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 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
  3. doi 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
  4. doi 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
  5. pmc 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
  6. pmc 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. doi 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
  8. ncbi Genetic polymorphism in the human UGT1A6 (planar phenol) UDP-glucuronosyltransferase: pharmacological implications
    M Ciotti
    Heritable Disorders Branch, National Institute of Child Health and Human Development, Bethesda, MD 20892 1830, USA
    Pharmacogenetics 7:485-95. 1997
  9. ncbi Human UGT1A6 pharmacogenetics: identification of a novel SNP, characterization of allele frequencies and functional analysis of recombinant allozymes in human liver tissue and in cultured cells
    Swati Nagar
    Department of Pharmacology, Fox Chase Cancer Center, Philadelphia, PA, USA
    Pharmacogenetics 14:487-99. 2004
  10. ncbi Evaluation of 5-hydroxytryptophol and other endogenous serotonin (5-hydroxytryptamine) analogs as substrates for UDP-glucuronosyltransferase 1A6
    Soundararajan Krishnaswamy
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
    Drug Metab Dispos 32:862-9. 2004

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

Publications173 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 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 ..
  3. doi 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 ..
  4. doi 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...
  5. pmc 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...
  6. pmc 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. doi 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...
  8. ncbi Genetic polymorphism in the human UGT1A6 (planar phenol) UDP-glucuronosyltransferase: pharmacological implications
    M Ciotti
    Heritable Disorders Branch, National Institute of Child Health and Human Development, Bethesda, MD 20892 1830, USA
    Pharmacogenetics 7:485-95. 1997
    Two missense mutations were uncovered in the UGT1A6 (HLUG P1) cDNA which codes for a human phenol-metabolizing UDP-glucuronosyltransferase...
  9. ncbi Human UGT1A6 pharmacogenetics: identification of a novel SNP, characterization of allele frequencies and functional analysis of recombinant allozymes in human liver tissue and in cultured cells
    Swati Nagar
    Department of Pharmacology, Fox Chase Cancer Center, Philadelphia, PA, USA
    Pharmacogenetics 14:487-99. 2004
    ..The UGT1A6 protein is expressed predominantly in liver and metabolizes small phenolic drugs including acetaminophen, ..
  10. ncbi Evaluation of 5-hydroxytryptophol and other endogenous serotonin (5-hydroxytryptamine) analogs as substrates for UDP-glucuronosyltransferase 1A6
    Soundararajan Krishnaswamy
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
    Drug Metab Dispos 32:862-9. 2004
    ..In this study, the contribution of UGT1A6 to the glucuronidation of endogenous structural analogs of serotonin, including 5-hydroxytryptophol, N-..
  11. ncbi Genetic variants in the UGT1A6 enzyme, aspirin use, and the risk of colorectal adenoma
    Andrew T Chan
    Gastrointestinal Unit, Massachusetts General Hospital and Harvard Medical School, GRJ 722, Boston, MA 02114, USA
    J Natl Cancer Inst 97:457-60. 2005
    Genetic variation in the uridine diphosphate glucuronosyltransferase 1A6 (UGT1A6) enzyme is associated with impaired metabolism of aspirin...
  12. ncbi UDP glucuronosyltransferase (UGT) 1A6 pharmacogenetics: I. Identification of polymorphisms in the 5'-regulatory and exon 1 regions, and association with human liver UGT1A6 gene expression and glucuronidation
    Soundararajan Krishnaswamy
    Molecular Pharmacogenetics Laboratory, Department of Pharmacology and Experimental Therapeutics, Tufts University, Boston, MA 02111, USA
    J Pharmacol Exp Ther 313:1331-9. 2005
    ..studies were conducted using a well characterized human liver bank (n = 54) and serotonin glucuronidation as a UGT1A6-specific phenotype marker...
  13. ncbi Genetic polymorphisms of UGT1A6 in a Japanese population
    Mayumi Saeki
    Project Team for Pharmacogenetics, National Institute of Health Sciences, Tokyo, Japan
    Drug Metab Pharmacokinet 20:85-90. 2005
    ..Then, 11 haplotypes in UGT1A6 were estimated...
  14. 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...
  15. 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...
  16. 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...
  17. 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...
  18. 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 ..
  19. 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 ..
  20. 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...
  21. 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...
  22. 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...
  23. doi 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 ..
  24. pmc 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...
  25. 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...
  26. 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...
  27. doi 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 ..
  28. 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...
  29. 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...
  30. 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 ..
  31. 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...
  32. 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 ..
  33. 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...
  34. 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...
  35. 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...
  36. 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...
  37. 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...
  38. 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...
  39. 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 ..
  40. 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-..
  41. doi 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...
  42. pmc 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...
  43. 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 ..
  44. pmc 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...
  45. 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 ..
  46. pmc 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...
  47. pmc 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 ..
  48. 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...
  49. 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...
  50. 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...
  51. 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...
  52. 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...
  53. 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...
  54. 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...
  55. 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...
  56. 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 ..
  57. 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)...
  58. 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...
  59. 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...
  60. doi 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...
  61. 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; ..
  62. 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...
  63. 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 ..
  64. 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...
  65. doi Genetic polymorphisms of UGT1A8, UGT1A9 and HNF-1α and gastrointestinal symptoms in renal transplant recipients taking mycophenolic acid
    Don Vu
    Mendez National Institute of Transplantation, Los Angeles, CA, United States Saint Vincent Medical Center, Los Angeles, CA, United States Western University of Health Sciences, Pomona, CA, United States
    Transpl Immunol 29:155-61. 2013
    ..In this study, we investigated whether polymorphisms of UDP-glucuronosyltransferases (UGT1) A8, 1A9, and hepatocyte nuclear factor (HNF1α) genes or pharmacokinetic parameters of mycophenolic acid (MPA) ..
  66. doi UDP-Gal/UDP-GlcNAc chimeric transporter complements mutation defect in mammalian cells deficient in UDP-Gal transporter
    Mariusz Olczak
    Laboratory of Biochemistry, Faculty of Biotechnology, University of Wrocław, 2 Tamka St, 50 137 Wrocław, Poland
    Biochem Biophys Res Commun 434:473-8. 2013
    ..construct chimeric transporters composed of the N-terminal portion of human NGT and the C-terminal portion of human UGT1 or UGT2 (NGT-UGT1 or NGT-UGT2, respectively), as well as of the N-terminal portion of UGT and C-terminal portion of ..
  67. ncbi Acute effects of novel selenazolidines on murine chemoprotective enzymes
    Wael El-Sayed
    University of Utah, Department of Pharmacology and Toxicology, Salt Lake City, UT 84112, United States
    Chem Biol Interact 162:31-42. 2006
    ..When given i.g., 2-butyl SCA (BSCA) resulted in elevations in alpha, mu and pi class Gsts, Ugt1a6, Tr, and Gpx, and 2-phenyl SCA (PhSCA) elevated GstP, Ugt1a9, Tr, Gpx (3 kb), and Meh...
  68. 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...
  69. ncbi Quantitative structure activity relationships for the glucuronidation of simple phenols by expressed human UGT1A6 and UGT1A9
    Brian T Ethell
    Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, Dundee, United Kingdom
    Drug Metab Dispos 30:734-8. 2002
    b>UGT1A6 and UGT1A9 have both been demonstrated to rapidly glucuronidate simple phenolic compounds...
  70. ncbi Characterization and profiling of hepatic cytochromes P450 and phase II xenobiotic-metabolizing enzymes in beluga whales (Delphinapterus leucas) from the St. Lawrence River Estuary and the Canadian Arctic
    Melissa A McKinney
    Great Lakes Institute for Environmental Research, University of Windsor, Windsor, Ont, Canada N9B 3P4
    Aquat Toxicol 69:35-49. 2004
    ..microsomal CYP1A, CYP2B, CYP3A, CYP2E, epoxide hydrolase (EH) and uridine diphosphoglucuronosyl transferase (UDPGT) isozymes...
  71. ncbi Tissue-specific, inducible, and hormonal control of the human UDP-glucuronosyltransferase-1 (UGT1) locus
    Shujuan Chen
    Laboratory of Environmental Toxicology, Department of Pharmacology, University of California, San Diego, La Jolla, 92093 0722, USA
    J Biol Chem 280:37547-57. 2005
    ..In maternal 14-day post-conception Tg-UGT1mice, liver UGT1A1, UGT1A4, and UGT1A6 were induced, with the levels returning to near normal by birth...
  72. ncbi Induction of UGT1A6 isoform by inflammatory conditions in rat astrocytes
    T Heurtaux
    Unité Mixte de Recherche CNRS Université Henri Poincaré Nancy 1, No 7561, Laboratoire de Pharmacologie, Faculte de Medecine, BP 184, 54505 Vandoeuvre Les Nancy Cedex, France
    Neuropharmacology 50:317-28. 2006
    ..This increase in glucuronidation activity was associated with an up-regulation of the UGT1A6 isoform mRNA level as shown by RT-PCR and gene reporter assay...
  73. pmc 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 ..
  74. doi 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...
  75. doi 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...
  76. 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...
  77. 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...
  78. doi 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...
  79. 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 ..
  80. 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...
  81. 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), ..
  82. pmc Immunochemical analysis of uridine diphosphate-glucuronosyltransferase in four patients with the Crigler-Najjar syndrome type I
    H H van Es
    Division of Gastroenterology, Academic Medical Center, Amsterdam, The Netherlands
    J Clin Invest 85:1199-205. 1990
    The functional heterogeneity of uridine diphosphate-glucuronosyltransferase (UDPGT) and its deficiency in human liver were investigated...
  83. ncbi Interactions between CYP2C9 and UGT1A6 polymorphisms and nonsteroidal anti-inflammatory drugs in colorectal cancer prevention
    Wade S Samowitz
    Department of Pathology, University of Utah Health Sciences Center, Salt Lake City, Utah 84132, USA
    Clin Gastroenterol Hepatol 4:894-901. 2006
    Variant genotypes of uridine diphosphate glucuronsyltransferase isoenzyme 1A6 (UGT1A6) associated with decreased metabolic activity have been associated with an enhanced protective effect of aspirin on the development of colorectal ..
  84. 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...
  85. 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...
  86. 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 ..
  87. 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)...
  88. 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 ..
  89. 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...
  90. doi 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...
  91. 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.
  92. pmc 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...
  93. pmc 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...
  94. pmc 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
    ....
  95. doi 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...
  96. pmc 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))...
  97. doi 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...
  98. doi 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)...
  99. doi 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...
  100. 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)...
  101. doi 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)...

Research Grants65

  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 ..