UGT1A6

Summary

Gene Symbol: UGT1A6
Description: UDP glucuronosyltransferase family 1 member A6
Alias: GNT1, HLUGP, HLUGP1, UDPGT, UDPGT 1-6, UGT1, UGT1A6S, UGT1F, UDP-glucuronosyltransferase 1-6, UDP glucuronosyltransferase 1 family, polypeptide A6, UDP glycosyltransferase 1 family, polypeptide A6, UDP-glucuronosyltransferase 1 family polypeptide A6s, 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 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
  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. 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. 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
  6. 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
  7. 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
  8. 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
  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 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

Research Grants

  1. MATURATION OF LIVER FOR THE METABOLISM OF BILIRUBIN
    Glenn Gourley; Fiscal Year: 1993
  2. Yuesheng Zhang; Fiscal Year: 2016
  3. Robert H Tukey; Fiscal Year: 2015
  4. UDP-GLUCURONYL-TRANSFERASE AND RADIOCONTRAST MEDIA
    ADRIANA COBO FRENKEL; Fiscal Year: 1980
  5. INHERITED DISORDERS OF BILIRUBIN GLUCURONIDATION
    Jayanta Roy Chowdhury; Fiscal Year: 1991
  6. JOHANNES NICOLAAS VAN DEN ANKER; Fiscal Year: 2014
  7. Synthesis of Conjugated Metabolites of Buprenophine
    Shixia Feng; Fiscal Year: 2002
  8. MEMBRANE BOUND DETOXICATION ENZYMES
    Richard Armstrong; Fiscal Year: 2000
  9. Robert H Tukey; Fiscal Year: 2016
  10. Organ-specific Ugt1 profiling in detoxifying the anticancer drug CPT-11
    Shujuan Chen; Fiscal Year: 2013

Detail Information

Publications209 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 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...
  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. 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. 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...
  6. 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...
  7. 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...
  8. 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-..
  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 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...
  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 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...
  13. 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...
  14. 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...
  15. 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...
  16. pmc Genome-wide association of serum bilirubin levels in Korean population
    Tae Wook Kang
    Medical Genomics Research Center, Korea Research Institute of Bioscience and Biotechnology, Yuseong Gu, Daejeon, Republic of Korea
    Hum Mol Genet 19:3672-8. 2010
    ..Our result supports the idea that there are considerable ethnic differences in genetic association of bilirubin levels between Koreans and European-derived populations...
  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 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...
  21. 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...
  22. 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...
  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. 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 ..
  25. 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...
  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 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...
  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 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 ..
  30. 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...
  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 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...
  33. 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...
  34. 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...
  35. 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...
  36. 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 ..
  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. 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...
  39. 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...
  40. 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 ..
  41. 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...
  42. 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...
  43. 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...
  44. 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 ..
  45. 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 ..
  46. 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...
  47. 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...
  48. 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...
  49. 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...
  50. 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...
  51. 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...
  52. 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...
  53. 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 ..
  54. 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; ..
  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 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...
  58. 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...
  59. 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 ..
  60. 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...
  61. 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...
  62. ncbi Mapping of the mouse bilirubin UDP-glucuronosyltransferase gene (Gnt-1) to chromosome 1 by restriction fragment length variations
    H Sato
    Department of Biology, Shiga University of Medical Science, Japan
    Biochem Genet 30:347-52. 1992
    ..length variations (RFLVs) were detected by using a rat cDNA probe for the bilirubin UDP-glucuronosyltransferase (UDPGT) gene between two mouse strains, 129/Sv and MOL-MIT. RFLVs of the gene were found by EcoRI and PvuII digestions...
  63. ncbi Promoters of auxin-induced genes from tobacco can lead to auxin-inducible and root tip-specific expression
    E J van der Zaal
    Department of Plant Molecular Biology, Leiden University, Netherlands
    Plant Mol Biol 16:983-98. 1991
    ..In this study we determined the sequences of three 103-like cDNAs and two 103-like genes, GNT1 and GNT35...
  64. pmc Cloning and stable expression of a new member of the human liver phenol/bilirubin: UDP-glucuronosyltransferase cDNA family
    R Wooster
    Biochemical Medicine, University of Dundee, Ninewells Hospital and Medical School, Scotland, U K
    Biochem J 278:465-9. 1991
    ..The C-terminal half of the sequence (246 amino acids) is 96% identical with the same portion of HlugP1, whereas the N-terminal half of the deduced protein sequences are only 38% identical...
  65. pmc Discrimination between Crigler-Najjar type I and II by expression of mutant bilirubin uridine diphosphate-glucuronosyltransferase
    J Seppen
    Department of Gastrointestinal and Liver Diseases, Academic Medical Centre, Amsterdam, The Netherlands
    J Clin Invest 94:2385-91. 1994
    ..All type I patients examined had mutations in the B-UGT1 gene that lead to completely inactive enzymes...
  66. 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...
  67. ncbi Comparison of stably expressed rat UGT1.1 and UGT2B1 in the glucuronidation of opioid compounds
    C D King
    Department of Pharmacology, University of Iowa, Iowa City 52242, USA
    Drug Metab Dispos 25:251-5. 1997
    ..glucuronidation efficiencies of opioid agonists, antagonists, and partial agonists with two rat UGT isoforms; UGT1.1, which is generally considered the "bilirubin UGT," and UGT2B1, which has previously been shown to catalyze the ..
  68. ncbi How knockout mouse lines will be used to study the role of drug-metabolizing enzymes and their receptors during reproduction and development, and in environmental toxicity, cancer, and oxidative stress
    D W Nebert
    Department of Environmental Health, University of Cincinnati Medical Center, OH 45267, U S A
    Biochem Pharmacol 53:249-54. 1997
    ..class 3" aldehyde dehydrogenase (Ahd4); a UDP glucuronosyltransferase having 4-methylumbelliferone as substrate (Ugt1a6); and a glutathione transferase having 2,4-dinitro-1-chlorobenzene as substrate (Gsta1, Ya)...
  69. ncbi Regulation of uridine diphosphate glucuronosyltransferase during the acute-phase response
    S I Strasser
    Department of Gastroenterology, St Vincent s Hospital, Fitzroy, Victoria, Australia
    J Gastroenterol Hepatol 13:88-94. 1998
    ..01). In contrast, the mRNA level of UGT1*1 (which metabolizes bilirubin, not phenols) was depressed to 16% of control (P<0...
  70. 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...
  71. ncbi Effects of polybrominated diphenyl ethers (PBDEs) and polychlorinated biphenyls (PCBs) on thyroid hormone and vitamin A levels in rats and mice
    S Hallgren
    Department of Pharmaceutical Biosciences, Uppsala University, Sweden
    Arch Toxicol 75:200-8. 2001
    ..However, induction of uridine diphosphoglucuronosyl transferase (UDPGT) was small and for most groups insignificant...
  72. ncbi Effects of polychlorinated biphenyls, kanechlor-500, on serum thyroid hormone levels in rats and mice
    Yoshihisa Kato
    School of Pharmaceutical Sciences, University of Shizuoka, 52 1, Yada, Shizuoka 422 8526, Japan
    Toxicol Sci 72:235-41. 2003
    ..Hepatic UDP-glucuronosyltransferases (UDP-GTs) UGT1A1 and UGT1A6, which efficiently mediate glucuronidation of T4 and promote the excretion of the hormones, were induced by KC500 ..
  73. ncbi Effect of spironolactone on the expression of rat hepatic UDP-glucuronosyltransferase
    Viviana A Catania
    Instituto de Fisiologia Experimental, CONICET Universidad Nacional de Rosario, Facultad de Ciencias Bioquimicas y Farmaceuticas, Suipacha 570, Rosario 2000, Argentina
    Biochem Pharmacol 66:171-7. 2003
    ..p-Nitrophenol glucuronidation rate and mRNA and protein levels of UGT1A6, the main isoform conjugating planar phenols, were not affected by the inducer...
  74. ncbi Contribution of the Ah receptor to the phenolic antioxidant-mediated expression of human and rat UDP-glucuronosyltransferase UGT1A6 in Caco-2 and rat hepatoma 5L cells
    Peter A Munzel
    Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Tübingen D 72074, Germany
    Biochem Pharmacol 66:841-7. 2003
    ..TCDD) and phenolic antioxidants such as tert-butylhydroquinone (tBHQ) are known to induce the expression of human UGT1A6 in Caco-2 cells...
  75. 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...
  76. ncbi Coimmunoprecipitation of UDP-glucuronosyltransferase isoforms and cytochrome P450 3A4
    Jacqueline J Fremont
    Merck and Co, 3535 General Atomics Court, San Diego, CA 92121, USA
    Mol Pharmacol 67:260-2. 2005
    ..Solubilized human liver microsomes were incubated with specific antibodies to UGT2B7, UGT1A6, UGT1A1, and CYP3A4, and the immunoprecipitates were run on SDS-polyacrylamide gel electrophoresis...
  77. ncbi Age, gender and region-specific differences in drug metabolising enzymes in rat ocular tissues
    Kayo Nakamura
    Kyoritsu University of Pharmacy, 1 5 30, Shibakoen, Minato ku, Tokyo 1 5 8512, Japan
    Exp Eye Res 81:710-5. 2005
    ..The expression levels of the UGTs, UGT1A1, UGT1A6 and UGT2B1, were also higher in the female extra-lenticular tissues but the expression of the GSTA subfamily (..
  78. ncbi Successful gene therapy of the Gunn rat by in vivo neonatal hepatic gene transfer using murine oncoretroviral vectors
    Marta Bellodi-Privato
    Biothérapies Hépatiques, INSERM CIC 04, CHU Hotel Dieu, 44093 Nantes Cedex 01, France
    Hepatology 42:431-8. 2005
    ..is a rare inherited metabolic disease characterized by complete absence of hepatic UDP-glucuronosyl transferase (UGT1), resulting in high levels of unconjugated bilirubin. CN1 is an attractive candidate disease for gene therapy...
  79. ncbi Induction of genes for metabolism and transport by trans-stilbene oxide in livers of Sprague-Dawley and Wistar-Kyoto rats
    A L Slitt
    Department of Pharmacology, Toxicology, and Therapeutics, University of Kansas Medical Center, Kansas City, KS 66160 7417, USA
    Drug Metab Dispos 34:1190-7. 2006
    ..CYP2B1/2, CYP3A1, epoxide hydrolase, heme oxygenase-1, UGT1A6, UGT2B1, multiple drug resistance protein (Mdr) 1a and 1b, as well as multidrug resistance-associated protein (Mrp)..
  80. ncbi N-glucuronidation of perfluorooctanesulfonamide by human, rat, dog, and monkey liver microsomes and by expressed rat and human UDP-glucuronosyltransferases
    Lin Xu
    Department of Pharmacology and Physiology, University of Rochester Medical Center, 601 Elmwood Avenue, Box 711, Rochester, NY 14642, USA
    Drug Metab Dispos 34:1406-10. 2006
    ..Expressed rat UGT1.1, UGT2B1, and UGT2B12 in HK293 cells catalyzed the N-glucuronidation of FOSA but at rates that were lower than ..
  81. ncbi Glucuronidation in the chimpanzee (Pan troglodytes): studies with acetaminophen, oestradiol and morphine
    H Wong
    Drug Metabolism and Pharmacokinetics, Genentech, Inc, 1 DNA Way, MS 86, South San Francisco, CA 94080, USA
    Xenobiotica 36:1178-90. 2006
    ..chimpanzee liver microsomes revealed a single immunoreactive band when probed with anti-human UGT1A1, anti-human UGT1A6, and anti-human UGT2B7...
  82. ncbi Toxicity profiles in rats treated with tumorigenic and nontumorigenic triazole conazole fungicides: Propiconazole, triadimefon, and myclobutanil
    Douglas C Wolf
    Environmental Carcinogenesis Division, National Health and Environmental Effects Research Laboratory, ORD, USEPA, Research Triangle Park, North Carolina 27711, USA
    Toxicol Pathol 34:895-902. 2006
    ..Uridine diphopho-glucuronosyl transferase (UDPGT), the T4 metabolizing enzyme measured as glucuronidation of 1-naphthol, was induced to the same extent after 30 ..
  83. ncbi Studies on the expression of liver detoxifying enzymes in rats fed seaweed (Monostroma nitidum)
    Albert Linton Charles
    Department of Tropical Agriculture and International Cooperation, National Pingtung University of Science and Technology NPUST, Pingtung 91201, Taiwan, ROC
    Food Chem Toxicol 45:2390-6. 2007
    ..However, an M. nitidum diet was found to significantly increase UGT1A1 and UGT1A6 mRNA levels and to decrease CYP1A1 mRNA levels in rat liver...
  84. 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...
  85. doi UDP-glucuronosyltransferases 1A6 and 1A10 catalyze reduced menadione glucuronidation
    Takahito Nishiyama
    Department of Drug Metabolism and Molecular Toxicology, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432 1 Horinouchi, Hachioji shi, Tokyo 192 0392, Japan
    Biochem Biophys Res Commun 371:247-50. 2008
    ..In contrast to these UGTs, only UGT1A6 exhibited 1-menadiol-preferential glucuronidating activity...
  86. doi Hepatic monooxygenase (CYP1A and CYP3A) and UDPGT enzymatic activities as biomarkers for long-term carbofuran exposure in tench (Tinca tinca L)
    David Hernández-Moreno
    Toxicology Area, Faculty of Veterinary Medicine, Avda de la Universidad, Caceres, Spain
    J Environ Sci Health B 43:395-404. 2008
    ..1A (CYP1A) and 3A (CYP3A) activities, as well as the phase II enzyme uridine diphospho-glucuronosyltransferase (UDPGT) activity were evaluated as adequate biomarkers of fish exposure to environmentally relevant concentrations of the ..
  87. doi Effects of Andrographis paniculata and Orthosiphon stamineus extracts on the glucuronidation of 4-methylumbelliferone in human UGT isoforms
    Sabariah Ismail
    Centre for Drug Research, Universiti Sains Malaysia, 11800, Penang, Malaysia
    Molecules 15:3578-92. 2010
    ..extracts on the in vitro glucuronidation of 4-methylumbelliferone (4MU) by recombinant human UGTs, UGT1A1, UGT1A3, UGT1A6, UGT1A7, UGT1A8, UGT1A10, UGT2B7 and UGT2B15 were determined...
  88. doi Metabolism of ebracteolata compound B studied in vitro with human liver microsomes, HepG2 cells, and recombinant human enzymes
    Xia Zhang
    Department of Pharmaceutical Analysis and Drug Metabolism, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, People s Republic of China
    Drug Metab Dispos 38:2157-65. 2010
    ..The results indicated that CYP3A4 was probably involved in ECB oxidative metabolism and UGT1A6 and UGT1A9 were important catalytic enzymes in ECB glucuronidation...
  89. doi Indole-3-carbinol enhances oxidative stress responses resulting in the induction of preneoplastic liver cell lesions in partially hepatectomized rats initiated with diethylnitrosamine
    Keisuke Shimamoto
    Laboratory of Veterinary Pathology, Tokyo University of Agriculture and Technology, 3 5 8 Saiwai cho, Fuchu, Tokyo 183 8509, Japan
    Toxicology 283:109-17. 2011
    ..receptor (AhR) and/or nuclear factor (erythroid-derived 2)-like 2 (Nrf2) gene batteries, such as Cyp1a2, Cyp1b1, Ugt1a6, Nrf2, Nqo1, Gsta5, Gstm2, Ggt1and Gpx2...
  90. pmc Polymorphisms of Aspirin-Metabolizing Enzymes CYP2C9, NAT2 and UGT1A6 in Aspirin-Intolerant Urticaria
    Nami Shrestha Palikhe
    Department of Allergy and Clinical Immunology, Ajou University School of Medicine, Suwon, Korea
    Allergy Asthma Immunol Res 3:273-6. 2011
    Acetyl salicylic acid (ASA) is metabolized by UDP-glucuronosyltransferase 1A6 (UGT1A6), cytochrome P4502C9 (CYP2C9), and N-acetyl transferase 2 (NAT2)...
  91. doi S-Glucuronidation of 7-mercapto-4-methylcoumarin by human UDP glycosyltransferases in genetically engineered fission yeast cells
    Daniela Buchheit
    PomBioTech GmbH, Campus Geb A1, D 66123 Saarbrucken, Germany
    Biol Chem 392:1089-95. 2011
    ..by whole cell biotransformation with fission yeast strains that recombinantly express all 19 human members of the UGT1 and UGT2 families, it was found that 13 isoenzymes were able to glucuronidate 7-mercapto-4-methylcoumarin, with ..
  92. doi Highly variable pH effects on the interaction of diclofenac and indomethacin with human UDP-glucuronosyltransferases
    Hongbo Zhang
    Center for Drug Research, University of Helsinki, Finland
    Toxicol In Vitro 26:1286-93. 2012
    ..4. On the other hand, UGT2B15 lost activity upon lowering the reaction pH to 6.0. UGT1A6 does not glucuronidate diclofenac and indomethacin...
  93. ncbi Non tumoral hyperserotoninaemia responsive to octreotide due to dual polymorphism in UGT1A1 and UGT1A6
    Anna Maladaki
    Division of Endocrinology and Metabolism, 1st Internal Medicine Department, AHEPA University Hospital, Aristotle University of Thessaloniki, Greece
    Hormones (Athens) 11:104-8. 2012
    ..The frequent occurrence of hyperserotoninaemia in Gilbert's syndrome may contribute, at least partly, to the nonspecific symptomatology commonly seen in these patients and should be promptly evaluated...
  94. pmc Red meat and poultry, cooking practices, genetic susceptibility and risk of prostate cancer: results from a multiethnic case-control study
    Amit D Joshi
    Department of Preventive Medicine, University of Southern California Keck School of Medicine, Norris Comprehensive Cancer Center Los Angeles, CA 90033, USA
    Carcinogenesis 33:2108-18. 2012
    ..12 SNPs and 2 copy number variants in 10 carcinogen metabolism genes: GSTP1, PTGS2, CYP1A2, CYP2E1, EPHX1, CYP1B1, UGT1A6, NAT2, GSTM1 and GSTT1...
  95. pmc Regulation of hepatic phase II metabolism in pregnant mice
    Xia Wen
    Dept of Pharmacology and Toxicology, Rutgers University Ernest Mario School of Pharmacy, 170 Frelinghuysen Rd Piscataway, NJ 08854, USA
    J Pharmacol Exp Ther 344:244-52. 2013
    ..Protein expression of Ugt1a6 also decreased and corresponded with reduced in vitro glucuronidation of bisphenol A in S9 fractions from livers ..
  96. doi A genome-wide assessment of variability in human serum metabolism
    Mun Gwan Hong
    Department of Medical Epidemiology and Biostatistics, Karolinska Institute, Stockholm, Sweden
    Hum Mutat 34:515-24. 2013
    ..mQTL SNPs and mQTL-harboring genes were over-represented across GWASs conducted to date, suggesting that these data may have utility in tracing the molecular basis of some complex disease associations...
  97. doi Comparative xenobiotic metabolism capacities and pesticide sensitivity in adults of Solea solea and Solea senegalensis
    Samuel Koenig
    Institute of Marine Sciences ICM CSIC, Pg Maritim de la Barceloneta 37 49, 08003 Barcelona, Spain
    Comp Biochem Physiol C Toxicol Pharmacol 157:329-36. 2013
    ..The conjugating activities of glutathione S-transferase (GST) and UPD-glucuronosyltransferase (UDPGT) were also assessed...
  98. doi Dysregulations of UDP-glucuronosyltransferases in rats with valproic acid and high fat diet induced fatty liver
    Lifang Zhang
    State Key Laboratory of Natural Medicines, Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, China
    Eur J Pharmacol 721:277-85. 2013
    ..Notably, the protein expression and enzymatic activity of UGT1A6 were significantly increased in rats treated with HFD or VPA alone, and were further enhanced by HFD and VPA co-..
  99. pmc Age-dependent pattern of cerebellar susceptibility to bilirubin neurotoxicity in vivo in mice
    Giulia Bortolussi
    International Centre for Genetic Engineering and Biotechnology ICGEB, 34149 Trieste, Italy
    Dis Model Mech 7:1057-68. 2014
    ..Severity of BIND was associated with genetic background, with 50% survival of C57BL/6‑Ugt1(-/-) mutant mice at postnatal day 5 (P5), and of FVB/NJ-Ugt1(-/-) mice at P11...
  100. doi A novel UGT1 marker associated with better tolerance against irinotecan-induced severe neutropenia in metastatic colorectal cancer patients
    S Chen
    Pharmacogenomics Laboratory, Centre Hospitalier Universitaire de Québec Research Center and Faculty of Pharmacy, Laval University, Quebec, Quebec, Canada
    Pharmacogenomics J 15:513-20. 2015
    The risk of severe irinotecan-induced neutropenia has been shown to be related to the UGT1 variant UGT1A1*28, which increases exposure to the potent metabolite SN-38...
  101. 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...

Research Grants57

  1. MATURATION OF LIVER FOR THE METABOLISM OF BILIRUBIN
    Glenn Gourley; Fiscal Year: 1993
    ..The bilirubin transferase enzyme, (B-UDPGt), will be isolated to homogeneity from normal rat liver after its selective induction by clofibrate administration...
  2. Yuesheng Zhang; Fiscal Year: 2016
    ..Two animal models will be used to test the hypothesis, including the UGT1A3 mouse model described above and the Tg-UGT1 mouse model (mice carry both the coding and the regulatory sequences of the human UGT1A3 gene)...
  3. Robert H Tukey; Fiscal Year: 2015
    ..provided by applicant): Human UDP-glucuronosyltransferase 1A1, which is part of 9-UGT1A proteins encoded by the UGT1 locus, plays a key role in many aspects of normal pathophysiology...
  4. UDP-GLUCURONYL-TRANSFERASE AND RADIOCONTRAST MEDIA
    ADRIANA COBO FRENKEL; Fiscal Year: 1980
    ..Among the enzymes to be investigated are UDP-Glucuronyl Transferase (UDPGT) and the cytochrome P450 of liver microsomes...
  5. INHERITED DISORDERS OF BILIRUBIN GLUCURONIDATION
    Jayanta Roy Chowdhury; Fiscal Year: 1991
    ..toxins and drugs are converted to polar conjugates, primarily in the liver, by UDP-glucuronosyltransferase (UDPGT)-mediated glucuronidation prior to excretion in the bile or urine...
  6. JOHANNES NICOLAAS VAN DEN ANKER; Fiscal Year: 2014
    ..of developmental stage (defined by both gestational, and postnatal age) to UDP-glucuronosyltransferase 1A6 (UGT1A6) and sulfotransferase 1A1 (SULT1A1) activity. 2...
  7. 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...
  8. MEMBRANE BOUND DETOXICATION ENZYMES
    Richard Armstrong; Fiscal Year: 2000
    ..for the investigations of UDP- glucuronosyltransferase include: (I) optimization of the expression of the phenol UDPGT in a baculovirus-based or bacterial systems and ; (ii) an exploration of the conformer specificity of the enzyme ..
  9. Robert H Tukey; Fiscal Year: 2016
    DESCRIPTION (provided by applicant): In humans, the UGT1 locus encodes 9 functional UGT1A genes...
  10. Organ-specific Ugt1 profiling in detoxifying the anticancer drug CPT-11
    Shujuan Chen; Fiscal Year: 2013
    ..Recently, we have generated an Ugt1 conditional knockout mouse model targeting deletion of the Ugt1 locus specifically in liver tissue (Ugt1?Hep mice)...
  11. PROTECTION FROM BENZO(A)PYRENE TOXICITY BY OLTIPRAZ
    JOSEPH RITTER; Fiscal Year: 2000
    ..Specific Aim 3: To determine if the UGT2B1 or UGT1.6 isoform represents a BP 7,8-diol UGT...
  12. Peter Cresswell; Fiscal Year: 2016
    ..one, glucosidase II, that removes a terminal glucose residue, and a second, UDP-glucose glycoprotein transferase 1 (UGT1) that replaces the glucose when the glycoprotein bearing the glycan is improperly folded...
  13. Daniel N Hebert; Fiscal Year: 2016
    ..Persistent lectin chaperone binding is directed by UDP-glucose: glycoprotein glucosyltransferase (UGT1)...
  14. Inflamation and the Risk of Endometrial Cancer
    Akila Viswanathan; Fiscal Year: 2010
    ..The role of genetic polymorphisms of the enzymes CYP2C9 and UGT1A6 in the metabolism of aspirin in relation to its effect will be studied...
  15. 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)...
  16. 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...
  17. Aspirin pharmacogenetics in the Aspirin/Folate Polyp Prevention Trial
    KAREN MAKAR; Fiscal Year: 2009
    ..ALOX5);2) prostaglandin transport: multidrug resistance protein 4 (MRP4);and 3) aspirin metabolism: CYP2C9 and UGT1A6. We propose to genotype 1121 subjects who participated in a randomized controlled trial (the Aspirin/Folate Polyp ..
  18. UDP GLUCURONOSYLTRANSFERASES IN PHARMACOLOGY
    Thomas Tephly; Fiscal Year: 2002
    ..mRNA and glucuronidation activities for UGT2B7 and UGT1A6 have been found in human brain...
  19. 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...
  20. 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...
  21. 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 ..
  22. STRUCTURE-FUNCTION OF HUMAN UDP-GLUCURONOSYLTRANSFERASES
    Anna Radominska Pandya; Fiscal Year: 1999
    ..four recombinant human UGT isoenzyme; two physiologically important UGTs, UGT2B4 (hyodeoxycholic acid-specific and UGT1*1 bilirubin specific), as well as UGT*6 (small, planar phenol- specific and UGT2B10, a novel UGT of unknown ..
  23. GLUCURONIDATION OF DIETARY AND ENVIRONMENTAL CARCINOGENS
    Robert Tukey; Fiscal Year: 2002
    ....
  24. Bilirubin and Photobilirubin: Metabolism & Exretion
    Antony McDonagh; Fiscal Year: 2005
    ..The work will lead to safer more effective treatment of familial hyperbilirubinemia and jaundice in the newborn. ..
  25. Regulated Properties of the Human UGT1A1 Gene.
    Robert Tukey; Fiscal Year: 2006
    ..Identifying the mechanisms that underlie expression of UGT1A1 may provide us with important clues toward improving expression of this gene and avoiding potential toxicities because of inadequate gene expression. ..
  26. Breast Cancer, Benign Breast Disease, and Isoflavone Metabolism in Chinese Women
    Johanna Lampe; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable] [unreadable]..
  27. HOST GENES AND COLONIC BACTERIA--PROBING FOR INHERITANCE
    Johanna Lampe; Fiscal Year: 2002
    ..If we can establish that the equol-producer phenotype is an inherited trait, we can then work to identify the associated genotype and determine more effectively whether this is a biomarker of breast cancer risk. ..
  28. Serum IGFs--Effects of a Soy Intervention in Humans
    Johanna Lampe; Fiscal Year: 2002
    ..It provides an ideal design to evaluate the effects of isoflavones on the IGF system and to explore relationships between IGFs and colonic epithelial cell proliferation in humans. ..
  29. HUMAN HEPATIC & INTESTINAL UDP GLUCURONOSYLTRANSFERASES
    Anna Radominska Pandya; Fiscal Year: 2002
    ..abstract_text> ..
  30. Hormone Status Postmenopause: Colonic Bacterial Effects
    Johanna Lampe; Fiscal Year: 2003
    ..The results of this study will provide novel data regarding the relationship of the equol-producer phenotype, a marker of colonic nticrofloral environment, to lifetime estrogen exposure. ..
  31. GLUTATHIONE AND MITOCHONDRIA IN TOXIC RENAL INJURY
    Lawrence Lash; Fiscal Year: 2003
    ..This information may have therapeutic applications for prevention of renal cellular injury or for understanding mitochondrial diseases or age-related decreases that occur in mitochondrial function. ..
  32. Acetaminophen Pharmacogenetics
    Michael H Court; Fiscal Year: 2010
    ..1A6, and 1A9 as major APAP glucuronidation enzymes, and identified 3 linked amino acid polymorphisms in the UGT1A6 gene that alter APAP glucuronidation by recombinant enzyme, and also 3 linked SNPs in the 3'UTR region shared ..
  33. Coordinate Regulation of Uptake and Efflux Transporters
    Curtis D Klaassen; Fiscal Year: 2010
    ....
  34. Structure-Function of UDP-Glucuronosyltransferases
    Anna Radominska Pandya; Fiscal Year: 2009
    ..It will also serve as a basis in the search for new drugs and inhibitors of specific UGT isoforms, thus affecting drug therapy, drug-drug interactions, and the risk of chemically-induced diseases, including cancer. ..
  35. SYNTHETIC ANALOGS OF GLUCAGON FOR DIABETES STUDIES
    CECILIA UNSON; Fiscal Year: 2008
    ..abstract_text> ..
  36. Environmental Hormones: Effects on Thyroid Function
    Curtis Klaassen; Fiscal Year: 2005
    ..abstract_text> ..
  37. UGT Polymorphisms and Hormonally-Mediated Biomarkers in Premenopausal Women
    Johanna Lampe; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  38. FLAVONOID BIOAVAILABILITY IN HUMANS-CELLULAR STUDIES
    Thomas Walle; Fiscal Year: 2005
    ..The findings from the proposed studies should help us understand the bioavailability of the flavonoids, facilitating optimization of the chemopreventive utility of these natural or synthetic compounds. ..
  39. Metabolism and Carcinogenicity of Heterocyclic Amines
    TERRY ZENSER; Fiscal Year: 2007
    ..Determine effect of DSS-induced colitis inflammation) in IQ carcinogenicity. The long-term goal is to understand the role of RNOS on HCA carcinogenesis. ..
  40. DNA Damage: Fruit & Vegetable Effects in a Feeding Trial
    Johanna Lampe; Fiscal Year: 2005
    ..The existing intervention provides an ideal design in which to evaluate the relationships between biotransformation enzyme systems and DNA damage in humans. ..
  41. Diet and Risk of Ovarian Cancer
    Ellen Chang; Fiscal Year: 2005
    ..The results of the proposed analyses will provide further understanding of the etiology of ovarian cancer. ..
  42. Breast and Bone Density: Impact of Colonic Environment
    Johanna Lampe; Fiscal Year: 2006
    ..If equol-producer phenotype can predict differences in cumulative estrogen exposure / metabolism, it may serve as an early marker of breast cancer risk. ..
  43. GLUTATHIONE TRANSFERASES IN HUMANS: DIETARY INFLUENCES
    Johanna Lampe; Fiscal Year: 2006
    ..abstract_text> ..
  44. Mechanisms of adverse host responses to antibiotics
    Michael Court; Fiscal Year: 2006
    ..unreadable] [unreadable] [unreadable]..
  45. CYP1A1 GENE AND ENVIRONMENTAL TOXICITY
    Daniel Nebert; Fiscal Year: 2005
    ..abstract_text> ..
  46. HEPATOBILIARY DISPOSITION IN TOXICOLOGY
    Curtis Klaassen; Fiscal Year: 2003
    ..abstract_text> ..
  47. GENOTOXICITY IN CYP1A2 DEFICIENT TRANSGENIC MICE
    Daniel Nebert; Fiscal Year: 2002
    ..S. population. ..
  48. Regulation of Hepatic Excretion of Xenobiotics by Mrps
    Curtis D Klaassen; Fiscal Year: 2010
    ..Elucidation of the role of Nrf2 in the regulation of the efflux transport process will have significant ramifications in toxicology, xenobiotics disposition, drug-drug interaction, and cancer chemoprevention. ..
  49. Molecular Genetics of Cadmium Toxicity
    Daniel W Nebert; Fiscal Year: 2010
    ....
  50. PAHs: Balance of Detoxication vs Metabolic Activation
    Daniel Nebert; Fiscal Year: 2009
    ..dissemination of ingested BaP and will be informative in clinical studies in which we would determine which haplotypes of these three human genes might be associated with resistance vs. sensitivity to PAH-induced toxicity and cancer. ..
  51. Human Gut Microflora Profiling for Population Studies
    Johanna Lampe; Fiscal Year: 2006
    ..abstract_text> ..
  52. Glucuronidation in Humans--Genotypes and Phenotypes
    Johanna Lampe; Fiscal Year: 2004
    ..The randomized cross-over design will allow us to test efficiently for diet effects within individuals, as well as for gene-by-diet and sex-by-diet interactions. ..
  53. Interaction Between Irinotecan and Dietary Flavonoids
    Lalitha Iyer; Fiscal Year: 2004
    ....
  54. MOLECULAR TOXICOLOGY IN HUMAN KIDNEY CELLS
    Lawrence Lash; Fiscal Year: 2007
    ..Achievement of these aims should build on our previous work in human kidney cells and extend it to provide a much more complete understanding of the various and complex ways in which DCVC affects the human kidney [unreadable] [unreadable]..
  55. Aspirin use, genetic variation in aspirin related-genes, and Hodgkin lymphoma ris
    Ellen Chang; Fiscal Year: 2007
    ..CYP2C9 and/or UGT1A6 (genes involved in aspirin metabolism) is associated with risk of HL; and, further, 4...