA; TRANSCRIPTION FACTOR; UNCLASSIFIED DRUG; GLUCURONIDE;

CONJUGATION; ENHANCER REGION; GENE EXPRESSION; GLUCURONIDATION; HUMAN; PROMOTER REGION; REGULATORY SEQUENCE; REVIEW; TISSUE SPECIFICITY; TRANSCRIPTION REGULATION; ANIMAL; ANTIBODY SPECIFICITY; ENZYMOLOGY; GENE EXPRESSION REGULATION; GENETIC TRANSCRIPTION; GENETICS; LIVER; METABOLISM;

ANIMALS; GENE EXPRESSION REGULATION, ENZYMOLOGIC; GLUCURONIDES; GLUCURONOSYLTRANSFERASE; HUMANS; LIVER; ORGAN SPECIFICITY; RNA, MESSENGER; TRANSCRIPTION, GENETIC;

EID: 84908604636     PISSN: 03602532     EISSN: 10979883     Source Type: Journal    
DOI: 10.3109/03602532.2014.973037     Document Type: Review

References (470)

1. Achour B, Rostami-Hodjegan A, Barber J. (2014a). Protein expression of various hepatic uridine 5′-diphosphate glucuronosyltransferase (UGT) enzymes and their inter-correlations: A meta-analysis. Biopharm Drug Dispos 35: 353-361.
2. Achour B, Russell MR, Barber J, Rostami-Hodjegan A. (2014b). Simultaneous quantification of the abundance of several cytochrome P450 and uridine 5′-diphospho-glucuronosyltransferase enzymes in human liver microsomes using multiplexed targeted proteomics. Drug Metab Dispos 42: 500-510.
3. Aden DP, Fogel A, Plotkin S, et al. (1979). Controlled synthesis of HBsAg in a differentiated human liver carcinoma-derived cell line. Nature 282: 615-616.
4. Al Saabi A, Allorge D, Sauvage FL, et al. (2013). Involvement of UDP-glucuronosyltransferases UGT1A9 and UGT2B7 in ethanol glucuronidation, and interactions with common drugs of abuse. Drug Metab Dispos 41: 568-574.
5. Aleksunes LM, Klaassen CD. (2012). Coordinated regulation of hepatic phase I and II drug-metabolizing genes and transporters using AhR-, CAR-, PXR-, PPARalpha-, and Nrf2-null mice. Drug Metab Dispos 40: 1366-1379.
6. Alonen A, Aitio O, Hakala K, et al. (2005). Biosynthesis of dobutamine monoglucuronides and glucuronidation of dobutamine by recombinant human UDP-glucuronosyltransferases. Drug Metab Dispos 33: 657-663.
7. Alonen A, Finel M, Kostiainen R. (2008). The human UDP-glucuronosyltransferase UGT1A3 is highly selective towards N2 in the tetrazole ring of losartan, candesartan, and zolarsartan. Biochem Pharmacol 76: 763-772.
8. Andersson TB, Kanebratt KP, Kenna JG. (2012). The HepaRG cell line: A unique in vitro tool for understanding drug metabolism and toxicology in human. Expert Opin Drug Metab Toxicol 8: 909-920.
9. Aninat C, Piton A, Glaise D, et al. (2006). Expression of cytochromes P450, conjugating enzymes and nuclear receptors in human hepatoma HepaRG cells. Drug Metab Dispos 34: 75-83.
10. Aprile S, Del Grosso E, Grosa G. (2010). Identification of the human UDP-glucuronosyltransferases involved in the glucuronidation of combretastatin A-4. Drug Metab Dispos 38: 1141-1146.
11. Argikar UA, Remmel RP. (2009). Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos 37: 229-236.
12. Aueviriyavit S, Furihata T, Morimoto K, et al. (2007). Hepatocyte nuclear factor 1 alpha and 4 alpha are factors involved in interindividual variability in the expression of UGT1A6 and UGT1A9 but not UGT1A1, UGT1A3 and UGT1A4 mRNA in human livers. Drug Metab Pharmacokinet 22: 391-395.
13. Augello MA, Hickey TE, Knudsen KE. (2011). FOXA1: Master of steroid receptor function in cancer. EMBO J 30: 3885-3894.
14. Balliet RM, Chen G, Gallagher CJ, et al. (2009). Characterization of UGTs active against SAHA and association between SAHA glucuronidation activity phenotype with UGT genotype. Cancer Res 69: 2981-2989.
15. Bao BY, Chuang BF, Wang Q, et al. (2008). Androgen receptor mediates the expression of UDP-glucuronosyltransferase 2 B15 and B17 genes. Prostate 68: 839-848.
16. Barbier O, Belanger A. (2008). Inactivation of androgens by UDP-glucuronosyltransferases in the human prostate. Best Pract Res Clin Endocrinol Metab 22: 259-270.
17. Barbier O, Duran-Sandoval D, Pineda-Torra I, et al. (2003a). Peroxisome proliferator-activated receptor alpha induces hepatic expression of the human bile acid glucuronidating UDP-glucuronosyltransferase 2B4 enzyme. J Biol Chem 278: 32852-32860.
18. Barbier O, Girard H, Inoue Y, et al. (2005). Hepatic expression of the UGT1A9 gene is governed by hepatocyte nuclear factor 4alpha. Mol Pharmacol 67: 241-249.
19. Barbier O, Torra IP, Sirvent A, et al. (2003b). FXR induces the UGT2B4 enzyme in hepatocytes: A potential mechanism of negative feedback control of FXR activity. Gastroenterology 124: 1926-1940.
20. Barbier O, Trottier J, Kaeding J, et al. (2009). Lipid-activated transcription factors control bile acid glucuronidation. Mol Cell Biochem 326: 3-8.
21. Barbier O, Turgeon D, Girard C, et al. (2000). 3′-azido-3′-deoxythimidine (AZT) is glucuronidated by human UDP-glucuronosyltransferase 2B7 (UGT2B7). Drug Metab Dispos 28: 497-502.
22. Barbier O, Villeneuve L, Bocher V, et al. (2003c). The UDP-glucuronosyltransferase 1A9 enzyme is a peroxisome proliferatoractivated receptor alpha and gamma target gene. J Biol Chem 278: 13975-13983.
23. Basseville A, Preisser L, de Carne Trecesson S, et al. (2011). Irinotecan induces steroid and xenobiotic receptor (SXR) signaling to detoxification pathway in colon cancer cells. Mol Cancer 10: 80.
24. Basu NK, Kole L, Basu M, et al. (2008). The major chemicaldetoxifying system of UDP-glucuronosyltransferases requires regulated phosphorylation supported by protein kinase C. J Biol Chem 283: 23048-23061.
25. Basu NK, Kole L, Owens IS. (2003). Evidence for phosphorylation requirement for human bilirubin UDP-glucuronosyltransferase (UGT1A1) activity. Biochem Biophys Res Commun 303: 98-104.
26. Basu NK, Kovarova M, Garza A, et al. (2005). Phosphorylation of a UDP-glucuronosyltransferase regulates substrate specificity. Proc Natl Acad Sci USA 102: 6285-6290.
27. Basu NK, Kubota S, Meselhy MR, et al. (2004). Gastrointestinally distributed UDP-glucuronosyltransferase 1A10, which metabolizes estrogens and nonsteroidal anti-inflammatory drugs, depends upon phosphorylation. J Biol Chem 279: 28320-28329.
28. Beaulieu M, Levesque E, Hum DW, Belanger A. (1996). Isolation and characterization of a novel cDNA encoding a human UDP-glucuronosyltransferase active on C19 steroids. J Biol Chem 271: 22855-22862.
29. Beaulieu M, Levesque E, Hum DW, Belanger A. (1998). Isolation and characterization of a human orphan UDP-glucuronosyltransferase, UGT2B11. Biochem Biophys Res Commun 248: 44-50.
30. Belanger A, Hum DW, Beaulieu M, et al. (1998). Characterization and regulation of UDP-glucuronosyltransferases in steroid target tissues. J Steroid Biochem Mol Biol 65: 301-310.
31. Belanger AS, Caron P, Harvey M, et al. (2009). Glucuronidation of the antiretroviral drug efavirenz by UGT2B7 and an in vitro investigation of drug-drug interaction with zidovudine. Drug Metab Dispos 37: 1793-1796.
32. Belanger AS, Tojcic J, Harvey M, Guillemette C. (2010). Regulation of UGT1A1 and HNF1 transcription factor gene expression by DNA methylation in colon cancer cells. BMC Mol Biol 11: 9.
33. Belanger G, Beaulieu M, Marcotte B, et al. (1995). Expression of transcripts encoding steroid UDP-glucuronosyltransferases in human prostate hyperplastic tissue and the LNCaP cell line. Mol Cell Endocrinol 113: 165-173.
34. Bellemare J, Rouleau M, Girard H, et al. (2010a). Alternatively spliced products of the UGT1A gene interact with the enzymatically active proteins to inhibit glucuronosyltransferase activity in vitro. Drug Metab Dispos 38: 1785-1789.
35. Bellemare J, Rouleau M, Harvey M, Guillemette C. (2010b). Modulation of the human glucuronosyltransferase UGT1A pathway by splice isoform polypeptides is mediated through protein-protein interactions. J Biol Chem 285: 3600-3607.
36. Bellemare J, Rouleau M, Harvey M, et al. (2010c). Alternative-splicing forms of the major phase II conjugating UGT1A gene negatively regulate glucuronidation in human carcinoma cell lines. Pharmacogenomics J 10: 431-441.
37. Benoit-Biancamano MO, Adam JP, Bernard O, et al. (2009a). A pharmacogenetics study of the human glucuronosyltransferase UGT1A4. Pharmacogenet Genomics 19: 945-954.
38. Benoit-Biancamano MO, Connelly J, Villeneuve L, et al. (2009b). Deferiprone glucuronidation by human tissues and recombinant UDP glucuronosyltransferase 1A6: An in vitro investigation of genetic and splice variants. Drug Metab Dispos 37: 322-329.
39. Bernard O, Guillemette C. (2004). The main role of UGT1A9 in the hepatic metabolism of mycophenolic acid and the effects of naturally occurring variants. Drug Metab Dispos 32: 775-778.
40. Bernard P, Goudonnet H, Artur Y, et al. (1999). Activation of the mouse TATA-less and human TATA-containing UDP-glucuronosyltransferase 1A1 promoters by hepatocyte nuclear factor 1. Mol Pharmacol 56: 526-536.
41. Beutler E, Gelbart T, Demina A. (1998). Racial variability in the UDP-glucuronosyltransferase 1 (UGT1A1) promoter: A balanced polymorphism for regulation of bilirubin metabolism? Proc Natl Acad Sci USA 95: 8170-8174.
42. Birrell SN, Bentel JM, Hickey TE, et al. (1995). Androgens induce divergent proliferative responses in human breast cancer cell lines. J Steroid Biochem Mol Biol 52: 459-467.
43. Bock KW. (2010). Functions and transcriptional regulation of adult human hepatic UDP-glucuronosyl-transferases (UGTs): Mechanisms responsible for interindividual variation of UGT levels. Biochem Pharmacol 80: 771-777.
44. Bock KW. (2011). From differential induction of UDP-glucuronosyltransferases in rat liver to characterization of responsible ligandactivated transcription factors, and their multilevel crosstalk in humans. Biochem Pharmacol 82: 9-16.
45. Bock KW. (2012). Human UDP-glucuronosyltransferases: Feedback loops between substrates and ligands of their transcription factors. Biochem Pharmacol 84: 1000-1006.
46. Bock KW, Forster A, Gschaidmeier H, et al. (1993). Paracetamol glucuronidation by recombinant rat and human phenol UDP-glucuronosyltransferases. Biochem Pharmacol 45: 1809-1814.
47. Bock KW, Kohle C. (2005). UDP-glucuronosyltransferase 1A6: Structural, functional, and regulatory aspects. Methods Enzymol 400: 57-75.
48. Boersma MG, van der Woude H, Bogaards J, et al. (2002). Regioselectivity of phase II metabolism of luteolin and quercetin by UDP-glucuronosyl transferases. Chem Res Toxicol 15: 662-670.
49. Bonzo JA, Belanger A, Tukey RH. (2007). The role of chrysin and the ah receptor in induction of the human UGT1A1 gene in vitro and in transgenic UGT1 mice. Hepatology 45: 349-360.
50. Bosma PJ, Chowdhury JR, Bakker C, et al. (1995). The genetic basis of the reduced expression of bilirubin UDP-glucuronosyltransferase 1 in Gilbert's syndrome. N Engl J Med 333: 1171-1175.
51. Bosma PJ, Seppen J, Goldhoorn B, et al. (1994). Bilirubin UDP-glucuronosyltransferase 1 is the only relevant bilirubin glucuronidating isoform in man. J Biol Chem 269: 17960-17964.
52. Boyd M, Hansen M, Jensen TG, et al. (2010). Genome-wide analysis of CDX2 binding in intestinal epithelial cells (Caco-2). J Biol Chem 285: 25115-25125.
53. Brand W, Boersma MG, Bik H, et al. (2010). Phase II metabolism of hesperetin by individual UDP-glucuronosyltransferases and sulfotransferases and rat and human tissue samples. Drug Metab Dispos 38: 617-625.
54. Bulger M, Groudine M. (2011). Functional and mechanistic diversity of distal transcription enhancers. Cell 144: 327-339.
55. Cai H, Nguyen N, Peterkin V, et al. (2010). A humanized UGT1 mouse model expressing the UGT1A1∗28 allele for assessing drug clearance by UGT1A1-dependent glucuronidation. Drug Metab Dispos 38: 879-886.
56. Cai L, Huang W, Chou KC. (2012). Prostate cancer with variants in CYP17 and UGT2B17 genes: A meta-analysis. Protein Pept Lett 19: 62-69.
57. Caillier B, Lepine J, Tojcic J, et al. (2007). A pharmacogenomics study of the human estrogen glucuronosyltransferase UGT1A3. Pharmacogenet Genomics 17: 481-495.
58. Carroll JS, Liu XS, Brodsky AS, et al. (2005). Chromosome-wide mapping of estrogen receptor binding reveals long-range regulation requiring the forkhead protein FoxA1. Cell 122: 33-43.
59. Chakraborty SK, Basu NK, Jana S, et al. (2012). Protein kinase Calpha and Src kinase support human prostate-distributed dihydrotestosterone-metabolizing UDP-glucuronosyltransferase 2B15 activity. J Biol Chem 287: 24387-24396.
60. Chan AT, Tranah GJ, Giovannucci EL, et al. (2005). Genetic variants in the UGT1A6 enzyme, aspirin use, and the risk of colorectal adenoma. J Natl Cancer Inst 97: 457-460.
61. Chen F, Ritter JK, Wang MG, et al. (1993). Characterization of a cloned human dihydrotestosterone/androstanediol UDP-glucuronosyltransferase and its comparison to other steroid isoforms. Biochemistry 32: 10648-10657.
62. Chen G, Blevins-Primeau AS, Dellinger RW, et al. (2007). Glucuronidation of nicotine and cotinine by UGT2B10: Loss of function by the UGT2B10 Codon 67 (Asp>Tyr) polymorphism. Cancer Res 67: 9024-9029.
63. Chen G, Dellinger RW, Sun D, et al. (2008a). Glucuronidation of tobacco-specific nitrosamines by UGT2B10. Drug Metab Dispos 36: 824-830.
64. Chen G, Giambrone Jr NE, Dluzen DF, et al. (2010a). Glucuronidation genotypes and nicotine metabolic phenotypes: Importance of functional UGT2B10 and UGT2B17 polymorphisms. Cancer Res 70: 7543-7552.
65. Chen G, Giambrone NE, Lazarus P. (2012a). Glucuronidation of trans- 3′-hydroxycotinine by UGT2B17 and UGT2B10. Pharmacogenet Genomics 22: 183-190.
66. Chen H, Yang K, Choi S, et al. (2009). Up-regulation of UDP-glucuronosyltransferase (UGT) 1A4 by 17beta-estradiol: A potential mechanism of increased lamotrigine elimination in pregnancy. Drug Metab Dispos 37: 1841-1847.
67. Chen M, Leduc B, Kerr S, et al. (2010b). Identification of human UGT2B7 as the major isoform involved in the O-glucuronidation of chloramphenicol. Drug Metab Dispos 38: 368-375.
68. Chen S, Beaton D, Nguyen N, et al. (2005). Tissue-specific, inducible, and hormonal control of the human UDP-glucuronosyltransferase-1 (UGT1) locus. J Biol Chem 280: 37547-37557.
69. Chen S, Yueh MF, Evans RM, Tukey RH. (2012b). Pregnane-X-receptor controls hepatic glucuronidation during pregnancy and neonatal development in humanized UGT1 mice. Hepatology 56: 658-667.
70. Chen Y, Xie S, Chen S, Zeng S. (2008b). Glucuronidation of flavonoids by recombinant UGT1A3 and UGT1A9. Biochem Pharmacol 76: 416-425.
71. Cheng Z, Radominska-Pandya A, Tephly TR. (1998a). Cloning and expression of human UDP-glucuronosyltransferase (UGT) 1A8. Arch Biochem Biophys 356: 301-305.
72. Cheng Z, Rios GR, King CD, et al. (1998b). Glucuronidation of catechol estrogens by expressed human UDP-glucuronosyltransferases (UGTs) 1A1, 1A3, and 2B7. Toxicol Sci 45: 52-57.
73. Chouinard S, Barbier O, Belanger A. (2007). UDP-glucuronosyltransferase 2B15 (UGT2B15) and UGT2B17 enzymes are major determinants of the androgen response in prostate cancer LNCaP cells. J Biol Chem 282: 33466-33474.
74. Chouinard S, Pelletier G, Belanger A, Barbier O. (2006a). Isoformspecific regulation of uridine diphosphate-glucuronosyltransferase 2B enzymes in the human prostate: Differential consequences for androgen and bioactive lipid inactivation. Endocrinology 147: 5431-5442.
75. Chouinard S, Tessier M, Vernouillet G, et al. (2006b). Inactivation of the pure antiestrogen fulvestrant and other synthetic estrogen molecules by UDP-glucuronosyltransferase 1A enzymes expressed in breast tissue. Mol Pharmacol 69: 908-920.
76. Chouinard S, Yueh MF, Tukey RH, et al. (2008). Inactivation by UDP-glucuronosyltransferase enzymes: The end of androgen signaling. J Steroid Biochem Mol Biol 109: 247-253.
77. Chu XY, Liang Y, Cai X, et al. (2009). Metabolism and renal elimination of gaboxadol in humans: Role of UDP-glucuronosyltransferases and transporters. Pharm Res 26: 459-468.
78. Chung D, Park D, Myers K, et al. (2013). dPeak: High resolution identification of transcription factor binding sites from PET and SET ChIP-Seq data. PLoS Comput Biol 9: e1003246.
79. Chung JY, Cho JY, Yu KS, et al. (2005). Effect of the UGT2B15 genotype on the pharmacokinetics, pharmacodynamics, and drug interactions of intravenous lorazepam in healthy volunteers. Clin Pharmacol Ther 77: 486-494.
80. Ciotti M, Basu N, Brangi M, Owens IS. (1999). Glucuronidation of 7-ethyl-10-hydroxycamptothecin (SN-38) by the human UDP-glucuronosyltransferases encoded at the UGT1 locus. Biochem Biophys Res Commun 260: 199-202.
81. Ciotti M, Chen F, Rubaltelli FF, Owens IS. (1998). Coding defect and a TATA box mutation at the bilirubin UDP-glucuronosyltransferase gene cause Crigler-Najjar type I disease. Biochim Biophys Acta 1407: 40-50.
82. Cirillo LA, Lin FR, Cuesta I, et al. (2002). Opening of compacted chromatin by early developmental transcription factors HNF3 (FoxA) and GATA-4. Mol Cell 9: 279-289.
83. Cirillo LA, Zaret KS. (1999). An early developmental transcription factor complex that is more stable on nucleosome core particles than on free DNA. Mol Cell 4: 961-969.
84. Claudel T, Inoue Y, Barbier O, et al. (2003). Farnesoid X receptor agonists suppress hepatic apolipoprotein CIII expression. Gastroenterology 125: 544-555.
85. Claudel T, Sturm E, Duez H, et al. (2002). Bile acid-activated nuclear receptor FXR suppresses apolipoprotein A-I transcription via a negative FXR response element. J Clin Invest 109: 961-971.
86. Coffman BL, Rios GR, King CD, Tephly TR. (1997). Human UGT2B7 catalyzes morphine glucuronidation. Drug Metab Dispos 25: 1-4.
87. Congiu M, Mashford ML, Slavin JL, Desmond PV. (2009). Coordinate regulation of metabolic enzymes and transporters by nuclear transcription factors in human liver disease. J Gastroenterol Hepatol 24: 1038-1044.
88. Court MH. (2005). Isoform-selective probe substrates for in vitro studies of human UDP-glucuronosyltransferases. Methods Enzymol 400: 104-116.
89. Court MH. (2010). Interindividual variability in hepatic drug glucuronidation: Studies into the role of age, sex, enzyme inducers, and genetic polymorphism using the human liver bank as a model system. Drug Metab Rev 42: 209-224.
90. Court MH, Duan SX, Guillemette C, et al. (2002). Stereoselective conjugation of oxazepam by human UDP-glucuronosyltransferases (UGTs): S-oxazepam is glucuronidated by UGT2B15, while R-oxazepam is glucuronidated by UGT2B7 and UGT1A9. Drug Metab Dispos 30: 1257-1265.
91. Court MH, Duan SX, Von Moltke LL, et al. (2001). Interindividual variability in acetaminophen glucuronidation by human liver microsomes: Identification of relevant acetaminophen UDP-glucuronosyltransferase isoforms. J Pharmacol Exp Ther 299: 998-1006.
92. Court MH, Zhang X, Ding X, et al. (2012). Quantitative distribution of mRNAs encoding the 19 human UDP-glucuronosyltransferase enzymes in 26 adult and 3 fetal tissues. Xenobiotica 42: 266-277.
93. Crozier A, Jaganath IB, Clifford MN. (2009). Dietary phenolics: Chemistry, bioavailability and effects on health. Nat Prod Rep 26: 1001-1043.
94. Czernik PJ, Little JM, Barone GW, et al. (2000). Glucuronidation of estrogens and retinoic acid and expression of UDP-glucuronosyltransferase 2B7 in human intestinal mucosa. Drug Metab Dispos 28: 1210-1216.
95. de Almagro MC, Selga E, Thibaut R, et al. (2011). UDP-glucuronosyltransferase 1A6 overexpression in breast cancer cells resistant to methotrexate. Biochem Pharmacol 81: 60-70.
96. de Haan GJ, Edelbroek P, Segers J, et al. (2004). Gestation-induced changes in lamotrigine pharmacokinetics: A monotherapy study. Neurology 63: 571-573.
97. Dellinger RW, Chen G, Blevins-Primeau AS, et al. (2007). Glucuronidation of PhIP and N-OH-PhIP by UDP-glucuronosyltransferase 1A10. Carcinogenesis 28: 2412-2418.
98. Dellinger RW, Fang JL, Chen G, et al. (2006). Importance of UDP-glucuronosyltransferase 1A10 (UGT1A10) in the detoxification of polycyclic aromatic hydrocarbons: Decreased glucuronidative activity of the UGT1A10139Lys isoform. Drug Metab Dispos 34: 943-949.
99. Dellinger RW, Matundan HH, Ahmed AS, et al. (2012). Anti-cancer drugs elicit re-expression of UDP-glucuronosyltransferases in melanoma cells. PLoS One 7: e47696.
100. Dluzen DF, Sun D, Salzberg AC, et al. (2014). Regulation of UDP-glucuronosyltransferase 1A1 expression and activity by microRNA 491-3p. J Pharmacol Exp Ther 348: 465-477.
101. Doane AS, Danso M, Lal P, et al. (2006). An estrogen receptor-negative breast cancer subset characterized by a hormonally regulated transcriptional program and response to androgen. Oncogene 25: 3994-4008.
102. Donato MT, Jover R, Gomez-Lechon MJ. (2013). Hepatic cell lines for drug hepatotoxicity testing: limitations and strategies to upgrade their metabolic competence by gene engineering. Curr Drug Metab 14: 946-968.
103. Donato MT, Lahoz A, Castell JV, Gomez-Lechon MJ. (2008). Cell lines: A tool for in vitro drug metabolism studies. Curr Drug Metab 9: 1-11.
104. Drummond F, Sowden J, Morrison K, Edwards YH. (1996). The caudaltype homeobox protein Cdx-2 binds to the colon promoter of the carbonic anhydrase 1 gene. Eur J Biochem 236: 670-681.
105. Drummond FJ, Sowden J, Morrison K, Edwards YH. (1998). Colon carbonic anhydrase 1: Transactivation of gene expression by the homeodomain protein Cdx2. FEBS Lett 423: 218-222.
106. Du J, You T, Chen X, Zhong D. (2013). Stereoselective glucuronidation of ornidazole in humans: Predominant contribution of UDP-glucuronosyltransferases 1A9 and 2B7. Drug Metab Dispos 41: 1306-1318.
107. Duguay Y, Baar C, Skorpen F, Guillemette C. (2004). A novel functional polymorphism in the uridine diphosphate-glucuronosyltransferase 2B7 promoter with significant impact on promoter activity. Clin Pharmacol Ther 75: 223-233.
108. Ebner T, Remmel RP, Burchell B. (1993). Human bilirubin UDP-glucuronosyltransferase catalyzes the glucuronidation of ethinylestradiol. Mol Pharmacol 43: 649-654.
109. Ebner T, Wagner K, Wienen W. (2010). Dabigatran acylglucuronide, the major human metabolite of dabigatran: In vitro formation, stability, and pharmacological activity. Drug Metab Dispos 38: 1567-1575.
110. Edavana VK, Dhakal IB, Williams S, et al. (2013a). Potential role of UGT1A4 promoter SNPs in anastrozole pharmacogenomics. Drug Metab Dispos 41: 870-877.
111. Edavana VK, Penney RB, Yao-Borengasser A, et al. (2013b). Fulvestrant up regulates UGT1A4 and MRPs through ERalpha and c-Myb pathways: A possible primary drug disposition mechanism. Springerplus 2: 620.
112. Ehmer U, Kalthoff S, Lankisch TO, et al. (2010). Shared regulation of UGT1A7 by hepatocyte nuclear factor (HNF) 1alpha and HNF4alpha. Drug Metab Dispos 38: 1246-1257.
113. Ehmer U, Vogel A, Schutte JK, et al. (2004). Variation of hepatic glucuronidation: Novel functional polymorphisms of the UDP-glucuronosyltransferase UGT1A4. Hepatology 39: 970-977.
114. Erichsen TJ, Aehlen A, Ehmer U, et al. (2010). Regulation of the human bile acid UDP-glucuronosyltransferase 1A3 by the farnesoid X receptor and bile acids. J Hepatol 52: 570-578.
115. Erichsen TJ, Ehmer U, Kalthoff S, et al. (2008). Genetic variability of aryl hydrocarbon receptor (AhR)-mediated regulation of the human UDP glucuronosyltransferase (UGT) 1A4 gene. Toxicol Appl Pharmacol 230: 252-260.
116. Fallon JK, Harbourt DE, Maleki SH, et al. (2008). Absolute quantification of human uridine-diphosphate glucuronosyl transferase (UGT) enzyme isoforms 1A1 and 1A6 by tandem LC-MS. Drug Metab Lett 2: 210-222.
117. Fallon JK, Neubert H, Goosen TC, Smith PC. (2013a). Targeted precise quantification of 12 human recombinant uridine-diphosphate glucuronosyl transferase 1A and 2B isoforms using nanoultra-high-performance liquid chromatography/tandem mass spectrometry with selected reaction monitoring. Drug Metab Dispos 41: 2076-2080.
118. Fallon JK, Neubert H, Hyland R, et al. (2013b). Targeted quantitative proteomics for the analysis of 14 UGT1As and -2Bs in human liver using NanoUPLC-MS/MS with selected reaction monitoring. J Proteome Res 12: 4402-4413.
119. Fedejko-Kap B, Bratton SM, Finel M, et al. (2012). Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: Highly selective substrates for UGT1A10. Drug Metab Dispos 40: 1736-1743.
120. Finel M, Li X, Gardner-Stephen D, et al. (2005). Human UDP-glucuronosyltransferase 1A5: Identification, expression, and activity. J Pharmacol Exp Ther 315: 1143-1149.
121. Fogh J, Fogh JM, Orfeo T. (1977a). One hundred and twenty-seven cultured human tumor cell lines producing tumors in nude mice. J Natl Cancer Inst 59: 221-226.
122. Fogh J, Wright WC, Loveless JD. (1977b). Absence of HeLa cell contamination in 169 cell lines derived from human tumors. J Natl Cancer Inst 58: 209-214.
123. Fujiwara R, Nguyen N, Chen S, Tukey RH. (2010). Developmental hyperbilirubinemia and CNS toxicity in mice humanized with the UDP glucuronosyltransferase 1 (UGT1) locus. Proc Natl Acad Sci USA 107: 5024-5029.
124. Gaganis P, Miners JO, Knights KM. (2007). Glucuronidation of fenamates: Kinetic studies using human kidney cortical microsomes and recombinant UDP-glucuronosyltransferase (UGT) 1A9 and 2B7. Biochem Pharmacol 73: 1683-1691.
125. Gagnon JF, Bernard O, Villeneuve L, et al. (2006). Irinotecan inactivation is modulated by epigenetic silencing of UGT1A1 in colon cancer. Clin Cancer Res 12: 1850-1858.
126. Gall WE, Zawada G, Mojarrabi B, et al. (1999). Differential glucuronidation of bile acids, androgens and estrogens by human UGT1A3 and 2B7. J Steroid Biochem Mol Biol 70: 101-108.
127. Gallagher CJ, Kadlubar FF, Muscat JE, et al. (2007). The UGT2B17 gene deletion polymorphism and risk of prostate cancer. A casecontrol study in Caucasians. Cancer Detect Prev 31: 310-315.
128. Gao X, Grignon DJ, Chbihi T, et al. (1995). Elevated 12-lipoxygenase mRNA expression correlates with advanced stage and poor differentiation of human prostate cancer. Urology 46: 227-237.
129. Gardner-Stephen D, Heydel JM, Goyal A, et al. (2004). Human PXR variants and their differential effects on the regulation of human UDP-glucuronosyltransferase gene expression. Drug Metab Dispos 32: 340-347.
130. Gardner-Stephen DA, Mackenzie PI. (2007a). Hepatocyte nuclear factor1 transcription factors are essential for the UDP-glucuronosyltransferase 1A9 promoter response to hepatocyte nuclear factor 4alpha. Pharmacogenet Genomics 17: 25-36.
131. Gardner-Stephen DA, Mackenzie PI. (2007b). Isolation of the UDP-glucuronosyltransferase 1A3 and 1A4 proximal promoters and characterization of their dependence on the transcription factor hepatocyte nuclear factor 1alpha. Drug Metab Dispos 35: 116-120.
132. Gardner-Stephen DA, Mackenzie PI. (2008). Liver-enriched transcription factors and their role in regulating UDP glucuronosyltransferase gene expression. Curr Drug Metab 9: 439-452.
133. Ghosal A, Hapangama N, Yuan Y, et al. (2004a). Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of ezetimibe (Zetia). Drug Metab Dispos 32: 314-320.
134. Ghosal A, Yuan Y, Hapangama N, et al. (2004b). Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of 3-hydroxydesloratadine. Biopharm Drug Dispos 25: 243-252.
135. Girard C, Barbier O, Veilleux G, et al. (2003). Human uridine diphosphate-glucuronosyltransferase UGT2B7 conjugates mineralocorticoid and glucocorticoid metabolites. Endocrinology 144: 2659-2668.
136. Girard H, Court MH, Bernard O, et al. (2004). Identification of common polymorphisms in the promoter of the UGT1A9 gene: Evidence that UGT1A9 protein and activity levels are strongly genetically controlled in the liver. Pharmacogenetics 14: 501-515.
137. Goldstein I, Rivlin N, Shoshana OY, et al. (2013). Chemotherapeutic agents induce the expression and activity of their clearing enzyme CYP3A4 by activating p53. Carcinogenesis 34: 190-198.
138. Goldstone JV. (2008). Environmental sensing and response genes in cnidaria: The chemical defensome in the sea anemone Nematostella vectensis. Cell Biol Toxicol 24: 483-502.
139. Goldstone JV, Hamdoun A, Cole BJ, et al. (2006). The chemical defensome: Environmental sensing and response genes in the Strongylocentrotus purpuratus genome. Dev Biol 300: 366-384.
140. Green MD, King CD, Mojarrabi B, et al. (1998). Glucuronidation of amines and other xenobiotics catalyzed by expressed human UDP-glucuronosyltransferase 1A3. Drug Metab Dispos 26: 507-512.
141. Green MD, Oturu EM, Tephly TR. (1994). Stable expression of a human liver UDP-glucuronosyltransferase (UGT2B15) with activity toward steroid and xenobiotic substrates. Drug Metab Dispos 22: 799-805.
142. Green MD, Tephly TR. (1996). Glucuronidation of amines and hydroxylated xenobiotics and endobiotics catalyzed by expressed human UGT1.4 protein. Drug Metab Dispos 24: 356-363.
143. Gregory PA, Gardner-Stephen DA, Rogers A, et al. (2006). The caudalrelated homeodomain protein Cdx2 and hepatocyte nuclear factor 1alpha cooperatively regulate the UDP-glucuronosyltransferase 2B7 gene promoter. Pharmacogenet Genomics 16: 527-536.
144. Gregory PA, Hansen AJ, Mackenzie PI. (2000). Tissue specific differences in the regulation of the UDP glucuronosyltransferase 2B17 gene promoter. Pharmacogenetics 10: 809-820.
145. Gregory PA, Lewinsky RH, Gardner-Stephen DA, Mackenzie PI. (2004a). Coordinate regulation of the human UDP-glucuronosyltransferase 1A8, 1A9, and 1A10 genes by hepatocyte nuclear factor 1alpha and the caudal-related homeodomain protein 2. Mol Pharmacol 65: 953-963.
146. Gregory PA, Lewinsky RH, Gardner-Stephen DA, Mackenzie PI. (2004b). Regulation of UDP glucuronosyltransferases in the gastrointestinal tract. Toxicol Appl Pharmacol 199: 354-363.
147. Gregory PA, Mackenzie PI. (2002). The homeodomain Pbx2-Prep1 complex modulates hepatocyte nuclear factor 1alpha-mediated activation of the UDP-glucuronosyltransferase 2B17 gene. Mol Pharmacol 62: 154-161.
148. Gripon P, Rumin S, Urban S, et al. (2002). Infection of a human hepatoma cell line by hepatitis B virus. Proc Natl Acad Sci USA 99: 15655-15660.
149. Grosse L, Campeau AS, Caron S, et al. (2013). Enantiomer selective glucuronidation of the non-steroidal pure anti-androgen bicalutamide by human liver and kidney: Role of the human UDP-glucuronosyltransferase (UGT)1A9 enzyme. Basic Clin Pharmacol Toxicol 113: 92-102.
150. Guillemette C, Hum DW, Belanger A. (1995). Specificity of glucuronosyltransferase activity in the human cancer cell line LNCaP, evidence for the presence of at least two glucuronosyltransferase enzymes. J Steroid Biochem Mol Biol 55: 355-362.
151. Guillemette C, Hum DW, Belanger A. (1996a). Evidence for a role of glucuronosyltransferase in the regulation of androgen action in the human prostatic cancer cell line LNCaP. J Steroid Biochem Mol Biol 57: 225-231.
152. Guillemette C, Hum DW, Belanger A. (1996b). Regulation of steroid glucuronosyltransferase activities and transcripts by androgen in the human prostatic cancer LNCaP cell line. Endocrinology 137: 2872-2879.
153. Guillemette C, Levesque E, Beaulieu M, et al. (1997). Differential regulation of two uridine diphospho-glucuronosyltransferases, UGT2B15 and UGT2B17, in human prostate LNCaP cells. Endocrinology 138: 2998-3005.
154. Guillemette C, Levesque E, Harvey M, et al. (2010). UGT genomic diversity: Beyond gene duplication. Drug Metab Rev 42: 24-44.
155. Hagenauer B, Salamon A, Thalhammer T, et al. (2001). In vitro glucuronidation of the cyclin-dependent kinase inhibitor flavopiridol by rat and human liver microsomes: Involvement of UDP-glucuronosyltransferases 1A1 and 1A9. Drug Metab Dispos 29: 407-414.
156. Hajdinjak T, Zagradisnik B. (2004). Prostate cancer and polymorphism D85Y in gene for dihydrotestosterone degrading enzyme UGT2B15: Frequency of DD homozygotes increases with Gleason Score. Prostate 59: 436-439.
157. Hall RE, Birrell SN, Tilley WD, Sutherland RL. (1994). MDA-MB-453, an androgen-responsive human breast carcinoma cell line with high level androgen receptor expression. Eur J Cancer 30A: 484-490.
158. Han SX, Wang L, Wu DQ. (2012). The association between UGT1A7 polymorphism and cancer risk: A meta-analysis. Cancer Epidemiol 36: e201-e206.
159. Hancks DC, Kazazian HH, Jr. (2010). SVA retrotransposons: Evolution and genetic instability. Semin Cancer Biol 20: 234-245.
160. Hanioka N, Hayashi K, Shimizudani T, et al. (2008a). Stereoselective glucuronidation of propranolol in human and cynomolgus monkey liver microsomes: Role of human hepatic UDP-glucuronosyltransferase isoforms, UGT1A9, UGT2B4 and UGT2B7. Pharmacology 82: 293-303.
161. Hanioka N, Naito T, Narimatsu S. (2008b). Human UDP-glucuronosyltransferase isoforms involved in bisphenol A glucuronidation. Chemosphere 74: 33-36.
162. Hanioka N, Nonaka Y, Saito K, et al. (2012). Effect of aflatoxin B1 on UDP-glucuronosyltransferase mRNA expression in HepG2 cells. Chemosphere 89: 526-529.
163. Hanioka N, Ozawa S, Jinno H, et al. (2001). Human liver UDP-glucuronosyltransferase isoforms involved in the glucuronidation of 7-ethyl-10-hydroxycamptothecin. Xenobiotica 31: 687-699.
164. Harbourt DE, Fallon JK, Ito S, et al. (2012). Quantification of human uridine-diphosphate glucuronosyl transferase 1A isoforms in liver, intestine, and kidney using nanobore liquid chromatography-tandem mass spectrometry. Anal Chem 84: 98-105.
165. Harden CL. (2007). Pregnancy and epilepsy. Semin Neurol 27: 453-459.
166. Harding D, Fournel-Gigleux S, Jackson MR, Burchell B. (1988). Cloning and substrate specificity of a human phenol UDP-glucuronosyltransferase expressed in COS-7 cells. Proc Natl Acad Sci USA 85: 8381-8385.
167. Harmsen S, Meijerman I, Beijnen JH, Schellens JH. (2007). The role of nuclear receptors in pharmacokinetic drug-drug interactions in oncology. Cancer Treat Rev 33: 369-380.
168. Harrington WR, Sengupta S, Katzenellenbogen BS. (2006). Estrogen regulation of the glucuronidation enzyme UGT2B15 in estrogen receptor-positive breast cancer cells. Endocrinology 147: 3843-3850.
169. Haslemo T, Loryan I, Ueda N, et al. (2012). UGT1A4∗3 encodes significantly increased glucuronidation of olanzapine in patients on maintenance treatment and in recombinant systems. Clin Pharmacol Ther 92: 221-227.
170. He X, Hesse LM, Hazarika S, et al. (2009). Evidence for oxazepam as an in vivo probe of UGT2B15: Oxazepam clearance is reduced by UGT2B15 D85Y polymorphism but unaffected by UGT2B17 deletion. Br J Clin Pharmacol 68: 721-730.
171. Hedrick CC, Kim MD, Natarajan RD, Nadler JL. (1999). 12-Lipoxygenase products increase monocyte: endothelial interactions. Adv Exp Med Biol 469: 455-460.
172. Hernandez N. (1993). TBP, a universal eukaryotic transcription factor? Genes Dev 7: 1291-1308.
173. Hewitt NJ, Lecluyse EL, Ferguson SS. (2007). Induction of hepatic cytochrome P450 enzymes: Methods, mechanisms, recommendations, and in vitro-in vivo correlations. Xenobiotica 37: 1196-1224.
174. Hiller A, Nguyen N, Strassburg CP, et al. (1999). Retigabine N-glucuronidation and its potential role in enterohepatic circulation. Drug Metab Dispos 27: 605-612.
175. Honn KV, Tang DG, Gao X, et al. (1994). 12-Lipoxygenases and 12(S)- HETE: Role in cancer metastasis. Cancer Metastasis Rev 13: 365-396.
176. Horn J, Milewska M, Arnold SM, Leggas M. (2011). Metabolic pathways of the camptothecin analog AR-67. Drug Metab Dispos 39: 683-692.
177. Horoszewicz JS, Leong SS, Chu TM, et al. (1980). The LNCaP cell line - A new model for studies on human prostatic carcinoma. Prog Clin Biol Res 37: 115-132.
178. Horoszewicz JS, Leong SS, Kawinski E, et al. (1983). LNCaP model of human prostatic carcinoma. Cancer Res 43: 1809-1818.
179. Howell A, Pippen J, Elledge RM, et al. (2005). Fulvestrant versus anastrozole for the treatment of advanced breast carcinoma: A prospectively planned combined survival analysis of two multicenter trials. Cancer 104: 236-239.
180. Howell A, Robertson JF, Abram P, et al. (2004). Comparison of fulvestrant versus tamoxifen for the treatment of advanced breast cancer in postmenopausal women previously untreated with endocrine therapy: A multinational, double-blind, randomized trial. J Clin Oncol 22: 1605-1613.
181. Hsieh TY, Shiu TY, Huang SM, et al. (2007). Molecular pathogenesis of Gilbert's syndrome: Decreased TATA-binding protein binding affinity of UGT1A1 gene promoter. Pharmacogenet Genomics 17: 229-236.
182. Hu DG, Gardner-Stephen D, Severi G, et al. (2010). A novel polymorphism in a forkhead box A1 (FOXA1) binding site of the human UDP glucuronosyltransferase 2B17 gene modulates promoter activity and is associated with altered levels of circulating androstane- 3alpha,17beta-diol glucuronide. Mol Pharmacol 78: 714-722.
183. Hu DG, Mackenzie PI. (2009). Estrogen receptor alpha, fos-related antigen-2, and c-Jun coordinately regulate human UDP glucuronosyltransferase 2B15 and 2B17 expression in response to 17beta-estradiol in MCF-7 cells. Mol Pharmacol 76: 425-439.
184. Hu DG, Mackenzie PI. (2010). Forkhead box protein A1 regulates UDP-glucuronosyltransferase 2B15 gene transcription in LNCaP prostate cancer cells. Drug Metab Dispos 38: 2105-2109.
185. Hu DG, Meech R, Lu L, et al. (2014a). Polymorphisms and haplotypes of the UDP-glucuronosyltransferase 2B7 gene promoter. Drug Metab Dispos 42: 854-862.
186. Hu DG, Rogers A, Mackenzie PI. (2014b). Epirubicin upregulates UDP glucuronosyltransferase 2B7 expression in liver cancer cells via the p53 pathway. Mol Pharmacol 85: 887-897.
187. Huskey SE, Magdalou J, Ouzzine M, et al. (1994). N-glucuronidation reactions. III. Regioselectivity of N-glucuronidation of methylbiphenyl tetrazole, methylbiphenyl triazole, and methylbiphenyl imidazole using human and rat recombinant UDP-glucuronosyltransferases stably expressed in V79 cells. Drug Metab Dispos 22: 659-662.
188. Hutt AJ, Caldwell J, Smith RL. (1986). The metabolism of aspirin in man: A population study. Xenobiotica 16: 239-249.
189. Innocenti F, Iyer L, Ramirez J, et al. (2001). Epirubicin glucuronidation is catalyzed by human UDP-glucuronosyltransferase 2B7. Drug Metab Dispos 29: 686-692.
190. Ishii Y, Hansen AJ, Mackenzie PI. (2000). Octamer transcription factor-1 enhances hepatic nuclear factor-1alpha-mediated activation of the human UDP glucuronosyltransferase 2B7 promoter. Mol Pharmacol 57: 940-947.
191. Itaaho K, Mackenzie PI, Ikushiro S, et al. (2008). The configuration of the 17-hydroxy group variably influences the glucuronidation of betaestradiol and epiestradiol by human UDP-glucuronosyltransferases. Drug Metab Dispos 36: 2307-2315.
192. Iwuchukwu OF, Tallarida RJ, Nagar S. (2011). Resveratrol in combination with other dietary polyphenols concomitantly enhances antiproliferation and UGT1A1 induction in Caco-2 cells. Life Sci 88: 1047-1054.
193. Iyer L, King CD, Whitington PF, et al. (1998). Genetic predisposition to the metabolism of irinotecan (CPT-11). Role of uridine diphosphate glucuronosyltransferase isoform 1A1 in the glucuronidation of its active metabolite (SN-38) in human liver microsomes. J Clin Invest 101: 847-854.
194. Iyer LV, Ho MN, Shinn WM, et al. (2003). Glucuronidation of 10-hydroxyestragole (10-HE) by human UDP-glucuronosyltransferases UGT2B7 and UGT1A9. Toxicol Sci 73: 36-43.
195. Izukawa T, Nakajima M, Fujiwara R, et al. (2009). Quantitative analysis of UDP-glucuronosyltransferase (UGT) 1A and UGT2B expression levels in human livers. Drug Metab Dispos 37: 1759-1768.
196. Jin C, Miners JO, Lillywhite KJ, Mackenzie PI. (1993a). Complementary deoxyribonucleic acid cloning and expression of a human liver uridine diphosphate-glucuronosyltransferase glucuronidating carboxylic acidcontaining drugs. J Pharmacol Exp Ther 264: 475-479.
197. Jin CJ, Mackenzie PI, Miners JO. (1997). The regio- and stereoselectivity of C19 and C21 hydroxysteroid glucuronidation by UGT2B7 and UGT2B11. Arch Biochem Biophys 341: 207-211.
198. Jin CJ, Miners JO, Burchell B, Mackenzie PI. (1993b). The glucuronidation of hydroxylated metabolites of benzo[a]pyrene and 2-acetylaminofluorene by cDNA-expressed human UDP-glucuronosyltransferases. Carcinogenesis 14: 2637-2639.
199. Jin CJ, Miners JO, Lillywhite KJ, Mackenzie PI. (1993c). cDNA cloning and expression of two new members of the human liver UDP-glucuronosyltransferase 2B subfamily. Biochem Biophys Res Commun 194: 496-503.
200. Jones NR, Lazarus P. (2014). UGT2B gene expression analysis in multiple tobacco carcinogen-targeted tissues. Drug Metab Dispos 42: 529-536.
201. Jones NR, Sun D, Freeman WM, Lazarus P. (2012). Quantification of Hepatic UDP glucuronosyltransferase 1A splice variant expression and correlation of UDP glucuronosyltransferase 1A1 variant expression with glucuronidation activity. J Pharmacol Exp Ther 342: 720-729.
202. Jover R, Bort R, Gomez-Lechon MJ, Castell JV. (1998). Re-expression of C/EBP alpha induces CYP2B6, CYP2C9 and CYP2D6 genes in HepG2 cells. FEBS Lett 431: 227-230.
203. Jude AR, Little JM, Bull AW, et al. (2001). 13-Hydroxy- and 13-oxooctadecadienoic acids: Novel substrates for human UDP-glucuronosyltransferases. Drug Metab Dispos 29: 652-655.
204. Jurka J, Kapitonov VV, Pavlicek A, et al. (2005). Repbase update, a database of eukaryotic repetitive elements. Cytogenet Genome Res 110: 462-467.
205. Kaeding J, Belanger J, Caron P, et al. (2008a). Calcitrol (1alpha,25-dihydroxyvitamin D3) inhibits androgen glucuronidation in prostate cancer cells. Mol Cancer Ther 7: 380-390.
206. Kaeding J, Bouchaert E, Belanger J, et al. (2008b). Activators of the farnesoid X receptor negatively regulate androgen glucuronidation in human prostate cancer LNCAP cells. Biochem J 410: 245-253.
207. Kaivosaari S, Finel M, Koskinen M. (2011). N-glucuronidation of drugs and other xenobiotics by human and animal UDP-glucuronosyltransferases. Xenobiotica 41: 652-669.
208. Kaivosaari S, Toivonen P, Hesse LM, et al. (2007). Nicotine glucuronidation and the human UDP-glucuronosyltransferase UGT2B10. Mol Pharmacol 72: 761-768.
209. Kalthoff S, Ehmer U, Freiberg N, et al. (2010a). Coffee induces expression of glucuronosyltransferases by the aryl hydrocarbon receptor and Nrf2 in liver and stomach. Gastroenterology 139: 1699-1710, 1710 e1-2.
210. Kalthoff S, Ehmer U, Freiberg N, et al. (2010b). Interaction between oxidative stress sensor Nrf2 and xenobiotic-activated aryl hydrocarbon receptor in the regulation of the human phase II detoxifying UDP-glucuronosyltransferase 1A10. J Biol Chem 285: 5993-6002.
211. Kamdem LK, Liu Y, Stearns V, et al. (2010). In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol 70: 854-869.
212. Kanebratt KP, Andersson TB. (2008). Evaluation of HepaRG cells as an in vitro model for human drug metabolism studies. Drug Metab Dispos 36: 1444-1452.
213. Kang SP, Ramirez J, House L, et al. (2010). A pharmacogenetic study of vorinostat glucuronidation. Pharmacogenet Genomics 20: 638-641.
214. Karypidis AH, Olsson M, Andersson SO, et al. (2008). Deletion polymorphism of the UGT2B17 gene is associated with increased risk for prostate cancer and correlated to gene expression in the prostate. Pharmacogenomics J 8: 147-151.
215. Kasai N, Sakaki T, Shinkyo R, et al. (2005). Metabolism of 26,26,26,27,27,27-F6-1 alpha,23S,25-trihydroxyvitamin D3 by human UDP-glucuronosyltransferase 1A3. Drug Metab Dispos 33: 102-107.
216. Kassahun K, Mattiuz E, Nyhart Jr E, et al. (1997). Disposition and biotransformation of the antipsychotic agent olanzapine in humans. Drug Metab Dispos 25: 81-93.
217. Kato Y, Izukawa T, Oda S, et al. (2013). Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos 41: 1389-1397.
218. Kato Y, Nakajima M, Oda S, et al. (2012). Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution. Drug Metab Dispos 40: 240-248.
219. Kelavkar U, Cohen C, Eling T, Badr K. (2002a). 15-Lipoxygenase-1 overexpression in prostate adenocarcinoma. Adv Exp Med Biol 507: 133-145.
220. Kelavkar U, Glasgow W, Eling TE. (2002b). The effect of 15-lipoxygenase-1 expression on cancer cells. Curr Urol Rep 3: 207-214.
221. Kelavkar UP, Cohen C, Kamitani H, et al. (2000). Concordant induction of 15-lipoxygenase-1 and mutant p53 expression in human prostate adenocarcinoma: Correlation with Gleason staging. Carcinogenesis 21: 1777-1787.
222. Kemp DC, Fan PW, Stevens JC. (2002). Characterization of raloxifene glucuronidation in vitro: Contribution of intestinal metabolism to presystemic clearance. Drug Metab Dispos 30: 694-700.
223. Kerdpin O, Elliot DJ, Mackenzie PI, Miners JO. (2006). Sulfinpyrazone C-glucuronidation is catalyzed selectively by human UDP-glucuronosyltransferase 1A9. Drug Metab Dispos 34: 1950-1953.
224. King CD, Rios GR, Assouline JA, Tephly TR. (1999). Expression of UDP-glucuronosyltransferases (UGTs) 2B7 and 1A6 in the human brain and identification of 5-hydroxytryptamine as a substrate. Arch Biochem Biophys 365: 156-162.
225. Knights KM, Winner LK, Elliot DJ, et al. (2009). Aldosterone glucuronidation by human liver and kidney microsomes and recombinant UDP-glucuronosyltransferases: Inhibition by NSAIDs. Br J Clin Pharmacol 68: 402-412.
226. Kpoghomou MA, Soatiana JE, Kalembo FW, et al. (2013). UGT2B17 polymorphism and risk of prostate cancer: A meta-analysis. ISRN Oncol 2013: 465916.
227. Krasinski SD, van Wering HM, Tannemaat MR, Grand RJ. (2001). Differential activation of intestinal gene promoters: Functional interactions between GATA-5 and HNF-1 alpha. Am J Physiol Gastrointest Liver Physiol 281: G69-G84.
228. Krishnaswamy S, Duan SX, von Moltke LL, et al. (2003). Validation of serotonin (5-hydroxtryptamine) as an in vitro substrate probe for human UDP-glucuronosyltransferase (UGT) 1A6. Drug Metab Dispos 31: 133-139.
229. Kuehl GE, Lampe JW, Potter JD, Bigler J. (2005). Glucuronidation of nonsteroidal anti-inflammatory drugs: Identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos 33: 1027-1035.
230. Kuehl GE, Murphy SE. (2003). N-glucuronidation of nicotine and cotinine by human liver microsomes and heterologously expressed UDP-glucuronosyltransferases. Drug Metab Dispos 31: 1361-1368.
231. Kweekel D, Guchelaar HJ, Gelderblom H. (2008). Clinical and pharmacogenetic factors associated with irinotecan toxicity. Cancer Treat Rev 34: 656-669.
232. Lacko M, Roelofs HM, Te Morsche RH, et al. (2009). Genetic polymorphisms in the tobacco smoke carcinogens detoxifying enzyme UGT1A7 and the risk of head and neck cancer. Head Neck 31: 1274-1281.
233. Laganiere J, Deblois G, Lefebvre C, et al. (2005). From the cover: Location analysis of estrogen receptor alpha target promoters reveals that FOXA1 defines a domain of the estrogen response. Proc Natl Acad Sci USA 102: 11651-11656.
234. Lai E, Prezioso VR, Smith E, et al. (1990). HNF-3A, a hepatocyteenriched transcription factor of novel structure is regulated transcriptionally. Genes Dev 4: 1427-1436.
235. Lankisch TO, Gillman TC, Erichsen TJ, et al. (2008). Aryl hydrocarbon receptor-mediated regulation of the human estrogen and bile acid UDP-glucuronosyltransferase 1A3 gene. Arch Toxicol 82: 573-582.
236. Lankisch TO, Vogel A, Eilermann S, et al. (2005). Identification and characterization of a functional TATA box polymorphism of the UDP glucuronosyltransferase 1A7 gene. Mol Pharmacol 67: 1732-1739.
237. Larsson SC, Wolk A. (2007). Coffee consumption and risk of liver cancer: A meta-analysis. Gastroenterology 132: 1740-1745.
238. Lautala P, Ethell BT, Taskinen J, Burchell B. (2000). The specificity of glucuronidation of entacapone and tolcapone by recombinant human UDP-glucuronosyltransferases. Drug Metab Dispos 28: 1385-1389.
239. Lee HS, Ji HY, Park EJ, Kim SY. (2007). In vitro metabolism of eupatilin by multiple cytochrome P450 and UDP-glucuronosyltransferase enzymes. Xenobiotica 37: 803-817.
240. Lepine J, Bernard O, Plante M, et al. (2004). Specificity and regioselectivity of the conjugation of estradiol, estrone, and their catecholestrogen and methoxyestrogen metabolites by human uridine diphospho-glucuronosyltransferases expressed in endometrium. J Clin Endocrinol Metab 89: 5222-5232.
241. Levesque E, Beaulieu M, Green MD, et al. (1997). Isolation and characterization of UGT2B15(Y85): A UDP-glucuronosyltransferase encoded by a polymorphic gene. Pharmacogenetics 7: 317-325.
242. Levesque E, Beaulieu M, Guillemette C, et al. (1998). Effect of interleukins on UGT2B15 and UGT2B17 steroid uridine diphosphate-glucuronosyltransferase expression and activity in the LNCaP cell line. Endocrinology 139: 2375-2381.
243. Levesque E, Beaulieu M, Hum DW, Belanger A. (1999). Characterization and substrate specificity of UGT2B4 (E458): A UDP-glucuronosyltransferase encoded by a polymorphic gene. Pharmacogenetics 9: 207-216.
244. Levesque E, Girard H, Journault K, et al. (2007). Regulation of the UGT1A1 bilirubin-conjugating pathway: Role of a new splicing event at the UGT1A locus. Hepatology 45: 128-138.
245. Levesque E, Menard V, Laverdiere I, et al. (2010). Extensive splicing of transcripts encoding the bile acid-conjugating enzyme UGT2B4 modulates glucuronidation. Pharmacogenet Genomics 20: 195-210.
246. Levesque E, Turgeon D, Carrier JS, et al. (2001). Isolation and characterization of the UGT2B28 cDNA encoding a novel human steroid conjugating UDP-glucuronosyltransferase. Biochemistry 40: 3869-3881.
247. Lewinsky RH, Smith PA, Mackenzie PI. (2005). Glucuronidation of bioflavonoids by human UGT1A10: Structure-function relationships. Xenobiotica 35: 117-129.
248. Li X, Bratton S, Radominska-Pandya A. (2007). Human UGT1A8 and UGT1A10 mRNA are expressed in primary human hepatocytes. Drug Metab Pharmacokinet 22: 152-161.
249. Li X, Shang L, Wu Y, et al. (2011). Identification of the human UDP-glucuronosyltransferase isoforms involved in the glucuronidation of the phytochemical ferulic acid. Drug Metab Pharmacokinet 26: 341-350.
250. Limenta LM, Jirasomprasert T, Tankanitlert J, et al. (2008). UGT1A6 genotype-related pharmacokinetics of deferiprone (L1) in healthy volunteers. Br J Clin Pharmacol 65: 908-916.
251. Lindberg BS, Johansson ED, Nilsson BA. (1974). Plasma levels of nonconjugated oestradiol-17beta and oestriol in high risk pregnancies. Acta Obstet Gynecol Scand Suppl 32: 37-51.
252. Little JM, Williams L, Xu J, Radominska-Pandya A. (2002). Glucuronidation of the dietary fatty acids, phytanic acid and docosahexaenoic acid, by human UDP-glucuronosyltransferases. Drug Metab Dispos 30: 531-533.
253. Loureiro AI, Bonifacio MJ, Fernandes-Lopes C, et al. (2006). Human metabolism of nebicapone (BIA 3-202), a novel catechol-o-methyltransferase inhibitor: Characterization of in vitro glucuronidation. Drug Metab Dispos 34: 1856-1862.
254. Loureiro AI, Fernandes-Lopes C, Bonifacio MJ, et al. (2011). Hepatic UDP-glucuronosyltransferase is responsible for eslicarbazepine glucuronidation. Drug Metab Dispos 39: 1486-1494.
255. Lu PH, Chen MB, Wu XY, et al. (2011). Genetic polymorphisms of UGT1A7 and cancer risk: Evidence from 21 case-control studies. Cancer Invest 29: 645-654.
256. Lu Y, Heydel JM, Li X, et al. (2005). Lithocholic acid decreases expression of UGT2B7 in Caco-2 cells: A potential role for a negative farnesoid X receptor response element. Drug Metab Dispos 33: 937-946.
257. Lubberstedt M, Muller-Vieira U, Mayer M, et al. (2011). HepaRG human hepatic cell line utility as a surrogate for primary human hepatocytes in drug metabolism assessment in vitro. J Pharmacol Toxicol Methods 63: 59-68.
258. Luo G, Guenthner T, Gan LS, Humphreys WG. (2004). CYP3A4 induction by xenobiotics: Biochemistry, experimental methods and impact on drug discovery and development. Curr Drug Metab 5: 483-505.
259. Lupien M, Eeckhoute J, Meyer CA, et al. (2008). FoxA1 translates epigenetic signatures into enhancer-driven lineage-specific transcription. Cell 132: 958-970.
260. Ma L, Sun J, Peng Y, et al. (2012). Glucuronidation of edaravone by human liver and kidney microsomes: Biphasic kinetics and identification of UGT1A9 as the major UDP-glucuronosyltransferase isoform. Drug Metab Dispos 40: 734-741.
261. Macintyre G, Bailey J, Haviv I, Kowalczyk A. (2010). IS-rSNP: A novel technique for in silico regulatory SNP detection. Bioinformatics 26: i524-i530.
262. Mackenzie PI, Bock KW, Burchell B, et al. (2005). Nomenclature update for the mammalian UDP glycosyltransferase (UGT) gene superfamily. Pharmacogenet Genomics 15: 677-685.
263. Mackenzie PI, Hu DG, Gardner-Stephen DA. (2010). The regulation of UDP-glucuronosyltransferase genes by tissue-specific and ligandactivated transcription factors. Drug Metab Rev 42: 99-109.
264. Mackenzie PI, Owens IS, Burchell B, et al. (1997). The UDP glycosyltransferase gene superfamily: Recommended nomenclature update based on evolutionary divergence. Pharmacogenetics 7: 255-269.
265. Macleod SL, Nowell S, Plaxco J, Lang NP. (2000). An allele-specific polymerase chain reaction method for the determination of the D85Y polymorphism in the human UDP-glucuronosyltransferase 2B15 gene in a case-control study of prostate cancer. Ann Surg Oncol 7: 777-782.
266. Mahajan MK, Uttamsingh V, Gan LS, et al. (2011). Identification and characterization of oxymetazoline glucuronidation in human liver microsomes: Evidence for the involvement of UGT1A9. J Pharm Sci 100: 784-793.
267. Malfatti MA, Felton JS. (2001). N-glucuronidation of 2-amino-1-methyl- 6-phenylimidazo[4,5-b]pyridine (PhIP) and N-hydroxy-PhIP by specific human UDP-glucuronosyltransferases. Carcinogenesis 22: 1087-1093.
268. Mano Y, Usui T, Kamimura H. (2007a). Contribution of UDP-glucuronosyltransferases 1A9 and 2B7 to the glucuronidation of indomethacin in the human liver. Eur J Clin Pharmacol 63: 289-296.
269. Mano Y, Usui T, Kamimura H. (2007b). Predominant contribution of UDP-glucuronosyltransferase 2B7 in the glucuronidation of racemic flurbiprofen in the human liver. Drug Metab Dispos 35: 1182-1187.
270. Mano Y, Usui T, Kamimura H. (2007c). The UDP-glucuronosyltransferase 2B7 isozyme is responsible for gemfibrozil glucuronidation in the human liver. Drug Metab Dispos 35: 2040-2044.
271. Marelli L, Stigliano R, Triantos C, et al. (2007). Transarterial therapy for hepatocellular carcinoma: which technique is more effective? A systematic review of cohort and randomized studies. Cardiovasc Intervent Radiol 30: 6-25.
272. Matsui K, Maruo Y, Sato H, Takeuchi Y. (2010). Combined effect of regulatory polymorphisms on transcription of UGT1A1 as a cause of Gilbert syndrome. BMC Gastroenterol 10: 57.
273. Maul R, Warth B, Schebb NH, et al. (2014). In vitro glucuronidation kinetics of deoxynivalenol by human and animal microsomes and recombinant human UGT enzymes. Arch Toxicol. [Epub ahead of print].
274. Mazur A, Lichti CF, Prather PL, et al. (2009). Characterization of human hepatic and extrahepatic UDP-glucuronosyltransferase enzymes involved in the metabolism of classic cannabinoids. Drug Metab Dispos 37: 1496-1504.
275. McCarroll SA, Hadnott TN, Perry GH, et al. (2006). Common deletion polymorphisms in the human genome. Nat Genet 38: 86-92.
276. Mehta RS, Barlow WE, Albain KS, et al. (2012). Combination anastrozole and fulvestrant in metastatic breast cancer. N Engl J Med 367: 435-444.
277. Menard V, Collin P, Margaillan G, Guillemette C. (2013). Modulation of the UGT2B7 enzyme activity by C-terminally truncated proteins derived from alternative splicing. Drug Metab Dispos 41: 2197-2205.
278. Menard V, Eap O, Harvey M, et al. (2009). Copy-number variations (CNVs) of the human sex steroid metabolizing genes UGT2B17 and UGT2B28 and their associations with a UGT2B15 functional polymorphism. Hum Mutat 30: 1310-1319.
279. Menard V, Eap O, Roberge J, et al. (2011). Transcriptional diversity at the UGT2B7 locus is dictated by extensive pre-mRNA splicing mechanisms that give rise to multiple mRNA splice variants. Pharmacogenet Genomics 21: 631-641.
280. Miksits M, Maier-Salamon A, Vo TP, et al. (2010). Glucuronidation of piceatannol by human liver microsomes: Major role of UGT1A1, UGT1A8 and UGT1A10. J Pharm Pharmacol 62: 47-54.
281. Milne AM, Burchell B, Coughtrie MW. (2011). A novel method for the immunoquantification of UDP-glucuronosyltransferases in human tissue. Drug Metab Dispos 39: 2258-2263.
282. Mitchelmore C, Troelsen JT, Spodsberg N, et al. (2000). Interaction between the homeodomain proteins Cdx2 and HNF1alpha mediates expression of the lactase-phlorizin hydrolase gene. Biochem J 346 Pt 2: 529-535.
283. Mitra PS, Basu NK, Basu M, et al. (2011). Regulated phosphorylation of a major UDP-glucuronosyltransferase isozyme by tyrosine kinases dictates endogenous substrate selection for detoxification. J Biol Chem 286: 1639-1648.
284. Mitra PS, Basu NK, Owens IS. (2009). Src supports UDP-glucuronosyltransferase- 2B7 detoxification of catechol estrogens associated with breast cancer. Biochem Biophys Res Commun 382: 651-656.
285. Mitro N, Vargas L, Romeo R, et al. (2007). T0901317 is a potent PXR ligand: Implications for the biology ascribed to LXR. FEBS Lett 581: 1721-1726.
286. Modi AA, Feld JJ, Park Y, et al. (2010). Increased caffeine consumption is associated with reduced hepatic fibrosis. Hepatology 51: 201-209.
287. Mojarrabi B, Butler R, Mackenzie PI. (1996). cDNA cloning and characterization of the human UDP glucuronosyltransferase, UGT1A3. Biochem Biophys Res Commun 225: 785-790.
288. Mojarrabi B, Mackenzie PI. (1997). The human UDP glucuronosyltransferase, UGT1A10, glucuronidates mycophenolic acid. Biochem Biophys Res Commun 238: 775-778.
289. Monaghan G, Burchell B, Boxer M. (1997). Structure of the human UGT2B4 gene encoding a bile acid UDP-glucuronosyltransferase. Mamm Genome 8: 692-694.
290. Moore NL, Buchanan G, Harris JM, et al. (2012). An androgen receptor mutation in the MDA-MB-453 cell line model of molecular apocrine breast cancer compromises receptor activity. Endocr Relat Cancer 19: 599-613.
291. Mori A, Maruo Y, Iwai M, et al. (2005). UDP-glucuronosyltransferase 1A4 polymorphisms in a Japanese population and kinetics of clozapine glucuronidation. Drug Metab Dispos 33: 672-675.
292. Moya M, Gomez-Lechon MJ, Castell JV, Jover R. (2010). Enhanced steatosis by nuclear receptor ligands: A study in cultured human hepatocytes and hepatoma cells with a characterized nuclear receptor expression profile. Chem Biol Interact 184: 376-387.
293. Munzel PA, Lehmkoster T, Bruck M, et al. (1998). Aryl hydrocarbon receptor-inducible or constitutive expression of human UDP glucuronosyltransferase UGT1A6. Arch Biochem Biophys 350: 72-78.
294. Munzel PA, Schmohl S, Buckler F, et al. (2003). Contribution of the Ah receptor to the phenolic antioxidant-mediated expression of human and rat UDP-glucuronosyltransferase UGT1A6 in Caco-2 and rat hepatoma 5L cells. Biochem Pharmacol 66: 841-847.
295. Murai T, Samata N, Iwabuchi H, Ikeda T. (2006). Human UDP-glucuronosyltransferase, UGT1A8, glucuronidates dihydrotestosterone to a monoglucuronide and further to a structurally novel diglucuronide. Drug Metab Dispos 34: 1102-1108.
296. Murata M, Warren EH, Riddell SR. (2003). A human minor histocompatibility antigen resulting from differential expression due to a gene deletion. J Exp Med 197: 1279-1289.
297. Mutlib AE, Goosen TC, Bauman JN, et al. (2006). Kinetics of acetaminophen glucuronidation by UDP-glucuronosyltransferases 1A1, 1A6, 1A9 and 2B15. Potential implications in acetaminopheninduced hepatotoxicity. Chem Res Toxicol 19: 701-709.
298. Nakajima M, Yamanaka H, Fujiwara R, et al. (2007). Stereoselective glucuronidation of 5-(4′-hydroxyphenyl)-5-phenylhydantoin by human UDP-glucuronosyltransferase (UGT) 1A1, UGT1A9, and UGT2B15: Effects of UGT-UGT interactions. Drug Metab Dispos 35: 1679-1686.
299. Nakamura A, Nakajima M, Higashi E, et al. (2008a). Genetic polymorphisms in the 5′-flanking region of human UDP-glucuronosyltransferase 2B7 affect the Nrf2-dependent transcriptional regulation. Pharmacogenet Genomics 18: 709-720.
300. Nakamura A, Nakajima M, Yamanaka H, et al. (2008b). Expression of UGT1A and UGT2B mRNA in human normal tissues and various cell lines. Drug Metab Dispos 36: 1461-1464.
301. Natarajan R, Reddy MA, Malik KU, et al. (2001). Signaling mechanisms of nuclear factor-kappab-mediated activation of inflammatory genes by 13-hydroperoxyoctadecadienoic acid in cultured vascular smooth muscle cells. Arterioscler Thromb Vasc Biol 21: 1408-1413.
302. Nehlig A, Debry G. (1994). Potential genotoxic, mutagenic and antimutagenic effects of coffee: a review. Mutat Res 317: 145-162.
303. Ngan S, Stronach EA, Photiou A, et al. (2009). Microarray coupled to quantitative RT-PCR analysis of androgen-regulated genes in human LNCaP prostate cancer cells. Oncogene 28: 2051-2063.
304. Nie D, Nemeth J, Qiao Y, et al. (2003). Increased metastatic potential in human prostate carcinoma cells by overexpression of arachidonate 12-lipoxygenase. Clin Exp Metastasis 20: 657-663.
305. Niemeyer ED, Brodbelt JS. (2013). Regiospecificity of human UDP-glucuronosyltransferase isoforms in chalcone and flavanone glucuronidation determined by metal complexation and tandem mass spectrometry. J Nat Prod 76: 1121-1132.
306. Nishihara M, Hiura Y, Kawaguchi N, et al. (2013). UDP-glucuronosyltransferase 2B15 (UGT2B15) is the major enzyme responsible for sipoglitazar glucuronidation in humans: Retrospective identification of the UGT isoform by in vitro analysis and the effect of UGT2B15∗2 mutation. Drug Metab Pharmacokinet 28: 475-484.
307. Nishimura M, Naito S. (2006). Tissue-specific mRNA expression profiles of human phase I metabolizing enzymes except for cytochrome P450 and phase II metabolizing enzymes. Drug Metab Pharmacokinet 21: 357-374.
308. Nishiyama T, Ogura K, Nakano H, et al. (2002). Reverse geometrical selectivity in glucuronidation and sulfation of cis- and trans-4-hydroxytamoxifens by human liver UDP-glucuronosyltransferases and sulfotransferases. Biochem Pharmacol 63: 1817-1830.
309. Nishiyama T, Ohnuma T, Inoue Y, et al. (2008). UDP-glucuronosyltransferases 1A6 and 1A10 catalyze reduced menadione glucuronidation. Biochem Biophys Res Commun 371: 247-250.
310. Nithipatikom K, Isbell MA, See WA, Campbell WB. (2006). Elevated 12- and 20-hydroxyeicosatetraenoic acid in urine of patients with prostatic diseases. Cancer Lett 233: 219-225.
311. O'Dwyer PJ, Catalano RB. (2006). Uridine diphosphate glucuronosyltransferase (UGT) 1A1 and irinotecan: Practical pharmacogenomics arrives in cancer therapy. J Clin Oncol 24: 4534-4538.
312. Oda S, Fukami T, Yokoi T, Nakajima M. (2013). Epigenetic regulation is a crucial factor in the repression of UGT1A1 expression in the human kidney. Drug Metab Dispos 41: 1738-1743.
313. Oda S, Fukami T, Yokoi T, Nakajima M. (2014). Epigenetic regulation of the tissue-specific expression of human UDP-glucuronosyltransferase (UGT) 1A10. Biochem Pharmacol 87: 660-667.
314. Oguri T, Takahashi T, Miyazaki M, et al. (2004). UGT1A10 is responsible for SN-38 glucuronidation and its expression in human lung cancers. Anticancer Res 24: 2893-2896.
315. Ohno A, Saito Y, Hanioka N, et al. (2004). Involvement of human hepatic UGT1A1, UGT2B4, and UGT2B7 in the glucuronidation of carvedilol. Drug Metab Dispos 32: 235-239.
316. Ohno S, Kawana K, Nakajin S. (2008). Contribution of UDP-glucuronosyltransferase 1A1 and 1A8 to morphine-6-glucuronidation and its kinetic properties. Drug Metab Dispos 36: 688-694.
317. Ohno S, Nakajin S. (2009). Determination of mRNA expression of human UDP-glucuronosyltransferases and application for localization in various human tissues by real-time reverse transcriptase-polymerase chain reaction. Drug Metab Dispos 37: 32-40.
318. Olsson M, Lindstrom S, Haggkvist B, et al. (2008). The UGT2B17 gene deletion is not associated with prostate cancer risk. Prostate 68: 571-575.
319. Orzechowski A, Schrenk D, Bock-Hennig BS, Bock KW. (1994). Glucuronidation of carcinogenic arylamines and their N-hydroxy derivatives by rat and human phenol UDP-glucuronosyltransferase of the UGT1 gene complex. Carcinogenesis 15: 1549-1553.
320. Ou Z, Huang M, Zhao L, Xie W. (2010). Use of transgenic mice in UDP-glucuronosyltransferase (UGT) studies. Drug Metab Rev 42: 123-131.
321. Park J, Chen L, Ratnashinge L, et al. (2006). Deletion polymorphism of UDP-glucuronosyltransferase 2B17 and risk of prostate cancer in African American and Caucasian men. Cancer Epidemiol Biomarkers Prev 15: 1473-1478.
322. Park J, Chen L, Shade K, Lazarus P, et al. (2004). Asp85tyr polymorphism in the udp-glucuronosyltransferase (UGT) 2B15 gene and the risk of prostate cancer. J Urol 171: 2484-2488.
323. Park JY, Tanner JP, Sellers TA, et al. (2007). Association between polymorphisms in HSD3B1 and UGT2B17 and prostate cancer risk. Urology 70: 374-379.
324. Patricia MK, Kim JA, Harper CM, et al. (1999). Lipoxygenase products increase monocyte adhesion to human aortic endothelial cells. Arterioscler Thromb Vasc Biol 19: 2615-2622.
325. Pawlowska M, Chu R, Fedejko-Kap B, et al. (2013). Metabolic transformation of antitumor acridinone C-1305 but not C-1311 via selective cellular expression of UGT1A10 increases cytotoxic response: Implications for clinical use. Drug Metab Dispos 41: 414-421.
326. Peck JD, Hulka BS, Poole C, et al. (2002). Steroid hormone levels during pregnancy and incidence of maternal breast cancer. Cancer Epidemiol Biomarkers Prev 11: 361-368.
327. Peer CJ, Sissung TM, Kim A, et al. (2012). Sorafenib is an inhibitor of UGT1A1 but is metabolized by UGT1A9: implications of genetic variants on pharmacokinetics and hyperbilirubinemia. Clin Cancer Res 18: 2099-2107.
328. Pellicciari R, Fiorucci S, Camaioni E, et al. (2002). 6-Alpha-ethylchenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J Med Chem 45: 3569-3572.
329. Pennell PB, Peng L, Newport DJ, et al. (2008). Lamotrigine in pregnancy: Clearance, therapeutic drug monitoring, and seizure frequency. Neurology 70: 2130-2136.
330. Picard N, Ratanasavanh D, Premaud A, et al. (2005). Identification of the UDP-glucuronosyltransferase isoforms involved in mycophenolic acid phase II metabolism. Drug Metab Dispos 33: 139-146.
331. Pillai S, Chellappan SP. (2009). ChIP on chip assays: Genome-wide analysis of transcription factor binding and histone modifications. Methods Mol Biol 523: 341-366.
332. Pillot T, Ouzzine M, Fournel-Gigleux S, et al. (1993). Glucuronidation of hyodeoxycholic acid in human liver. Evidence for a selective role of UDP-glucuronosyltransferase 2B4. J Biol Chem 268: 25636-25642.
333. Pineda Torra I, Claudel T, Duval C, et al. (2003). Bile acids induce the expression of the human peroxisome proliferator-activated receptor alpha gene via activation of the farnesoid X receptor. Mol Endocrinol 17: 259-272.
334. Pontoglio M, Barra J, Hadchouel M, et al. (1996). Hepatocyte nuclear factor 1 inactivation results in hepatic dysfunction, phenylketonuria, and renal Fanconi syndrome. Cell 84: 575-585.
335. Precht JC, Schroth W, Klein K, et al. (2013). The letrozole phase 1 metabolite carbinol as a novel probe drug for UGT2B7. Drug Metab Dispos 41: 1906-1913.
336. Prueksaritanont T, Subramanian R, Fang X, et al. (2002a). Glucuronidation of statins in animals and humans: A novel mechanism of statin lactonization. Drug Metab Dispos 30: 505-512.
337. Prueksaritanont T, Tang C, Qiu Y, et al. (2002b). Effects of fibrates on metabolism of statins in human hepatocytes. Drug Metab Dispos 30: 1280-1287.
338. Prueksaritanont T, Zhao JJ, Ma B, et al. (2002c). Mechanistic studies on metabolic interactions between gemfibrozil and statins. J Pharmacol Exp Ther 301: 1042-1051.
339. Quintana AM, Liu F, O'Rourke JP, Ness SA. (2011). Identification and regulation of c-Myb target genes in MCF-7 cells. BMC Cancer 11: 30.
340. Radominska-Pandya A, Little JM, Czernik PJ. (2001). Human UDP-glucuronosyltransferase 2B7. Curr Drug Metab 2: 283-298.
341. Radominska-Pandya A, Little JM, Pandya JT, et al. (1998). UDP-glucuronosyltransferases in human intestinal mucosa. Biochim Biophys Acta 1394: 199-208.
342. Radominska A, Little J, Pyrek JS, et al. (1993). A novel UDP-Glcspecific glucosyltransferase catalyzing the biosynthesis of 6-Oglucosides of bile acids in human liver microsomes. J Biol Chem 268: 15127-15135.
343. Rae JM, Johnson MD, Lippman ME, Flockhart DA. (2001). Rifampin is a selective, pleiotropic inducer of drug metabolism genes in human hepatocytes: Studies with cDNA and oligonucleotide expression arrays. J Pharmacol Exp Ther 299: 849-857.
344. Ramirez J, Iyer L, Journault K, et al. (2002). In vitro characterization of hepatic flavopiridol metabolism using human liver microsomes and recombinant UGT enzymes. Pharm Res 19: 588-594.
345. Ramirez J, Liu W, Mirkov S, et al. (2007). Lack of association between common polymorphisms in UGT1A9 and gene expression and activity. Drug Metab Dispos 35: 2149-2153.
346. Ramirez J, Mirkov S, Zhang W, et al. (2008). Hepatocyte nuclear factor- 1 alpha is associated with UGT1A1, UGT1A9 and UGT2B7 mRNA expression in human liver. Pharmacogenomics J 8: 152-161.
347. Raungrut P, Uchaipichat V, Elliot DJ, et al. (2010). In vitro-in vivo extrapolation predicts drug-drug interactions arising from inhibition of codeine glucuronidation by dextropropoxyphene, fluconazole, ketoconazole, and methadone in humans. J Pharmacol Exp Ther 334: 609-618.
348. Reilly KB, Srinivasan S, Hatley ME, et al. (2004). 12/15-Lipoxygenase activity mediates inflammatory monocyte/endothelial interactions and atherosclerosis in vivo. J Biol Chem 279: 9440-9450.
349. Ren Q, Murphy SE, Zheng Z, Lazarus P. (2000). O-Glucuronidation of the lung carcinogen 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol (NNAL) by human UDP-glucuronosyltransferases 2B7 and 1A9. Drug Metab Dispos 28: 1352-1360.
350. Ribas J, Ni X, Haffner M, et al. (2009). miR-21: An androgen receptorregulated microRNA that promotes hormone-dependent and hormoneindependent prostate cancer growth. Cancer Res 69: 7165-7169.
351. Ritter JK, Chen F, Sheen YY, Lubet RA, Owens IS. (1992a). Two human liver cDNAs encode UDP-glucuronosyltransferases with 2 log differences in activity toward parallel substrates including hyodeoxycholic acid and certain estrogen derivatives. Biochemistry 31: 3409-3414.
352. Ritter JK, Chen F, Sheen YY, et al. (1992b). A novel complex locus UGT1 encodes human bilirubin, phenol, and other UDP-glucuronosyltransferase isozymes with identical carboxyl termini. J Biol Chem 267: 3257-3261.
353. Ritter JK, Kessler FK, Thompson MT, et al. (1999). Expression and inducibility of the human bilirubin UDP-glucuronosyltransferase UGT1A1 in liver and cultured primary hepatocytes: Evidence for both genetic and environmental influences. Hepatology 30: 476-484.
354. Robinson JL, MacArthur S, Ross-Innes CS, et al. (2011). Androgen receptor driven transcription in molecular apocrine breast cancer is mediated by FoxA1. EMBO J 30: 3019-3027.
355. Ross GW, Abbott RD, Petrovitch H, et al. (2000). Association of coffee and caffeine intake with the risk of Parkinson disease. JAMA 283: 2674-2679.
356. Rouleau M, Collin P, Bellemare J, et al. (2013). Protein-protein interactions between the bilirubin-conjugating UDP-glucuronosyltransferase UGT1A1 and its shorter isoform 2 regulatory partner derived from alternative splicing. Biochem J 450: 107-114.
357. Rouleau M, Roberge J, Bellemare J, Guillemette C. (2014). Dual roles for splice variants of the glucuronidation pathway as regulators of cellular metabolism. Mol Pharmacol 85: 29-36.
358. Rowbotham SE, Illingworth NA, Daly AK, et al. (2010). Role of UDP-glucuronosyltransferase isoforms in 13-cis retinoic acid metabolism in humans. Drug Metab Dispos 38: 1211-1217.
359. Ruan JQ, Yan R. (2014). Regioselective glucuronidation of the isoflavone calycosin by human liver microsomes and recombinant human UDP-glucuronosyltransferases. Chem Biol Interact 220C: 231-240.
360. Rutzky LP, Kaye CI, Siciliano MJ, et al. (1980). Longitudinal karyotype and genetic signature analysis of cultured human colon adenocarcinoma cell lines LS180 and LS174T. Cancer Res 40: 1443-1448.
361. Sadeque AJ, Usmani KA, Palamar S, et al. (2012). Identification of human UDP-glucuronosyltransferases involved in N-carbamoyl glucuronidation of lorcaserin. Drug Metab Dispos 40: 772-778.
362. Sahi J, Grepper S, Smith C. (2010). Hepatocytes as a tool in drug metabolism, transport and safety evaluations in drug discovery. Curr Drug Discov Technol 7: 188-198.
363. Sakaguchi T, Gu X, Golden HM, et al. (2002). Cloning of the human claudin-2 5′-flanking region revealed a TATA-less promoter with conserved binding sites in mouse and human for caudal-related homeodomain proteins and hepatocyte nuclear factor-1alpha. J Biol Chem 277: 21361-21370.
364. Salazar-Martinez E, Willett WC, Ascherio A, et al. (2004). Coffee consumption and risk for type 2 diabetes mellitus. Ann Intern Med 140: 1-8.
365. Sato Y, Nagata M, Kawamura A, et al. (2012). Protein quantification of UDP-glucuronosyltransferases 1A1 and 2B7 in human liver microsomes by LC-MS/MS and correlation with glucuronidation activities. Xenobiotica 42: 823-829.
366. Sato Y, Nagata M, Tetsuka K, et al. (2014). Optimized methods for targeted peptide-based quantification of human uridine 5′-diphosphate-glucuronosyltransferases in biological specimens using liquid chromatography-tandem mass spectrometry. Drug Metab Dispos 42: 885-889.
367. Schaefer O, Ohtsuki S, Kawakami H, et al. (2012). Absolute quantification and differential expression of drug transporters, cytochrome P450 enzymes, and UDP-glucuronosyltransferases in cultured primary human hepatocytes. Drug Metab Dispos 40: 93-103.
368. Schebb NH, Franze B, Maul R, et al. (2012). In vitro glucuronidation of the antibacterial triclocarban and its oxidative metabolites. Drug Metab Dispos 40: 25-31.
369. Schwab N, Skopp G. (2014). Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem 406: 2325-2332.
370. Schwaninger AE, Meyer MR, Zapp J, Maurer HH. (2009). The role of human UDP-glucuronyltransferases on the formation of the methylenedioxymethamphetamine (ecstasy) phase II metabolites R- and S-3-methoxymethamphetamine 4-O-glucuronides. Drug Metab Dispos 37: 2212-2220.
371. Senekeo-Effenberger K, Chen S, Brace-Sinnokrak E, et al. (2007). Expression of the human UGT1 locus in transgenic mice by 4-chloro- 6-(2,3-xylidino)-2-pyrimidinylthioacetic acid (WY-14643) and implications on drug metabolism through peroxisome proliferator-activated receptor alpha activation. Drug Metab Dispos 35: 419-427.
372. Seo KA, Bae SK, Choi YK, et al. (2010). Metabolism of 10- and 4-hydroxymidazolam by glucuronide conjugation is largely mediated by UDP-glucuronosyltransferases 1A4, 2B4, and 2B7. Drug Metab Dispos 38: 2007-2013.
373. Seo KA, Kim HJ, Jeong ES, et al. (2014). In vitro assay of six UGT isoforms in human liver microsomes, using cocktails of probe substrates and LC-MS/MS. Drug Metab Dispos 42: 1803-1810.
374. Setlur SR, Chen CX, Hossain RR, et al. (2010). Genetic variation of genes involved in dihydrotestosterone metabolism and the risk of prostate cancer. Cancer Epidemiol Biomarkers Prev 19: 229-239.
375. Shen H, Zhang Y, Ding H, et al. (2008). Farnesoid X receptor induces GLUT4 expression through FXR response element in the GLUT4 promoter. Cell Physiol Biochem 22: 1-14.
376. Shen L, Wu LC, Sanlioglu S, et al. (1994). Structure and genetics of the partially duplicated gene RP located immediately upstream of the complement C4A and the C4B genes in the HLA class III region. Molecular cloning, exon-intron structure, composite retroposon, and breakpoint of gene duplication. J Biol Chem 269: 8466-8476.
377. Shimada Y, Imamura M, Wagata T, et al. (1992). Characterization of 21 newly established esophageal cancer cell lines. Cancer 69: 277-284.
378. Shindoh J, Kaseb A, Vauthey JN. (2013). Surgical strategy for liver cancers in the era of effective chemotherapy. Liver Cancer 2: 47-54.
379. Shiraga T, Yajima K, Suzuki K, et al. (2012a). Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine. Drug Metab Dispos 40: 276-282.
380. Shiraga T, Yajima K, Teragaki T, et al. (2012b). Identification of enzymes responsible for the N-oxidation of darexaban glucuronide, the pharmacologically active metabolite of darexaban, and the glucuronidation of darexaban N-oxides in human liver microsomes. Biol Pharm Bull 35: 413-421.
381. Shoda T, Fukuhara K, Goda Y, Okuda H. (2009). 4-Hydroxy-3-methoxymethamphetamine glucuronide as a phase II metabolite of 3,4-methylenedioxymethamphetamine: Enzyme-assisted synthesis and involvement of human hepatic uridine 50-diphosphate-glucuronosyltransferase 2B15 in the glucuronidation. Chem Pharm Bull (Tokyo) 57: 472-475.
382. Siller M, Anzenbacher P, Anzenbacherova E, et al. (2011). In vitro interaction of a novel neutrophil growth factor with human liver microsomal cytochromes P450 and the contribution of UDP-glucuronosyltransferases to its metabolism. Xenobiotica 41: 934-944.
383. Sivertsson L, Edebert I, Palmertz MP, et al. (2013). Induced CYP3A4 expression in confluent Huh7 hepatoma cells as a result of decreased cell proliferation and subsequent pregnane X receptor activation. Mol Pharmacol 83: 659-670.
384. Smith CM, Faucette SR, Wang H, Lecluyse EL. (2005). Modulation of UDP-glucuronosyltransferase 1A1 in primary human hepatocytes by prototypical inducers. J Biochem Mol Toxicol 19: 96-108.
385. Sneitz N, Vahermo M, Mosorin J, et al. (2013). Regiospecificity and stereospecificity of human UDP-glucuronosyltransferases in the glucuronidation of estriol, 16-epiestriol, 17-epiestriol, and 13-epiestradiol. Drug Metab Dispos 41: 582-591.
386. Soars MG, Petullo DM, Eckstein JA, et al. (2004). An assessment of UDP-glucuronosyltransferase induction using primary human hepatocytes. Drug Metab Dispos 32: 140-148.
387. Soule HD, Vazguez J, Long A, et al. (1973). A human cell line from a pleural effusion derived from a breast carcinoma. J Natl Cancer Inst 51: 1409-1416.
388. Sridar C, Hanna I, Hollenberg PF. (2013). Quantitation of UGT1A1 in human liver microsomes using stable isotope-labelled peptides and mass spectrometry based proteomic approaches. Xenobiotica 43: 336-345.
389. Starlard-Davenport A, Lyn-Cook B, Radominska-Pandya A. (2008a). Identification of UDP-glucuronosyltransferase 1A10 in non-malignant and malignant human breast tissues. Steroids 73: 611-620.
390. Starlard-Davenport A, Lyn-Cook B, Radominska-Pandya A. (2008b). Novel identification of UDP-glucuronosyltransferase 1A10 as an estrogen-regulated target gene. Steroids 73: 139-147.
391. Starlard-Davenport A, Xiong Y, Bratton S, et al. (2007). Phenylalanine(90) and phenylalanine(93) are crucial amino acids within the estrogen binding site of the human UDP-glucuronosyltransferase 1A10. Steroids 72: 85-94.
392. Sten T, Qvisen S, Uutela P, et al. (2006). Prominent but reverse stereoselectivity in propranolol glucuronidation by human UDP-glucuronosyltransferases 1A9 and 1A10. Drug Metab Dispos 34: 1488-1494.
393. Strahm E, Sjoberg U, Garle M, et al. (2013). Implication of human UGT2B7, 2B15, and 2B17 in 19-norandrosterone metabolism. Front Endocrinol (Lausanne) 4: 75.
394. Strassburg CP, Kneip S, Topp J, et al. (2000). Polymorphic gene regulation and interindividual variation of UDP-glucuronosyltransferase activity in human small intestine. J Biol Chem 275: 36164-36171.
395. Strassburg CP, Manns MP, Tukey RH. (1998a). Expression of the UDP-glucuronosyltransferase 1A locus in human colon. Identification and characterization of the novel extrahepatic UGT1A8. J Biol Chem 273: 8719-8726.
396. Strassburg CP, Nguyen N, Manns MP, Tukey RH. (1998b). Polymorphic expression of the UDP-glucuronosyltransferase UGT1A gene locus in human gastric epithelium. Mol Pharmacol 54: 647-654.
397. Strassburg CP, Nguyen N, Manns MP, Tukey RH. (1999a). UDP-glucuronosyltransferase activity in human liver and colon. Gastroenterology 116: 149-160.
398. Strassburg CP, Oldhafer K, Manns MP, Tukey RH. (1997). 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: 212-220.
399. Strassburg CP, Strassburg A, Nguyen N, et al. (1999b). Regulation and function of family 1 and family 2 UDP-glucuronosyltransferase genes (UGT1A, UGT2B) in human oesophagus. Biochem J 338: 489-498.
400. Stringer F, Scott G, Valbuena M, et al. (2013). The effect of genetic polymorphisms in UGT2B15 on the pharmacokinetic profile of sipoglitazar, a novel anti-diabetic agent. Eur J Clin Pharmacol 69: 423-430.
401. Sugatani J. (2013). Function, genetic polymorphism, and transcriptional regulation of human UDP-glucuronosyltransferase (UGT) 1A1. Drug Metab Pharmacokinet 28: 83-92.
402. Sugatani J, Kojima H, Ueda A, et al. (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.
403. Sugatani J, Nishitani S, Yamakawa K, et al. (2005). Transcriptional regulation of human UGT1A1 gene expression: activated glucocorticoid receptor enhances constitutive androstane receptor/pregnane X receptor-mediated UDP-glucuronosyltransferase 1A1 regulation with glucocorticoid receptor-interacting protein 1. Mol Pharmacol 67: 845-855.
404. Sugatani J, Yamakawa K, Tonda E, et al. (2004). The induction of human UDP-glucuronosyltransferase 1A1 mediated through a distal enhancer module by flavonoids and xenobiotics. Biochem Pharmacol 67: 989-1000.
405. Sugatani J, Yamakawa K, Yoshinari K, et al. (2002). Identification of a defect in the UGT1A1 gene promoter and its association with hyperbilirubinemia. Biochem Biophys Res Commun 292: 492-497.
406. Suh E, Traber PG. (1996). An intestine-specific homeobox gene regulates proliferation and differentiation. Mol Cell Biol 16: 619-625.
407. Sun C, Southard C, Witonsky DB, et al. (2010a). Allelic imbalance (AI) identifies novel tissue-specific cis-regulatory variation for human UGT2B15. Hum Mutat 31: 99-107.
408. Sun D, Chen G, Dellinger RW, et al. (2006). Characterization of tamoxifen and 4-hydroxytamoxifen glucuronidation by human UGT1A4 variants. Breast Cancer Res 8: R50.
409. Sun D, Chen G, Dellinger RW, et al. (2010b). Characterization of 17-dihydroexemestane glucuronidation: Potential role of the UGT2B17 deletion in exemestane pharmacogenetics. Pharmacogenet Genomics 20: 575-585.
410. Sun D, Jones NR, Manni A, Lazarus P. (2013). Characterization of raloxifene glucuronidation: Potential role of UGT1A8 genotype on raloxifene metabolism in vivo. Cancer Prev Res (Phila) 6: 719-730.
411. Takahashi Y, Nakayama K, Itoh S, Kamataki T. (1997). Upstream stimulatory factor 1 (USF1) suppresses induction of CYP1A1 mRNA by 3-methylcholanthrene (MC) in HepG2 cells. Biochem Biophys Res Commun 240: 293-297.
412. Takayama K, Kaneshiro K, Tsutsumi S, et al. (2007). Identification of novel androgen response genes in prostate cancer cells by coupling chromatin immunoprecipitation and genomic microarray analysis. Oncogene 26: 4453-4463.
413. Takekuma Y, Takenaka T, Yamazaki K, et al. (2007). Stereoselective metabolism of racemic carvedilol by UGT1A1 and UGT2B7, and effects of mutation of these enzymes on glucuronidation activity. Biol Pharm Bull 30: 2146-2153.
414. Takenaga N, Ishii M, Kamei T, Yasumori T. (2002). Structure-activity relationship in O-glucuronidation of indolocarbazole analogs. Drug Metab Dispos 30: 494-497.
415. Tchernof A, Levesque E, Beaulieu M, et al. (1999). Expression of the androgen metabolizing enzyme UGT2B15 in adipose tissue and relative expression measurement using a competitive RT-PCR method. Clin Endocrinol (Oxf) 50: 637-642.
416. Tirona RG. (2011). Molecular mechanisms of drug transporter regulation. Handb Exp Pharmacol 201: 373-402.
417. Togawa H, Shinkai S, Mizutani T. (2008). Induction of human UGT1A1 by bilirubin through AhR dependent pathway. Drug Metab Lett 2: 231-237.
418. Toide K, Takahashi Y, Yamazaki H, et al. (2002). Hepatocyte nuclear factor-1alpha is a causal factor responsible for interindividual differences in the expression of UDP-glucuronosyltransferase 2B7 mRNA in human livers. Drug Metab Dispos 30: 613-615.
419. Tom BH, Rutzky LP, Oyasu R, et al. (1977). Human colon adenocarcinoma cells. II. Tumorigenic and organoid expression in vivo and in vitro. J Natl Cancer Inst 58: 1507-1512.
420. Tricker AR. (2003). Nicotine metabolism, human drug metabolism polymorphisms, and smoking behaviour. Toxicology 183: 151-173.
421. Troelsen JT, Mitchelmore C, Spodsberg N, et al. (1997). Regulation of lactase-phlorizin hydrolase gene expression by the caudal-related homoeodomain protein Cdx-2. Biochem J 322: 833-888.
422. Trottier J, Verreault M, Grepper S, et al. (2006). Human UDP-glucuronosyltransferase (UGT)1A3 enzyme conjugates chenodeoxycholic acid in the liver. Hepatology 44: 1158-1170.
423. Tulchinsky D, Hobel CJ, Yeager E, Marshall JR. (1972). Plasma estrone, estradiol, estriol, progesterone, and 17-hydroxyprogesterone in human pregnancy. I. Normal pregnancy. Am J Obstet Gynecol 112: 1095-1100.
424. Turgeon D, Carrier JS, Chouinard S, Belanger A. (2003a). Glucuronidation activity of the UGT2B17 enzyme toward xenobiotics. Drug Metab Dispos 31: 670-676.
425. Turgeon D, Carrier JS, Levesque E, et al. (2000). Isolation and characterization of the human UGT2B15 gene, localized within a cluster of UGT2B genes and pseudogenes on chromosome 4. J Mol Biol 295: 489-504.
426. Turgeon D, Carrier JS, Levesque E, et al. (2001). Relative enzymatic activity, protein stability, and tissue distribution of human steroidmetabolizing UGT2B subfamily members. Endocrinology 142: 778-787.
427. Turgeon D, Chouinard S, Belanger P, et al. (2003b). Glucuronidation of arachidonic and linoleic acid metabolites by human UDP-glucuronosyltransferases. J Lipid Res 44: 1182-1191.
428. Uchaipichat V, Suthisisang C, Miners JO. (2013). The glucuronidation of R- and S-lorazepam: Human liver microsomal kinetics, UDP-glucuronosyltransferase enzyme selectivity, and inhibition by drugs. Drug Metab Dispos 41: 1273-1284.
429. Usui T, Kuno T, Ueyama H, et al. (2006). Proximal HNF1 element is essential for the induction of human UDP-glucuronosyltransferase 1A1 by glucocorticoid receptor. Biochem Pharmacol 71: 693-701.
430. Veldscholte J, Berrevoets CA, Ris-Stalpers C, et al. (1992). The androgen receptor in LNCaP cells contains a mutation in the ligand binding domain which affects steroid binding characteristics and response to antiandrogens. J Steroid Biochem Mol Biol 41: 665-669.
431. Veldscholte J, Ris-Stalpers C, Kuiper GG, et al. (1990a). A mutation in the ligand binding domain of the androgen receptor of human LNCaP cells affects steroid binding characteristics and response to antiandrogens. Biochem Biophys Res Commun 173: 534-540.
432. Veldscholte J, Voorhorst-Ogink MM, Bolt-De Vries J, et al. (1990b). Unusual specificity of the androgen receptor in the human prostate tumor cell line LNCaP: High affinity for progestagenic and estrogenic steroids. Biochim Biophys Acta 1052: 187-194.
433. Verreault M, Kaeding J, Caron P, et al. (2010). Regulation of endobiotics glucuronidation by ligand-activated transcription factors: Physiological function and therapeutic potential. Drug Metab Rev 42: 110-122.
434. Verreault M, Senekeo-Effenberger K, Trottier J, et al. (2006). The liver X-receptor alpha controls hepatic expression of the human bile acidglucuronidating UGT1A3 enzyme in human cells and transgenic mice. Hepatology 44: 368-378.
435. Vogel A, Ockenga J, Ehmer U, et al. (2002). Polymorphisms of the carcinogen detoxifying UDP-glucuronosyltransferase UGT1A7 in proximal digestive tract cancer. Z Gastroenterol 40: 497-502.
436. Vyhlidal CA, Rogan PK, Leeder JS. (2004). Development and refinement of pregnane X receptor (PXR) DNA binding site model using information theory: Insights into PXR-mediated gene regulation. J Biol Chem 279: 46779-46786.
437. Wang H, Xing J, Grover D, et al. (2005). SVA elements: A hominidspecific retroposon family. J Mol Biol 354: 994-1007.
438. Wang J, Zhuang J, Iyer S, et al. (2012). Sequence features and chromatin structure around the genomic regions bound by 119 human transcription factors. Genome Res 22: 1798-1812.
439. Wang J, Zhuang J, Iyer S, et al. (2013). Factorbook.org: A Wiki-based database for transcription factor-binding data generated by the ENCODE consortium. Nucleic Acids Res 41: D171-D176.
440. Wang Z, Wong T, Hashizume T, et al. (2014). Human UGT1A4 and UGT1A3 conjugate 25-hydroxyvitamin D3: Metabolite structure, kinetics, inducibility, and interindividual variability. Endocrinology 155: 2052-2063.
441. Watanabe Y, Nakajima M, Ohashi N, et al. (2003). Glucuronidation of etoposide in human liver microsomes is specifically catalyzed by UDP-glucuronosyltransferase 1A1. Drug Metab Dispos 31: 589-595.
442. Watanabe Y, Nakajima M, Yokoi T. (2002). Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos 30: 1462-1469.
443. Wiener D, Doerge DR, Fang JL, et al. (2004). Characterization of N-glucuronidation of the lung carcinogen 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol (NNAL) in human liver: Importance of UDP-glucuronosyltransferase 1A4. Drug Metab Dispos 32: 72-79.
444. Wilson III W, Pardo-Manuel de Villena F, Lyn-Cook BD, et al. (2004). Characterization of a common deletion polymorphism of the UGT2B17 gene linked to UGT2B15. Genomics 84: 707-714.
445. Wittkopp PJ, Kalay G. (2012). Cis-regulatory elements: Molecular mechanisms and evolutionary processes underlying divergence. Nat Rev Genet 13: 59-69.
446. Wu B, Xu B, Hu M. (2011). Regioselective glucuronidation of flavonols by six human UGT1A isoforms. Pharm Res 28: 1905-1918.
447. Xia YL, Liang SC, Zhu LL, et al. (2014). Identification and characterization of human UDP-glucuronosyltransferases responsible for the glucuronidation of fraxetin. Drug Metab Pharmacokinet 29: 135-140.
448. Xie S, Chen Y, Chen S, Zeng S. (2011). Structure-metabolism relationships for the glucuronidation of flavonoids by UGT1A3 and UGT1A9. J Pharm Pharmacol 63: 297-304.
449. Xie W, Yeuh MF, Radominska-Pandya A, et al. (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.
450. Yamanaka H, Nakajima M, Katoh M, et al. (2004). A novel polymorphism in the promoter region of human UGT1A9 gene (UGT1A9∗22) and its effects on the transcriptional activity. Pharmacogenetics 14: 329-332.
451. Yamanaka H, Nakajima M, Katoh M, et al. (2005). Trans-3′- hydroxycotinine O- and N-glucuronidations in human liver microsomes. Drug Metab Dispos 33: 23-30.
452. Yamanaka H, Nakajima M, Katoh M, Yokoi T. (2007). Glucuronidation of thyroxine in human liver, jejunum, and kidney microsomes. Drug Metab Dispos 35: 1642-1648.
453. Yasar U, Greenblatt DJ, Guillemette C, Court MH. (2013). Evidence for regulation of UDP-glucuronosyltransferase (UGT) 1A1 protein expression and activity via DNA methylation in healthy human livers. J Pharm Pharmacol 65: 874-883.
454. Yoder Graber AL, Ramirez J, Innocenti F, Ratain MJ. (2007). UGT1A1∗28 genotype affects the in vitro glucuronidation of thyroxine in human livers. Pharmacogenet Genomics 17: 619-627.
455. Yoshigae Y, Konno K, Takasaki W, Ikeda T. (2000). Characterization of UDP-glucuronosyltransferases (UGTS) involved in the metabolism of troglitazone in rats and humans. J Toxicol Sci 25: 433-441.
456. Yueh MF, Huang YH, Hiller A, et al. (2003). Involvement of the xenobiotic response element (XRE) in Ah receptor-mediated induction of human UDP-glucuronosyltransferase 1A1. J Biol Chem 278: 15001-15006.
457. Yueh MF, Mellon PL, Tukey RH. (2011). Inhibition of human UGT2B7 gene expression in transgenic mice by the constitutive androstane receptor. Mol Pharmacol 79: 1053-1060.
458. Yueh MF, Nguyen N, Famourzadeh M, et al. (2001). The contribution of UDP-glucuronosyltransferase 1A9 on CYP1A2-mediated genotoxicity by aromatic and heterocyclic amines. Carcinogenesis 22: 943-950.
459. Yueh MF, Tukey RH. (2007). Nrf2-Keap1 signaling pathway regulates human UGT1A1 expression in vitro and in transgenic UGT1 mice. J Biol Chem 282: 8749-8758.
460. Zanelli U, Caradonna NP, Hallifax D, et al. (2012). Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs. Drug Metab Dispos 40: 104-110.
461. Zanger UM, Schwab M. (2013). Cytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation. Pharmacol Ther 138: 103-141.
462. Zaret K. (1999). Developmental competence of the gut endoderm: Genetic potentiation by GATA and HNF3/fork head proteins. Dev Biol 209: 1-10.
463. Zhang H, Soikkeli A, Tolonen A, et al. (2012). Highly variable pH effects on the interaction of diclofenac and indomethacin with human UDP-glucuronosyltransferases. Toxicol In Vitro 26: 1286-1293.
464. Zhang JY, Zhan J, Cook CS, et al. (2003). Involvement of human UGT2B7 and 2B15 in rofecoxib metabolism. Drug Metab Dispos 31: 652-658.
465. Zheng Z, Fang JL, Lazarus P. (2002). Glucuronidation: An important mechanism for detoxification of benzo[a]pyrene metabolites in aerodigestive tract tissues. Drug Metab Dispos 30: 397-403.
466. Zheng Z, Park JY, Guillemette C, et al. (2001). Tobacco carcinogen-detoxifying enzyme UGT1A7 and its association with orolaryngeal cancer risk. J Natl Cancer Inst 93: 1411-1418.
467. Zhou D, Guo J, Linnenbach AJ, et al. (2010a). Role of human UGT2B10 in N-glucuronidation of tricyclic antidepressants, amitriptyline, imipramine, clomipramine, and trimipramine. Drug Metab Dispos 38: 863-870.
468. Zhou J, Tracy TS, Remmel RP. (2010b). Glucuronidation of dihydrotestosterone and trans-androsterone by recombinant UDP-glucuronosyltransferase (UGT) 1A4: Evidence for multiple UGT1A4 aglycone binding sites. Drug Metab Dispos 38: 431-440.
469. Zhu AZ, Zhou Q, Cox LS, et al. (2013). Variation in trans-3′- hydroxycotinine glucuronidation does not alter the nicotine metabolite ratio or nicotine intake. PLoS One 8: e70938.
470. Zielinska A, Lichti CF, Bratton S, et al. (2008). Glucuronidation of monohydroxylated warfarin metabolites by human liver microsomes and human recombinant UDP-glucuronosyltransferases. J Pharmacol Exp Ther 324: 139-148.