UGT1A6

Summary

Gene Symbol: UGT1A6
Description: UDP glucuronosyltransferase 1 family, polypeptide A6
Alias: GNT1, HLUGP, HLUGP1, UDPGT, UDPGT 1-6, UGT1, UGT1A6S, UGT1F, UDP glycosyltransferase 1 family, polypeptide A6, UDP-glucuronosyltransferase 1 family polypeptide A6s, UDP-glucuronosyltransferase 1-6, UDP-glucuronosyltransferase 1-F, UDP-glucuronosyltransferase 1A6, UGT-1F, UGT1*6, UGT1-06, UGT1.6, phenol-metabolizing UDP-glucuronosyltransferase
Species: human

Top Publications

  1. ncbi Extrahepatic expression of NAD(P)H:menadione oxidoreductase, UDP glucuronosyltransferase-1A6, microsomal aldehyde dehydrogenase, and hepatic nuclear factor-1 alpha mRNAs in ch/ch and 14CoS/14CoS mice
    V Vasiliou
    Center for Environmental Genetics, University of Cincinnati Medical Center, Ohio 45267 0056, USA
    Biochem Biophys Res Commun 233:631-6. 1997
  2. ncbi Nuclear UDP-glucuronosyltransferases: identification of UGT2B7 and UGT1A6 in human liver nuclear membranes
    Anna Radominska-Pandya
    Department of Biochemistry and Molecular Biology, University of Arkansas for Medical Sciences, Little Rock, Arkansas, 77205, USA
    Arch Biochem Biophys 399:37-48. 2002
  3. ncbi Decrease in serum thyroxine level by phenobarbital in rats is not necessarily dependent on increase in hepatic UDP-glucuronosyltransferase
    Yoshihisa Kato
    School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan
    Drug Metab Dispos 33:1608-12. 2005
  4. ncbi Hepatic biotransformation responses in Atlantic salmon exposed to retinoic acids and 3,3',4,4'-tetrachlorobiphenyl (PCB congener 77)
    Augustine Arukwe
    Department of Biology, Norwegian University of Science and Technology NTNU, Høyskoleringen 5, 7491 Trondheim, Norway
    Comp Biochem Physiol C Toxicol Pharmacol 147:470-82. 2008
  5. ncbi Interactions between human UDP-glucuronosyltransferase (UGT) 2B7 and UGT1A enzymes
    Ryoichi Fujiwara
    Drug Metabolism and Toxicology, Faculty of Pharmaceutical Sciences, Kanazawa University, Kakuma machi, Kanazawa 920 1192, Japan
    J Pharm Sci 99:442-54. 2010
  6. ncbi Genome-wide association meta-analysis for total serum bilirubin levels
    Andrew D Johnson
    National Heart Lung and Blood Institute s The Framingham Heart Study, 73 Mt Wayte Avenue, Suite 2, Framingham, MA 01702, USA
    Hum Mol Genet 18:2700-10. 2009
  7. ncbi Common variants in the SLCO1B3 locus are associated with bilirubin levels and unconjugated hyperbilirubinemia
    Serena Sanna
    Istituto di Neurogenetica e Neurofarmacologia del Consiglio Nazionale delle Ricerche, Monserrato, 09042 Cagliari, Italy
    Hum Mol Genet 18:2711-8. 2009
  8. ncbi UGT1A1, UGT1A6 and UGT1A7 genetic analysis: repercussion for irinotecan pharmacogenetics in the São Miguel Island Population (Azores, Portugal)
    Paula R Pacheco
    Molecular Genetics and Pathology Unit, Hospital of Divino Espirito Santo of Ponta Delgada, São Miguel Island, Azores, Portugal
    Mol Diagn Ther 13:261-8. 2009
  9. ncbi Cloning of two human liver bilirubin UDP-glucuronosyltransferase cDNAs with expression in COS-1 cells
    J K Ritter
    Section on Genetic Disorders of Drug Metabolism, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20892
    J Biol Chem 266:1043-7. 1991
  10. ncbi Human UDP-glucuronosyltransferases: metabolism, expression, and disease
    R H Tukey
    Department of Chemistry and Biochemistry, Cancer Center, University of California, San Diego, La Jolla 92093, USA
    Annu Rev Pharmacol Toxicol 40:581-616. 2000

Research Grants

  1. Inflamation and the Risk of Endometrial Cancer
    Akila Viswanathan; Fiscal Year: 2007
  2. Metabolism and Toxicity of Acetaminophen in Preterm Infants
    JOHANNES NICOLAAS VAN DEN ANKER; Fiscal Year: 2010
  3. Synthesis of Conjugated Metabolites of Buprenophine
    Shixia Feng; Fiscal Year: 2002
  4. STUDIES ON UDP-GLUCURONOSYLTRANSFERASES
    Thomas Tephly; Fiscal Year: 1993
  5. UDP-GLUCURONYLTRANSFERASES
    Thomas Tephly; Fiscal Year: 1990
  6. Drug Metabolism and Chronic Liver Disease
    Robert Branch; Fiscal Year: 2005
  7. Pharmacoepidemiology and Pharmacogenetics of a Statin AE
    Bruce Psaty; Fiscal Year: 2007
  8. Aspirin, UGT1A6 Genotype, and Colon Gene Expression
    Johanna Lampe; Fiscal Year: 2006
  9. PROTECTION AGAINST BENZO{A} PYRENE TOXICITY BY OLTIPRAZ
    JOSEPH RITTER; Fiscal Year: 2004
  10. UDP GLUCURONOSYLTRANSFERASES IN PHARMACOLOGY
    Thomas Tephly; Fiscal Year: 2002

Detail Information

Publications166 found, 100 shown here

  1. ncbi Extrahepatic expression of NAD(P)H:menadione oxidoreductase, UDP glucuronosyltransferase-1A6, microsomal aldehyde dehydrogenase, and hepatic nuclear factor-1 alpha mRNAs in ch/ch and 14CoS/14CoS mice
    V Vasiliou
    Center for Environmental Genetics, University of Cincinnati Medical Center, Ohio 45267 0056, USA
    Biochem Biophys Res Commun 233:631-6. 1997
    ..by ROM-mediated oxidative stress: NAD(P)H:menadione oxidoreductase (Nmo1) and UDP glucuronosyltransferase-1A6 (Ugt1a6)...
  2. ncbi Nuclear UDP-glucuronosyltransferases: identification of UGT2B7 and UGT1A6 in human liver nuclear membranes
    Anna Radominska-Pandya
    Department of Biochemistry and Molecular Biology, University of Arkansas for Medical Sciences, Little Rock, Arkansas, 77205, USA
    Arch Biochem Biophys 399:37-48. 2002
    We have demonstrated the subcellular localization of the human UDP-glucuronosyltransferases (UGTs), UGT2B7 and UGT1A6, in endoplasmic reticulum (ER) and nuclear membrane from human hepatocytes and cell lines, by in situ immunostaining and ..
  3. ncbi Decrease in serum thyroxine level by phenobarbital in rats is not necessarily dependent on increase in hepatic UDP-glucuronosyltransferase
    Yoshihisa Kato
    School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan
    Drug Metab Dispos 33:1608-12. 2005
    ..that there is a poor correlation between increase in the levels of UDP-glucuronosyltransferases, UGT1A1 and UGT1A6, and decrease in the levels of serum total thyroxine (T4) and free T4 in phenobarbital (PB)-treated rats, although ..
  4. ncbi Hepatic biotransformation responses in Atlantic salmon exposed to retinoic acids and 3,3',4,4'-tetrachlorobiphenyl (PCB congener 77)
    Augustine Arukwe
    Department of Biology, Norwegian University of Science and Technology NTNU, Høyskoleringen 5, 7491 Trondheim, Norway
    Comp Biochem Physiol C Toxicol Pharmacol 147:470-82. 2008
    ..Liver samples collected from all exposure groups were analyzed for gene (RARalpha, AhR2alpha, AhR2beta, CYP1A1, UGT1 and GSTpi) expression using real-time PCR and activity (7-ethoxyresorufin O-deethylase (EROD), UGT and GST) using ..
  5. ncbi Interactions between human UDP-glucuronosyltransferase (UGT) 2B7 and UGT1A enzymes
    Ryoichi Fujiwara
    Drug Metabolism and Toxicology, Faculty of Pharmaceutical Sciences, Kanazawa University, Kakuma machi, Kanazawa 920 1192, Japan
    J Pharm Sci 99:442-54. 2010
    ..activities were investigated using double expression systems in HEK293 cells (UGT2B7/UGT1A1, UGT2B7/UGT1A4, UGT2B7/UGT1A6, and UGT2B7/UGT1A9). Native-PAGE analysis clearly revealed that UGT2B7 forms homo-oligomers...
  6. ncbi Genome-wide association meta-analysis for total serum bilirubin levels
    Andrew D Johnson
    National Heart Lung and Blood Institute s The Framingham Heart Study, 73 Mt Wayte Avenue, Suite 2, Framingham, MA 01702, USA
    Hum Mol Genet 18:2700-10. 2009
    ..In analyses for association with gallbladder disease or gallstones, top bilirubin SNPs in UGT1A1 and SLCO1B1 were not associated...
  7. ncbi Common variants in the SLCO1B3 locus are associated with bilirubin levels and unconjugated hyperbilirubinemia
    Serena Sanna
    Istituto di Neurogenetica e Neurofarmacologia del Consiglio Nazionale delle Ricerche, Monserrato, 09042 Cagliari, Italy
    Hum Mol Genet 18:2711-8. 2009
    ..Thus, SLC01B3 appears to be involved in the regulation of serum bilirubin levels in healthy individuals and in some bilirubin-related disorders that are only partially explained by other known gene variants...
  8. ncbi UGT1A1, UGT1A6 and UGT1A7 genetic analysis: repercussion for irinotecan pharmacogenetics in the São Miguel Island Population (Azores, Portugal)
    Paula R Pacheco
    Molecular Genetics and Pathology Unit, Hospital of Divino Espirito Santo of Ponta Delgada, São Miguel Island, Azores, Portugal
    Mol Diagn Ther 13:261-8. 2009
    ..UGT1A proteins have been implicated as risk factors for both the development of cancer and adverse drug effects...
  9. ncbi Cloning of two human liver bilirubin UDP-glucuronosyltransferase cDNAs with expression in COS-1 cells
    J K Ritter
    Section on Genetic Disorders of Drug Metabolism, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20892
    J Biol Chem 266:1043-7. 1991
    ..These cDNAs which encode functional bilirubin UDP-glucuronosyltransferases will allow the isolation of an appropriate gene to develop a gene therapy model for patients which have the totally deficient trait...
  10. ncbi Human UDP-glucuronosyltransferases: metabolism, expression, and disease
    R H Tukey
    Department of Chemistry and Biochemistry, Cancer Center, University of California, San Diego, La Jolla 92093, USA
    Annu Rev Pharmacol Toxicol 40:581-616. 2000
    ..The role of the UGTs in metabolism and different disease states in humans is the topic of this review...
  11. ncbi Frequent co-occurrence of the TATA box mutation associated with Gilbert's syndrome (UGT1A1*28) with other polymorphisms of the UDP-glucuronosyltransferase-1 locus (UGT1A6*2 and UGT1A7*3) in Caucasians and Egyptians
    Christoph Kohle
    Institute of Pharmacology and Toxicology, University of Tubingen, Tubingen, Germany
    Biochem Pharmacol 65:1521-7. 2003
    ..Furthermore, co-occurrence of UGT1A1*28 and UGT1A6*2 has been observed...
  12. ncbi Effects of genetic polymorphisms in metabolic enzymes on the relationships between 8-hydroxydeoxyguanosine levels in human leukocytes and urinary 1-hydroxypyrene and 2-naphthol concentrations
    Yong Dae Kim
    Department of Preventive Medicine, College of Medicine, Chungbuk National University, South Korea
    J Occup Health 45:160-7. 2003
    ..and to evaluate the effects of cigarette smoking and the genetic polymorphisms of CYP1A1, CYP2E1, GSTM1, NAT2 and UGT1A6 on the relationship...
  13. ncbi Triiodothyronine and estradiol increase the serum level of androstanediol glucuronide but do not influence androgen UDP-glucuronyl transferase activity in the female rat
    E C Pirog
    VA Medical Center, Lexington, Kentucky
    Horm Metab Res 26:226-8. 1994
    ..07 nmol/l) in the control and the estradiol and T3 treatment groups. Androgen UDPGT activity in liver microsomes was not altered by treatment with testosterone, estradiol or T3...
  14. ncbi A possible mechanism for decrease in serum thyroxine level by polychlorinated biphenyls in Wistar and Gunn rats
    Yoshihisa Kato
    School of Pharmaceutical Sciences, COE Program in the 21st Century, University of Shizuoka, 52 1, Yada, Shizuoka 422 8526, Japan
    Toxicol Sci 81:309-15. 2004
    ..the PCB-induced decrease in rats is generally thought to occur through induction of T(4)-UDP-GT, UGT1A1, and UGT1A6. In the present study, to further clarify the relationship between the decrease in serum T(4) level and the ..
  15. ncbi Imipramine N-glucuronidation in human liver microsomes: biphasic kinetics and characterization of UDP-glucuronosyltransferase isoforms
    Miki Nakajima
    Division of Drug Metabolism, Faculty of Pharmaceutical Sciences, Kanazawa University, Kanazawa, Japan
    Drug Metab Dispos 30:636-42. 2002
    ..Supersomes or Bacurosomes) or human B-lymphoblastoid cells tested in the present study (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A7, UGT1A8, UGT1A9, UGT1A10, UGT2B7, and UGT2B15), only UGT1A4 showed imipramine N-glucuronosyltransferase ..
  16. ncbi Androgen UDP-glucuronyl transferase activity is found primarily in liver in the rat
    E C Pirog
    VA Medical Center, Lexington, Kentucky
    J Androl 14:2-8. 1993
    UDP-glucuronyl transferase (UDPGT) activity was determined for androgens in tissue minces and microsomal fractions from the liver and extrahepatic tissues (kidney, skin, prostate, and preputial glands) of the male rat...
  17. ncbi An internal signal sequence mediates the targeting and retention of the human UDP-glucuronosyltransferase 1A6 to the endoplasmic reticulum
    M Ouzzine
    UMR CNRS 7561 Université Henri Poincaré Nancy 1, Faculte de Medecine, BP 184, 54505 Vanduvre lès Nancy, France
    J Biol Chem 274:31401-9. 1999
    The human UDP-glucuronosyltransferase isoform UGT1A6 is predicted to be a type I transmembrane protein anchored in the endoplasmic reticulum by a single C-terminal transmembrane domain, followed by a short cytoplasmic tail...
  18. ncbi Piscine UDP-glucuronosyltransferase 1B
    Michael J Leaver
    Institute of Aquaculture, University of Stirling, Stirling FK9 4LA, UK
    Aquat Toxicol 84:356-65. 2007
    ..The deduced amino acid sequences share greater similarity with mammalian UGT1 family genes than UGT2 genes (44-47% and 39-40% amino acid identity, respectively) and have been designated UGT1B...
  19. ncbi The 3-methylcholanthrene-inducible UDP-glucuronosyltransferase deficiency in the hyperbilirubinemic rat (Gunn rat) is caused by a -1 frameshift mutation
    T Iyanagi
    Division of Biochemistry, University of Tsukuba, Ibaraki, Japan
    J Biol Chem 264:21302-7. 1989
    ..rat which has unconjugated hyperbilirubinemia as a result of the absence of hepatic UDP-glucuronosyltransferase (UDPGT) activity toward bilirubin...
  20. ncbi Identification of a genetic alteration in the code for bilirubin UDP-glucuronosyltransferase in the UGT1 gene complex of a Crigler-Najjar type I patient
    J K Ritter
    Human Genetics Branch, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20892
    J Clin Invest 90:150-5. 1992
    ..K., J. M. Crawford, and I. S. Owens. 1991. J. Biol. Chem. 266:1043-1047) led to the discovery of a unique locus, UGT1, which encodes a family of UDP-glucuronosyltransferase isozymes, including the two bilirubin forms (Ritter, J. K...
  21. ncbi Influence of N-terminal domain histidine and proline residues on the substrate selectivities of human UDP-glucuronosyltransferase 1A1, 1A6, 1A9, 2B7, and 2B10
    Oranun Kerdpin
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Drug Metab Dispos 37:1948-55. 2009
    ..The conserved N-terminal domain histidine of UGT1A1, UGT1A6, UGT1A9, and UGT2B7 was mutated to proline and leucine 34 of UGT2B10 was substituted with histidine, and the ..
  22. ncbi Identification of aspartic acid and histidine residues mediating the reaction mechanism and the substrate specificity of the human UDP-glucuronosyltransferases 1A
    Dong Li
    UMR 7561, Faculté de Médecine and UMR 7036, Faculte des Sciences, CNRS Université Henri Poincaré Nancy 1, 54505 Vandoeuvre les Nancy, France
    J Biol Chem 282:36514-24. 2007
    The human UDP-glucuronosyltransferase UGT1A6 is the primary phenol-metabolizing UDP-glucuronosyltransferase isoform...
  23. ncbi The "albumin effect" and drug glucuronidation: bovine serum albumin and fatty acid-free human serum albumin enhance the glucuronidation of UDP-glucuronosyltransferase (UGT) 1A9 substrates but not UGT1A1 and UGT1A6 activities
    Andrew Rowland
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Drug Metab Dispos 36:1056-62. 2008
    ..Fatty acids had no effect on 4MU glucuronidation by UGT1A1 and UGT1A6 but, paradoxically, all forms of albumin altered the kinetic model for 4MU glucuronidation by UGT1A6 (from ..
  24. ncbi Activation of glucuronidation through reduction of a disulfide bond in rat UDP-glucuronosyltransferase 1A6
    Shin ichi Ikushiro
    Department of Life Science, Graduate School of Science, Himeji Institute of Technology, Harima Science Garden City, Hyogo 678 1297, Japan
    Biochemistry 41:12813-20. 2002
    ..p-NP glucuronidation in Gunn rat hepatic microsomes lacking UGT1 isozymes was not affected by DTT, indicating that UGT1A6 in the microsomes is mainly involved in the activation...
  25. ncbi Human liver UDP-glucuronosyltransferase isoforms involved in the glucuronidation of 7-ethyl-10-hydroxycamptothecin
    N Hanioka
    Division of Environmental Chemistry, National Institute of Health Sciences, Tokyo, Japan
    Xenobiotica 31:687-99. 2001
    ..2. The glucuronidation of SN-38 was catalysed by UGT1A1, UGT1A3, UGT1A6 and UGT1A9 as well as by liver microsomes...
  26. ncbi Determination of UDP-glucuronosyltransferase UGT1A6 activity in human and rat liver microsomes by HPLC with UV detection
    N Hanioka
    Division of Environmental Chemistry, National Institute of Health Sciences, 1 18 1 Kamiyoga, Setagaya Ku, Tokyo 158 8501, Japan
    J Pharm Biomed Anal 25:65-75. 2001
    A simple and sensitive method for the determination of UDP-glucuronosyltransferase UGT1A6 activity using 4-methylumbelliferone (4-MU) and 4-nitrophenol (4-NP) as substrates in human and rat liver microsomes by high-performance liquid ..
  27. ncbi Thyroxine-metabolizing rat uridine diphosphate-glucuronosyltransferase 1A7 is regulated by thyroid hormone receptor
    Yoshikazu Emi
    Graduate School of Life Science, University of Hyogo, Harima Science Park City, Hyogo, Japan
    Endocrinology 148:6124-33. 2007
    ..Determination of the UGT1 isoforms responsible for glucuronidation of T(4) has yet to be conclusively established...
  28. ncbi Bilirubin UDP-glucuronosyltransferase 1 is the only relevant bilirubin glucuronidating isoform in man
    P J Bosma
    Division of Gastroenterology, Academic Medical Centre, Amsterdam, The Netherlands
    J Biol Chem 269:17960-4. 1994
    ..Based on the expression of cDNAs in COS cells, two UGT isoforms in human liver, B-UGT1 and B-UGT2, have been reported to catalyze bilirubin glucuronidation...
  29. ncbi An alternative promoter contributes to tissue- and inducer-specific expression of the rat UDP-glucuronosyltransferase 1A6 gene
    D J Auyeung
    Department of Pharmacology and Toxicology, Medical College of Virginia Campus of Virginia Commonwealth University, Richmond, Virginia 23298, USA
    Toxicol Appl Pharmacol 174:60-8. 2001
    UDP-glucuronosyltransferase 1A6 (UGT1A6), a key enzyme catalyzing the glucuronidation of small planar phenols and amines, is expressed in a tissue- and inducer-dependent manner...
  30. ncbi The novel UGT1 gene complex links bilirubin, xenobiotics, and therapeutic drug metabolism by encoding UDP-glucuronosyltransferase isozymes with a common carboxyl terminus
    I S Owens
    Heritable Disorders Branch, National Institute of Child and Human Development, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Pharmacokinet Biopharm 24:491-508. 1996
    ..The human bilirubin and phenol transferases are encoded by the same gene complex which we designate UGT1. The gene arrangement indicates there are 6 exon 1s each with a promoter and each of which can predictably undergo ..
  31. ncbi Characterization of paracetamol UDP-glucuronosyltransferase activity in human liver microsomes
    J O Miners
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, Adelaide, South Australia
    Biochem Pharmacol 40:595-600. 1990
    ..in human livers microsomes and to assess the substrate specificity of the paracetamol UDP-glucuronosyltransferase (UDPGT) activity...
  32. ncbi Drug-responsive and tissue-specific alternative expression of multiple first exons in rat UDP-glucuronosyltransferase family 1 (UGT1) gene complex
    Y Emi
    Department of Life Science, Faculty of Science, Himeji Institute of Technology, Harima Science Park City, Hyogo
    J Biochem 117:392-9. 1995
    Genomic clones of UDP-glucuronosyltransferase family 1 (UGT1) were isolated from wild-type Wistar rats. The UGT1 locus spans > 120 kb and forms a gene complex...
  33. ncbi Gastrointestinally distributed UDP-glucuronosyltransferase 1A10, which metabolizes estrogens and nonsteroidal anti-inflammatory drugs, depends upon phosphorylation
    Nikhil K Basu
    Heritable Disorders Branch, National Institute of Child Health and Human Development, National Institutes of Health, Room 9S 21, Building 10, Bethesda, MD 20892, USA
    J Biol Chem 279:28320-9. 2004
    Among gastrointestinal distributed isozymes encoded at the UGT1 locus, UDP-glucuronosyltransferase 1A10 (UGT1A10) metabolizes a number of important chemicals. Similar to broad conversion of phytoestrogens (Basu, N. K., Ciotti, M...
  34. ncbi Accelerated degradation of mislocalized UDP-glucuronosyltransferase family 1 (UGT1) proteins in Gunn rat hepatocytes
    Yoshikazu Emi
    Department of Life Science, Faculty of Science, Himeji Institute of Technology, Harima Science Park City, Hyogo 678 1297, Japan
    Arch Biochem Biophys 405:163-9. 2002
    ..A premature termination codon is predicted to produce truncated UGT1 proteins that lack the COOH-terminal 116 amino acids in Gunn rat...
  35. ncbi The glucuronidation of exogenous and endogenous compounds by stably expressed rat and human UDP-glucuronosyltransferase 1.1
    C D King
    Department of Pharmacology, University of Iowa, Iowa City 52242, USA
    Arch Biochem Biophys 332:92-100. 1996
    ..1 share > 70% identity in their deduced primary amino acid sequences. We have previously shown that rat UGT1.1, stably expressed in human embryonic kidney 293 cells, catalyzes the glucuronidation of bilirubin and the mixed ..
  36. ncbi UDP-glucuronosyltransferase 1A6 is the major isozyme responsible for protocatechuic aldehyde glucuronidation in human liver microsomes
    Hui Xin Liu
    Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, No 457 Zhongshan Rd, Dalian 116023 China
    Drug Metab Dispos 36:1562-9. 2008
    ..5 +/- 26.2 microM for M-2, respectively. The PAL glucuronidation activity was significantly correlated with UGT1A6 activity rather than with UGT1A9 activity from 15 individual HLMs...
  37. ncbi UDP-glucuronosyltransferase (UGT1A1*28 and UGT1A6*2) polymorphisms in Caucasians and Asians: relationships to serum bilirubin concentrations
    J W Lampe
    Cancer Prevention Research Program, Fred Hutchinson Cancer Research Center, Seattle, Washington 98109 1024, USA
    Pharmacogenetics 9:341-9. 1999
    ..Two missense mutations on one allele of UGT1A6 (UGT1A6*2) result in T181A and R184S amino acid substitutions and reduced activity against phenolics, such as 4-..
  38. ncbi Developmental hyperbilirubinemia and CNS toxicity in mice humanized with the UDP glucuronosyltransferase 1 (UGT1) locus
    Ryoichi Fujiwara
    Laboratory of Environmental Toxicology, Department of Chemistry and Biochemistry, University of California San Diego, La Jolla, CA 92093, USA
    Proc Natl Acad Sci U S A 107:5024-9. 2010
    ..The human UGT1 locus, encoding all 9-UGT1A genes including UGT1A1, was expressed in Ugt1(-/-) mice...
  39. ncbi A phenylalanine codon deletion at the UGT1 gene complex locus of a Crigler-Najjar type I patient generates a pH-sensitive bilirubin UDP-glucuronosyltransferase
    J K Ritter
    Section on Genetic Disorders of Drug Metabolism, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20892
    J Biol Chem 268:23573-9. 1993
    ..M., Kimura, S., Yeatman, M. T., and Owens, I. S. (1992) J. Biol. Chem. 267, 3257-3261) of the single-copy UGT1 gene complex encoding both bilirubin and phenol UDP-glucuronosyltransferases (transferase) has been critical to the ..
  40. ncbi A critical amino acid residue, asp446, in UDP-glucuronosyltransferase
    H Iwano
    Department of Veterinary Biochemistry, School of Veterinary Medicine, Rakuno Gakuen University, Ebetsu, Hokkaido 069, Japan
    Biochem J 325:587-91. 1997
    ..We obtained a rat phenol UGT (UGT1*06) cDNA (named Ysh) from male rat liver by reverse-transcription (RT)-PCR using pfu polymerase...
  41. ncbi Molecular basis of multiple UDP-glucuronosyltransferase isoenzyme deficiencies in the hyperbilirubinemic rat (Gunn rat)
    T Iyanagi
    Division of Biochemistry, University of Tsukuba, Ibaraki, Japan
    J Biol Chem 266:24048-52. 1991
    ..rat which has unconjugated hyperbilirubinemia as a result of the absence of hepatic UDP-glucuronosyltransferase (UDPGT) activity toward bilirubin...
  42. ncbi Splice-site mutations: a novel genetic mechanism of Crigler-Najjar syndrome type 1
    S Gantla
    Department of Medicine, Albert Einstein College of Medicine, Bronx, New York 10461, USA
    Am J Hum Genet 62:585-92. 1998
    ..exons of the gene (UGT1A1) encoding the uridinediphosphoglucuronate glucuronosyltransferase (UGT) isoform bilirubin-UGT1 were implicated in the absence or inactivation of the enzyme...
  43. ncbi Effects on extrahepatic UDP-glucuronosyltransferases in hypophysectomized rat
    Hiroshi Yokota
    Department of Veterinary Biochemistry, School of Veterinary Medicine, Rakuno Gakuen University, Ebetsu, Hokkaido 069 0836, Japan
    J Biochem 132:265-70. 2002
    ..The mRNA of UGT1A6, which is an isoform contributing to the glucuronidation of various phenolic xenobiotics such as 1-naphthol, were ..
  44. ncbi Adaptive evolution of multiple-variable exons and structural diversity of drug-metabolizing enzymes
    Can Li
    Department of Human Genetics, University of Utah, Salt Lake City, Utah 84112, USA
    BMC Evol Biol 7:69. 2007
    ..of gene clusters with multiple-variable-first exons, including the drug-metabolizing UDP glucuronosyltransferase (UGT1) and I-branching beta-1,6-N-acetylglucosaminyltransferase (GCNT2, also known as IGNT) clusters, organized in a ..
  45. ncbi Polymorphism of UDP-glucuronosyltransferase and drug metabolism
    Yoshihiro Maruo
    Department of Pediatrics, Shiga University of Medical Science, Seta, Otsu, Shiga 520 2192, Japan
    Curr Drug Metab 6:91-9. 2005
    ..a widespread presence of diverse polymorphisms in other isoforms of UGT1 as well as the UGT2 family, including UGT1A6, UGTG1A7, UGT1A8, UGT1A10, UGT2B4, UGT2B7 and UGT2B15...
  46. ncbi Acetaminophen UDP-glucuronosyltransferase in ferrets: species and gender differences, and sequence analysis of ferret UGT1A6
    M H Court
    Laboratory of Comparative Pharmacogenetics, Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    J Vet Pharmacol Ther 24:415-22. 2001
    ..Finally, the exon 1 region of UGT1A6, a major acetaminophen-UGT, was sequenced...
  47. ncbi Transcriptional activation of the UDP-glucuronosyltransferase 1A7 gene in rat liver by aryl hydrocarbon receptor ligands and oltipraz
    R P Metz
    Department of Pharmacology and Toxicology, Virginia Commonwealth University, Medical College of Virginia, Richmond, Virginia 23298, USA
    J Biol Chem 273:5607-14. 1998
    ..A 27-kilobase region that included the UGT1A7/UGT1A6 promoter regions was cloned...
  48. ncbi Expression of hepatic UDP-glucuronosyltransferase 1A1 and 1A6 correlated with increased expression of the nuclear constitutive androstane receptor and peroxisome proliferator-activated receptor alpha in male rats fed a high-fat and high-sucrose diet
    Makoto Osabe
    Department of Pharmaco Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, 52 1 Yada, Shizuoka 422 8526, Japan
    Drug Metab Dispos 36:294-302. 2008
    ..Messenger RNA and protein levels of UGT1A1 and UGT1A6 in the liver but not the jejunum were increased in male rats fed the HF1 diet...
  49. ncbi A mutation in bilirubin uridine 5'-diphosphate-glucuronosyltransferase isoform 1 causing Crigler-Najjar syndrome type II
    P J Bosma
    Department of Hepatogastroenterology, Academisch Medisch Centrum, Amsterdam, The Netherlands
    Gastroenterology 105:216-20. 1993
    ..Both B-UGT isoenzymes (B-UGT1 and B-UGT2) identified in humans are derived from a single gene by alternative splicing...
  50. ncbi Cloning and stable expression of a cDNA encoding a rat liver UDP-glucuronosyltransferase (UDP-glucuronosyltransferase 1.1) that catalyzes the glucuronidation of opioids and bilirubin
    B L Coffman
    Department of Pharmacology, University of Iowa, Iowa City 52242, USA
    Mol Pharmacol 47:1101-5. 1995
    ..Clone pM1 was found to be a full length cDNA coding for a member of the rat UGT1 gene family. Specifically, pM1 represents the full length homologue of the Gunn rat liver pseudo-gene product UGT1...
  51. ncbi Purification and properties of a rat liver phenobarbital-inducible 4-hydroxybiphenyl UDP-glucuronosyltransferase
    P Styczynski
    Department of Pharmacology, University of Iowa, Iowa City 52242
    Mol Pharmacol 40:80-4. 1991
    A phenobarbital-inducible rat hepatic microsomal UDP-glucuronosyltransferase (UDPGT) that catalyzes the glucuronidation of 4-hydroxybiphenyl (4-HBP) has been purified to homogeneity...
  52. ncbi Identification and analysis of drug-responsive expression of UDP-glucuronosyltransferase family 1 (UGT1) isozyme in rat hepatic microsomes using anti-peptide antibodies
    S Ikushiro
    Department of Life Science, Faculty of Science, Himeji Institute of Technology, Hyogo, Japan
    Arch Biochem Biophys 324:267-72. 1995
    Expression of rat hepatic UDP-glucuronosyltransferase family 1 (UGT1) isozymes has been examined using anti-peptide antibodies raised against a conserved carboxyl-terminal portion of all isozymes and variable amino-terminal portions of ..
  53. ncbi The UDP glucuronosyltransferase gene superfamily: suggested nomenclature based on evolutionary divergence
    B Burchell
    Department of Biochemical Medicine, Ninewells Hospital and Medical School, Dundee, Scotland
    DNA Cell Biol 10:487-94. 1991
    ..g., human or murine UGT2B1. Recent experimental evidence suggests that several exons of the UGT1 gene might be shared, indicating that distinct UGT1 transcripts and proteins may arise via alternative splicing; ..
  54. ncbi Structural heterogeneity at the UDP-glucuronosyltransferase 1 locus: functional consequences of three novel missense mutations in the human UGT1A7 gene
    C Guillemette
    Department of Biology and Center for Cancer Research, Massachusetts Institute of Technology, Cambridge, USA
    Pharmacogenetics 10:629-44. 2000
    ..gene, which codes for the putative substrate-binding domain, revealing a high structural heterogeneity at the UGT1 gene locus...
  55. ncbi The induction of hepatic microsomal UDP-glucuronosyltransferase by the methylsulfonyl metabolites of polychlorinated biphenyl congeners in rats
    Y Kato
    School of Pharmaceutical Sciences, University of Shizuoka, 52 1, Yada, Shizuoka, Japan
    Chem Biol Interact 125:107-15. 2000
    ..4-MeSO(2)-CB149) increased the activity of UDP-GT toward chloramphenicol (UGT2B1) but not toward 4-nitrophenol (UGT1A6) and 4-methylumbelliferone (UGT1A6)...
  56. ncbi A 66-base-pair enhancer module activates the expression of a distinct isoform of UDP-glucuronosyltransferase family 1 (UGT1A2) in primary hepatocytes
    Y Emi
    Department of Life Science, Faculty of Science, Himeji Institute of Technology, Harima Science Park City, Hyogo, 678 1297, Japan
    Arch Biochem Biophys 378:384-92. 2000
    UGT1A2, an isoform of the UDP-glucuronosyltransferase family 1 (UGT1), is not expressed in the rat liver, but its expression was highly induced in primary cultures of rat hepatocytes...
  57. ncbi UDP-glucuronosyltransferase 1A6 overexpression in breast cancer cells resistant to methotrexate
    M Cristina de Almagro
    Department of Biochemistry and Molecular Biology, School of Pharmacy, University of Barcelona, Av Diagonal 643, E 08028 Barcelona, Spain
    Biochem Pharmacol 81:60-70. 2011
    ..This family of genes is involved in Phase II metabolism. UGT1A6 was the main isoform responsible for UGT1A family overexpression in these cells...
  58. ncbi The novel bilirubin/phenol UDP-glucuronosyltransferase UGT1 gene locus: implications for multiple nonhemolytic familial hyperbilirubinemia phenotypes
    I S Owens
    Section of Genetic Disorders of Drug Metabolism, National Institute of Child Health and Human Development, Bethesda, MD 20892
    Pharmacogenetics 2:93-108. 1992
    ..the complex disease phenotype in the Gunn rat and by the isolation and description of a novel human gene complex, UGT1, which encodes multiple and independently-regulated transferase isozymes that contain identical carboxyl terminal ..
  59. ncbi Molecular cloning of the baboon UDP-glucuronosyltransferase 1A gene family: evolution of the primate UGT1 locus and relevance for models of human drug metabolism
    Casper S Caspersen
    Division of Neonatology, Department of Pediatrics, Columbia University, New York, New York 10032, USA
    Pharmacogenet Genomics 17:11-24. 2007
    ..Glucuronidation by the UDP glucuronosyltransferase 1A enzymes (UGT1As) is a major pathway for elimination of drugs and endogenous substances, such as bilirubin...
  60. ncbi Effects of cruciferous vegetables and their constituents on drug metabolizing enzymes involved in the bioactivation of DNA-reactive dietary carcinogens
    H Steinkellner
    Institute of Cancer Research, University of Vienna, Vienna, Austria
    Mutat Res 480:285-97. 2001
    ..These effects were paralleled by induction of uridine-di-phospho-glucuronosyl transferase (UDPGT) which is very probably the mechanism of protection against HAs by cruciferous vegetables...
  61. ncbi Maternal intake of quercetin during gestation alters ex vivo benzo[a]pyrene metabolism and DNA adduct formation in adult offspring
    K Vanhees
    Department of Toxicology, School for Nutrition and Toxicology Research Institute Maastricht NUTRIM, Maastricht University, PO Box 616, 6200 MD Maastricht, The Netherlands
    Mutagenesis 27:445-51. 2012
    ..In utero quercetin exposure resulted in significantly enhanced gene expression of Cyp1a1, Cyp1b1, Nqo1 and Ugt1a6 in liver of foetuses at Day 14.5 of gestation...
  62. ncbi UGT1A6 polymorphisms modulated lung cancer risk in a Chinese population
    Ley Fang Kua
    Department of Haematology Oncology, National University Cancer Institute of Singapore, Singapore, Singapore
    PLoS ONE 7:e42873. 2012
    ..The purpose of this study was to evaluate the association of UGT1A6 polymorphisms and haplotypes with lung cancer risk and to evaluate the functional significance of UGT1A6 ..
  63. ncbi Identification of human UDP-glucuronosyltransferases involved in N-carbamoyl glucuronidation of lorcaserin
    Abu J M Sadeque
    Department of Drug Metabolism and Pharmacokinetics, Arena Pharmaceuticals, Inc, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
    Drug Metab Dispos 40:772-8. 2012
    ..glucuronidation was predominantly catalyzed by three UGT2Bs (UGT2B7, UGT2B15, and UGT2B17), whereas two UGT1As (UGT1A6 and UGT1A9) played a minor role. UGT2B15 was most efficient, with an apparent K(m) value of 51.6 ± 1...
  64. ncbi Genetic polymorphisms in UDP-glucuronosyltransferase 1A6 are not associated with NSAIDs-related peptic ulcer haemorrhage
    Martijn G H van Oijen
    Department of Gastroenterology and Hepatology, Radboud University Nijmegen Medical Centre, 6500 HB Nijmegen, The Netherlands
    Drug Metab Lett 3:199-204. 2009
    UDP-glucuronosyltransferase 1A6 (UGT1A6) is involved in metabolizing non-steroidal anti-inflammatory drugs (NSAIDs)...
  65. ncbi Targeted salmon gene array (SalArray): a toxicogenomic tool for gene expression profiling of interactions between estrogen and aryl hydrocarbon receptor signalling pathways
    Anne Skjetne Mortensen
    Department of Biology, Norwegian University of Science and Technology NTNU, Høgskoleringen 5, 7491 Trondheim, Norway
    Chem Res Toxicol 20:474-88. 2007
    ..zona radiata protein (Zr-protein), and vigilin for the ER pathway and AhRalpha, AhRbeta, AhRR, ARNT, CYP1A1, UDPGT, and a 20S proteasome beta-subunit for the AhR pathway...
  66. ncbi Quantification of human uridine-diphosphate glucuronosyl transferase 1A isoforms in liver, intestine, and kidney using nanobore liquid chromatography-tandem mass spectrometry
    David E Harbourt
    Division of Molecular Pharmaceutics, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, North Carolina 27599, USA
    Anal Chem 84:98-105. 2012
    ..Methods for absolute quantification of UGT1A1 and UGT1A6 were previously established utilizing stable isotope peptide internal standards with liquid chromatography-tandem ..
  67. ncbi The influence of UGT1A6 variants and aspirin use in a randomized trial of celecoxib for prevention of colorectal adenoma
    Andrew T Chan
    Gastrointestinal Unit, Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA
    Cancer Prev Res (Phila) 5:61-72. 2012
    Aspirin and celecoxib prevent colorectal adenoma recurrence. Genetic variants in the UGT1A6 enzyme are associated with delayed aspirin metabolism and greater chemopreventive efficacy...
  68. ncbi Oligomerization of the UDP-glucuronosyltransferase 1A proteins: homo- and heterodimerization analysis by fluorescence resonance energy transfer and co-immunoprecipitation
    Theresa N Operaña
    Department of Chemistry and Biochemistry, Laboratory of Environmental Toxicology, University of California, San Diego, La Jolla, California 92093, USA
    J Biol Chem 282:4821-9. 2007
    ..This technique demonstrated that UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A7, UGT1A8, UGT1A9, and UGT1A10 self-oligomerize (homodimerize)...
  69. ncbi 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
    Kathy Senekeo Effenberger
    Leichtag Biomedical Research Building, University of California, San Diego, La Jolla, CA 92093 0722, USA
    Drug Metab Dispos 35:419-27. 2007
    ..In the present study, UGT1A1, UGT1A3, UGT1A4, and UGT1A6 have been identified as targets of the peroxisome proliferator-activated receptor (PPAR) alpha in human ..
  70. ncbi Modification by curcumin of mutagenic activation of carcinogenic N-nitrosamines by extrahepatic cytochromes P-450 2B1 and 2E1 in rats
    Yukio Mori
    Institute of Biological Pharmacy, Gifu Pharmaceutical University, 6 1, Mitahora higashi 5 chome, Gifu 502 8585, Japan
    Cancer Sci 97:896-904. 2006
    ..by immunoblot analyses and Ames preincubation test, respectively, and bilirubin, 4-nitrophenol and testosterone UDPGT activities in F344 rats treated with curcumin and/or NMBA...
  71. ncbi Carriers and patients with muscle-eye-brain disease can be rapidly diagnosed by enzymatic analysis of fibroblasts and lymphoblasts
    Jiri Vajsar
    The Hospital for Sick Children, Toronto, ONT Canada
    Neuromuscul Disord 16:132-6. 2006
    ..1 activity to the activity of a glycosyltransferase control (N-acetylglucosaminyltransferase 1; GnT1) in fibroblasts was on average 0.006 in muscle-eye-brain patients and 0.045 in controls...
  72. ncbi The role of Ah receptor in induction of human UDP-glucuronosyltransferase 1A1
    Mei Fei Yueh
    Department of Pharmacology, Chemistry and Biochemistry, Laboratory of Environmental Toxicology, University of California, San Diego, La Jolla, USA
    Methods Enzymol 400:75-91. 2005
    ..Similar to regulation of CYP1A1, the transcriptional activation of UGT1A1 by TCDD is mediated through the aryl hydrocarbon receptor...
  73. ncbi Persistent glycoprotein misfolding activates the glucosidase II/UGT1-driven calnexin cycle to delay aggregation and loss of folding competence
    Maurizio Molinari
    Institute for Research in Biomedicine, CH 6500 Bellinzona, Switzerland
    Mol Cell 20:503-12. 2005
    ..the fate of a glycoprotein with a reversible, temperature-dependent folding defect in cells with and without UGT1. Upon persistent misfolding, tsO45 G was slowly released from calnexin and entered a second level of retention-..
  74. ncbi No evidence that polymorphisms in CYP2C8, CYP2C9, UGT1A6, PPARdelta and PPARgamma act as modifiers of the protective effect of regular NSAID use on the risk of colorectal carcinoma
    Louise E McGreavey
    Biomedical Research Centre, Ninewells Hospital and Medical School, Dundee, UK
    Pharmacogenet Genomics 15:713-21. 2005
    ..Our objective was to investigate whether or not a number of the polymorphic genes involved in the metabolism of NSAIDs, including cytochrome P450 s (CYPs), act as modifiers of this protective effect...
  75. ncbi In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation
    Donglu Zhang
    Pharmaceutical Candidate Optimization, Bristol Myers Squibb, P O Box 4000, Princeton, NJ 08543, USA
    Drug Metab Dispos 33:1729-39. 2005
    ..The IC50 values found for all compounds for UGT1A6, 1A9, and 2B7 were >100 microM...
  76. ncbi Product inhibition of UDP-glucuronosyltransferase (UGT) enzymes by UDP obfuscates the inhibitory effects of UGT substrates
    Ryoichi Fujiwara
    Drug Metabolism and Toxicology, Division of Pharmaceutical Sciences, Graduate School of Medical Science, Kanazawa University, Kakuma machi, Kanazawa 920 1192, Japan
    Drug Metab Dispos 36:361-7. 2008
    ..1-Naphthol and 4-nitrophenol are probe substrates for human UGT1A6. In the present study, we found that UGT1A1-catalyzed estradiol 3-O-glucuronide formation and UGT1A4-catalyzed ..
  77. ncbi Comparative analysis of involvement of UGT1 and UGT2 splice variants of UDP-galactose transporter in glycosylation of macromolecules in MDCK and CHO cell lines
    Dorota Maszczak-Seneczko
    Laboratory of Biochemistry, Faculty of Biotechnology, University of Wroclaw, Tamka 2, 50 137, Wroclaw, Poland
    Glycoconj J 28:481-92. 2011
    ..Previously, only single forms of UGT were identified in both cell lines, UGT1 in MDCK cells and UGT2 in CHO cells...
  78. ncbi Mayo Genome Consortia: a genotype-phenotype resource for genome-wide association studies with an application to the analysis of circulating bilirubin levels
    Suzette J Bielinski
    Division of Epidemiology, Mayo Clinic, 200 First Street SW, Rochester, MN 55905, USA
    Mayo Clin Proc 86:606-14. 2011
    ....
  79. ncbi Interspecies comparison of the glucuronidation processes in the man, monkey, pig, dog and rat
    Jaroslav Matal
    Department of Pharmacology, Faculty of Medicine and Dentistry, Palacky University, Olomouc, Czech Republic
    Neuro Endocrinol Lett 29:738-43. 2008
    ..The study is focused on determination of the enzyme activity of UGT1A6 (having also a toxicological importance) in microsomes of different species.
  80. ncbi Deferiprone glucuronidation by human tissues and recombinant UDP glucuronosyltransferase 1A6: an in vitro investigation of genetic and splice variants
    Marie Odile Benoit-Biancamano
    CHUQ Research Center, 2705, Boul Laurier, T3 48, G1V 4G2, Quebec, QC, Canada
    Drug Metab Dispos 37:322-9. 2009
    ..DG was measured by liquid chromatography coupled with mass spectrometry. DG was primarily produced in vitro by UGT1A6, and a second glucuronide metabolite was discovered...
  81. ncbi Human UDP-glucuronosyltransferase isoforms involved in bisphenol A glucuronidation
    Nobumitsu Hanioka
    Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, Okayama, Japan
    Chemosphere 74:33-6. 2008
    ..using human liver microsomes and recombinant human UGTs expressed in insect cells (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B4, UGT2B7, UGT2B15 and UGT2B17)...
  82. ncbi [Relationship between genetic polymorphisms of phase I and phase II metabolizing enzymes and DNA damage of workers exposed to vinyl chloride monomer]
    Fang Ji
    Department of Occupational Health, School of Public Health, Fudan University, Key Laboratory of Public Health Safety, Ministry of Education, Shanghai 200032, China
    Wei Sheng Yan Jiu 38:7-11. 2009
    ..To investigate the association between genetic polymorphisms in phase I and phase II metabolism genes and DNA damage in peripheral blood lymphocytes of workers exposed to vinyl chloride monomer (VCM)...
  83. ncbi UDP-glucuronosyltransferase activity toward digitoxigenin monodigitoxoside in human liver microsomes
    B Lacarelle
    Laboratoire de Toxicocinetique et Pharmacocinetique, Faculte de Pharmacie, Marseille, France
    Drug Metab Dispos 21:338-41. 1993
    The properties of UDP-glucuronosyltransferase (UDPGT) toward digitoxigenin-monodigitoxoside (DT1) have been studied in human liver microsomes...
  84. ncbi Comparison of inducibility of sulfotransferase and UDP-glucuronosyltransferase mRNAs by prototypical microsomal enzyme inducers in primary cultures of human and cynomolgus monkey hepatocytes
    Masuhiro Nishimura
    Department of Drug Metabolism, Division of Pharmacology, Drug Safety and Metabolism, Otsuka Pharmaceutical Factory, Inc, Naruto, Tokushima, Japan
    Drug Metab Pharmacokinet 23:45-53. 2008
    ..They also increased the mRNA levels of UGT1A6 and UGT1A9 in cynomolgus monkey hepatocytes, though the extent of elevation of UGT1A6 and UGT1A9 mRNA levels was ..
  85. ncbi Factorial design applied for multiple endpoint toxicity evaluation in Atlantic salmon (Salmo salar L.) hepatocytes
    Liv Søfteland
    National Institute of Nutrition and Seafood Research, N 5817 Bergen, Norway
    Toxicol In Vitro 23:1455-64. 2009
    ..employed to create CYP1A dose-response curves and to quantify the transcriptional levels of eight genes (CYP1A, UDPGT, HSP70, GR, GPX, MnSOD, GST and p53)...
  86. ncbi Interaction of bisphenol A with human UDP-glucuronosyltransferase 1A6 enzyme
    Nobumitsu Hanioka
    Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, 1 1 1 Tsushima naka, Okayama 700 8530, Japan
    Environ Toxicol 23:407-12. 2008
    The effects of bisphenol A (BPA) on UDP-glucuronosyltransferase 1A6 (UGT1A6) activities in microsomes from human livers and yeast cells expressing human UGT1A6 (humUGT1A6) were investigated...
  87. ncbi Genetic diversity at the UGT1 locus is amplified by a novel 3' alternative splicing mechanism leading to nine additional UGT1A proteins that act as regulators of glucuronidation activity
    Hugo Girard
    Laboratory of Pharmacogenomics, Oncology and Molecular Endocrinology Research Center, CHUL Research Center and Faculty of Pharmacy, Laval University, Quebec, Canada
    Pharmacogenet Genomics 17:1077-89. 2007
    The gene UGT1 encodes phase II detoxification proteins involved in the elimination of small hydrophobic substances of both endogenous and exogenous origin...
  88. ncbi Takashi Iyanagi: UGT1 gene complex: from Gunn rat to human
    Shinichi Ikushiro
    Department of Biotechnology, Faculty of Engineering, Toyama Prefectural University, Toyama, Japan
    Drug Metab Rev 42:14-22. 2010
    ..A novel clue to elucidate the gene structure of mammalian UGT1 was cDNA cloning of rat UGT1A6 from the hyperbilirubinemic Gunn rat by Professor Takashi Iyanagi Ph.D...
  89. ncbi Cis-resveratrol glucuronidation kinetics in human and recombinant UGT1A sources
    O F Iwuchukwu
    Department of Pharmaceutical Sciences, Temple University School of Pharmacy, 3307 North Broad Street, Philadelphia, PA 19140, USA
    Xenobiotica 40:102-8. 2010
    ..in human liver and intestinal microsomes and in uridine diphosphate-glucuronosyltransferases (UGTs) UGT1A1, UGT1A6, UGT1A9, and UGT1A10. Kinetic parameters were estimated for the major cis-resveratrol-3-O-glucuronide (cis-R3G)...
  90. ncbi Liverbeads: a practical and relevant in vitro model for gene induction investigations
    Ihab Al Khansa
    Bayer CropScience, Toxicologie Recherche, Sophia Antipolis, France
    Drug Metab Dispos 38:1598-604. 2010
    ..PCN), and clofibric acid (CLO) and analyzed for mRNA levels of Cyp1a1, Cyp2b1, Cyp3a1, Cyp4a1, Ugt1a6, and Ugt2b1. In addition, for PB and PCN, the results were compared with those obtained in rat liver in vivo...
  91. ncbi The development of UDP-glucuronosyltransferases 1A1 and 1A6 in the pediatric liver
    Shogo J Miyagi
    Department of Tropical Medicine, Medical Microbiology and Pharmacology, John A Burns School of Medicine, University of Hawaii at Manoa, 651 Ilalo St, BSB 320, Honolulu, HI 96813, USA
    Drug Metab Dispos 39:912-9. 2011
    ..Maximal activity of 0.7690 nmol · min · (-1) mg protein(-1) was observed for UGT1A1 at 3.8 months. For UGT1A6, activity matured at 14 months (4.737 nmol · min · (-1)mg protein(-1))...
  92. ncbi Fluorescence-based high-throughput screening assay for drug interactions with UGT1A6
    Anne Soikkeli
    Division of Pharmaceutical Technology, University of Helsinki, Viikinkaari 5E, Helsinki, Finland
    Assay Drug Dev Technol 9:496-502. 2011
    ..screening assay for screening potential inhibitors and/or substrates for recombinant human UGTs-here, for the UGT1A6. The assay is based on the increase in fluorescence intensity when 1-naphthol is glucuronidated...
  93. ncbi Refolding of human beta-1-2 GlcNAc transferase (GnT1) and the role of its unpaired Cys 121
    A Sami Saribas
    Neose Technologies, Inc, 102 Rock Road, Horsham, PA 19044, USA
    Biochem Biophys Res Commun 362:381-6. 2007
    ..b>GnT1 mutants were prepared by replacing a predicted unpaired cysteine (C121) with alanine (C121A), serine (C121S), ..
  94. ncbi Functional analysis of six human aryl hydrocarbon receptor variants in a Japanese population
    Satoru Koyano
    Project Team for Pharmacogenetics, National Institute of Health Sciences, 1 18 1 Kamiyoga, Setagaya Ku, Tokyo 158 8501, Japan
    Drug Metab Dispos 33:1254-60. 2005
    ..AhR) is an important transcriptional regulator involved in the induction of CYP1A1, CYP1A2, CYP1B1, UGT1A1, and UGT1A6. In this study, functional properties of four novel naturally occurring human AhR variants (K401R, N487D, I514T, ..
  95. ncbi Genetic defects of the UDP-glucuronosyltransferase-1 (UGT1) gene that cause familial non-haemolytic unconjugated hyperbilirubinaemias
    D J Clarke
    Department of Molecular and Cellular Pathology, University of Dundee, Ninewells Medical School, Scotland, UK
    Clin Chim Acta 266:63-74. 1997
    ..Here we describe genetic defects that occur in the UGT1 gene complex that cause three non-haemolytic unconjugated hyperbilirubinaemia syndromes...
  96. ncbi Functional co-expression of xenobiotic metabolizing enzymes, rat cytochrome P450 1A1 and UDP-glucuronosyltransferase 1A6, in yeast microsomes
    Shin ichi Ikushiro
    Department of Life Science, Graduate School of Science, Himeji Institute of Technology, Harima Science Garden City, Hyogo 678 1297, Japan
    Biochim Biophys Acta 1672:86-92. 2004
    ..in vitro, xenobiotic metabolizing enzymes, rat cytochrome P450 1A1 (P450 1A1) and UDP-glucuronosyltransferase 1A6 (UGT1A6) were co-expressed in Saccharomyces cerevisiae AH22...
  97. ncbi Determination of 7-hydroxycoumarin and its glucuronide and sulphate conjugates in liver slice incubates by capillary zone electrophoresis
    C F Duffy
    School of Biological Sciences, Dublin City University, Glasnevin, Ireland
    J Pharm Biomed Anal 17:1279-84. 1998
    ..21 microM (0.5 microgram ml-1) for the sulphate and 6.17 microM (1 microgram ml)-1 for 7-hydroxycoumarin. Mean inter- and intra-assay results are presented for all three analytes, respectively...
  98. ncbi Treatment of mammalian cells with the endoplasmic reticulum-proliferator compactin strongly induces recombinant and endogenous xenobiotic metabolizing enzymes and 3-hydroxy-3-methylglutaryl-CoA reductase in vitro
    L McLaughlin
    Biomedical Research Centre and Department of Molecular and Cellular Pathology, University of Dundee, Ninewells Hospital and Medical School, Dundee, DD1 9SY, UK
    J Cell Sci 112:515-23. 1999
    ..High levels of recombinant UDP-glucuronosyltransferase UGT1A6 were achieved by amplification of the UGT1A6 cDNA using the dihydrofolate reductase cDNA as selectable marker in ..
  99. ncbi Mono- and Diglucuronide formation from benzo[a]pyrene and chrysene diphenols by AHH-1 cell-expressed UDP-glucuronosyltransferase UGT1A7
    K W Bock
    Institute of Toxicology, University of Tubingen, Germany
    Biochem Pharmacol 57:653-6. 1999
    Polycyclic aromatic hydrocarbon (PAH)-type compounds induce at least two rat UDP-glucuronosyltransferase isoforms, UGT1A6 and UGT1A7...
  100. ncbi Induction of hepatic phase II drug-metabolizing enzymes by 1,7-phenanthroline in rats is accompanied by induction of MRP3
    Sui Wang
    Department of Drug Metabolism, Merck Research Laboratories, P O Box 2000, RY80L 109, Rahway, NJ 07065, USA
    Drug Metab Dispos 31:773-5. 2003
    ..At 150 mg/kg/day, PH treatment resulted in significant increases in hepatic mRNA levels of Mrp3 (36-fold), UGT1A6 (20-fold), UGT2B1 (4-fold), and quinone reductase (QR, 5-fold), compared with the vehicle-treated group...
  101. ncbi Characterization of selective induction and alteration of xenobiotic biotransforming enzymes by vanadium during diethylnitrosamine-induced chemical rat liver carcinogenesis
    A Bishayee
    Department of Pharmaceutical Technology, Jadavpur University, Calcutta, India
    Oncol Res 11:41-53. 1999
    ..5.99), aryl hydrocarbon hydroxylase (AHH, EC 1.14.14.2), and UDP-glucuronyl transferase (UDPGT, EC 2.4.1...

Research Grants63

  1. Inflamation and the Risk of Endometrial Cancer
    Akila Viswanathan; Fiscal Year: 2007
    ..The role of genetic polymorphisms of the enzymes CYP2C9 and UGT1A6 in the metabolism of aspirin in relation to its effect will be studied...
  2. Metabolism and Toxicity of Acetaminophen in Preterm Infants
    JOHANNES NICOLAAS VAN DEN ANKER; Fiscal Year: 2010
    ..of developmental stage (defined by both gestational, and postnatal age) to UDP-glucuronosyltransferase 1A6 (UGT1A6) and sulfotransferase 1A1 (SULT1A1) activity. 2...
  3. Synthesis of Conjugated Metabolites of Buprenophine
    Shixia Feng; Fiscal Year: 2002
    ..The enzymatic synthesis will use either uridine diphosphate glucuronosyltransferase (UDPGT) in solution or immobilized UDPGT to catalyze the reactions...
  4. STUDIES ON UDP-GLUCURONOSYLTRANSFERASES
    Thomas Tephly; Fiscal Year: 1993
    ..Active and FNZ-labeled morphine UDPGT will be purified to homogeneity using Fractogel, chromatofocusing and affinity chromatography...
  5. UDP-GLUCURONYLTRANSFERASES
    Thomas Tephly; Fiscal Year: 1990
    ..Determination of hepatic lobular localization and distribution of p-nitrophenol UDP-glucuronyltransferase (PNP-UDPGT), 17Beta-OH steroid UDPGT and 3Alpha-OH steroid UDPGT by immunohistochemical analyses is planned...
  6. Drug Metabolism and Chronic Liver Disease
    Robert Branch; Fiscal Year: 2005
    ..measure intestinal and hepatic contributions to CYP3A metabolism and Part 3: oral administration of acetaminophen (UGT1A6) simultaneously with intravenous morphine (UGT2B7)...
  7. Pharmacoepidemiology and Pharmacogenetics of a Statin AE
    Bruce Psaty; Fiscal Year: 2007
    ..who did not take gemfibrozil will be sequenced to identify new single nucleotide polymorphisms (SNPs) in CYP2C8, UGT1 Al and UGT1 A3...
  8. Aspirin, UGT1A6 Genotype, and Colon Gene Expression
    Johanna Lampe; Fiscal Year: 2006
    ..Enzymes prominently involved in metabolizing aspirin are UDP-glucuronosyltransferases (UGT). UGT1A6 is a polymorphic UGT and its variant alleles metabolize aspirin less efficiently...
  9. PROTECTION AGAINST BENZO{A} PYRENE TOXICITY BY OLTIPRAZ
    JOSEPH RITTER; Fiscal Year: 2004
    ..Specific Aim 3 will continue studies of the mechanisms controlling the hepatic expression of rat UGT1A6 and UGT1A7 by oltipraz and PAHs...
  10. UDP GLUCURONOSYLTRANSFERASES IN PHARMACOLOGY
    Thomas Tephly; Fiscal Year: 2002
    ..mRNA and glucuronidation activities for UGT2B7 and UGT1A6 have been found in human brain...
  11. Predictors of Adult Leukemia
    Julie Ross; Fiscal Year: 2009
    ..risk factor, and d) the role of genetic susceptibility genes including PON1, CYPs (2C9,3A4,2E1,2D6), GSTs (M1/T1), UGT1A6, PLA2, ODC, MDR1, MPO, NQ01, LEPR, and LEP...
  12. Inflammation and Ovarian Cancer
    Roberta Ness; Fiscal Year: 2007
    ..cancer; 4) in a secondary aim, explore whether allelic variants in the NSAID metabolizing enzymes CYP2C9 and UGT1A6 interact with NSAID use to reduce the risk of ovarian cancer...
  13. NATURAL & SYNTHETIC COUMARINS AS ANTICARCINOGENIC AGENTS
    John DiGiovanni; Fiscal Year: 2002
    ..the effects of coumarins on the levels and expression of epidermal uridine-5'- diphosphoglucuronyltransferase (UDPGT), glutathione-S-transferase (GST), epoxide hydrase (EH), and/or sulfotransferase (ST); and 4) to determine the ..