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Genomes and Genes | B BurchellSummaryAffiliation: University of Dundee Country: UK Publications
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Molecular genetic basis of Gilbert's syndromeB Burchell
Department of Molecular and Cellular Pathology, Ninewells Medical School, The University, Dundee, Scotland
J Gastroenterol Hepatol 14:960-6. 1999..The genetic variation described as Gilbert's syndrome may lead to pharmacological variation in drug glucuronidation and unexpected toxicity from therapeutic agents...- Drug-mediated toxicity caused by genetic deficiency of UDP-glucuronosyltransferasesB Burchell
Department of Molecular Pathology, Ninewells Medical School, University of Dundee, Dundee, UK
Toxicol Lett 112:333-40. 2000..Recently, adverse effects of anticancer agents have been observed in Gilbert's patients due to reduced drug or bilirubin glucuronidation... - Genetic variation of human UDP-glucuronosyltransferase: implications in disease and drug glucuronidationBrian Burchell
Department of Molecular and Cellular Pathology, Ninewells Medical School, University of Dundee, Dundee, Scotland
Am J Pharmacogenomics 3:37-52. 2003..Additional novel polymorphisms in this gene family are yet to be revealed and studied, but will have a profound effect on the development of new drugs and therapies... - Gilbert's syndrome is a contributory factor in prolonged unconjugated hyperbilirubinemia of the newbornG Monaghan
Departments of Molecular and Cellular Pathology, Child Health, and Obstetrics and Gynaecology, University of Dundee, Ninewells Hospital and Medical School, Dundee, Scotland
J Pediatr 134:441-6. 1999..CONCLUSIONS: A genetic predisposition to develop prolonged neonatal hyperbilirubinemia in breast-fed infants is associated with TATA box polymorphism of the UGT1A1 gene and will be recognized as Gilbert's syndrome in adulthood... - Genetic defects of the UDP-glucuronosyltransferase-1 (UGT1) gene that cause familial non-haemolytic unconjugated hyperbilirubinaemiasD J Clarke
Department of Molecular and Cellular Pathology, University of Dundee, Ninewells Medical School, Scotland, UK
Clin Chim Acta 266:63-74. 1997..Current methods used for the diagnosis and treatment of these diseases are discussed... - Almokalant glucuronidation in human liver and kidney microsomes: evidence for the involvement of UGT1A9 and 2B7B K Gaiser
Department of Molecular and Cellular Pathology, Ninewells Medical School, University of Dundee DD1 9SY, UK
Xenobiotica 33:1073-83. 2003..68 and 1.06 mM almost identical to the 1A9. 4. The results suggest a significant role for UGT1A9 and 2B7 in the catalysis of almokalant glucuronidation... - Structure of the human UGT2B4 gene encoding a bile acid UDP-glucuronosyltransferaseG Monaghan
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, The University of Dundee, DD1 9SY, Scotland, UK
Mamm Genome 8:692-4. 1997 - Characterization of the uridine diphosphate-glucuronosyltransferase-catalyzing thyroid hormone glucuronidation in manK A Findlay
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, University of Dundee, Scotland
J Clin Endocrinol Metab 85:2879-83. 2000..Bioactive T3 is not significantly glucuronidated by these isoforms and other UGTs, and sulfotransferases may be involved... - In vitro analysis of human drug glucuronidation and prediction of in vivo metabolic clearanceM G Soars
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, Dundee, Scotland
J Pharmacol Exp Ther 301:382-90. 2002..The use of cryopreserved hepatocytes as an in vitro tool to predict in vivo metabolism was also assessed with an excellent correlation obtained for a number of extensively glucuronidated drugs (R(2) = 0.80, p < 0.001)... - 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 vitroL 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..Since this effect extends to heterologously expressed enzymes, it also provides an efficient means by which to increase the levels of recombinant ER proteins... - Drug glucuronidation by human renal UDP-glucuronosyltransferasesK A McGurk
Department of Molecular and Cellular Pathology, University of Dundee, Ninewells Hospital and Medical School, Scotland, UK
Biochem Pharmacol 55:1005-12. 1998..The human kidney was capable of conjugating various structurally diverse drugs and xenobiotics... 
Genetic and environmental factors associated with variation of human xenobiotic glucuronidation and sulfationB Burchell
Department of Biochemical Medicine, Ninewells Medical School, University, Dundee, Scotland, UK
Environ Health Perspect 105:739-47. 1997..This will leed to the better prediction of variation of xenobiotic glucuronidation and sulfation in man...- Evaluation of the marmoset as a model species for drug glucuronidationM G Soars
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, Dundee, UK
Xenobiotica 31:849-60. 2001.... - Cloning and characterization of a canine UDP-glucuronosyltransferaseM G Soars
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, Dundee, DD1 9SY, Scotland, UK
Arch Biochem Biophys 391:218-24. 2001..07 nmol/min/mg protein), a class of compounds extensively glucuronidated by human UGT1A6. Based on sequence homology and common catalytic activity, this dog UGT1A protein appears to be the canine orthologue of human UGT1A6... - Cloning and stable expression of a new member of the human liver phenol/bilirubin: UDP-glucuronosyltransferase cDNA familyR Wooster
Biochemical Medicine, University of Dundee, Ninewells Hospital and Medical School, Scotland, U K
Biochem J 278:465-9. 1991..These results suggest that the two isoenzymes may be derived from the same gene by differential splicing of the gene product... - Expression of a human liver cDNA encoding a UDP-glucuronosyltransferase catalysing the glucuronidation of hyodeoxycholic acid in cell cultureS Fournel-Gigleux
Department of Biochemistry, Medical Sciences Institute, The University, Dundee, Scotland
FEBS Lett 243:119-22. 1989..These results suggest that this UDPGT isoenzyme may be responsible for the glucuronidation of 6 alpha-hydroxy bile acids in human liver... - Cloning and substrate specificity of a human phenol UDP-glucuronosyltransferase expressed in COS-7 cellsD Harding
Department of Biochemistry, The University, Dundee, Scotland
Proc Natl Acad Sci U S A 85:8381-5. 1988..The glucuronidation of testosterone, androsterone, and estrone was not catalyzed by this cloned UDP-glucuronosyltransferase... - DD angiotensin-converting enzyme gene polymorphism is associated with endothelial dysfunction in normal humansR Butler
University Department of Clinical Pharmacology, Ninewells Hospital and Medical School, Dundee, UK
Hypertension 33:1164-8. 1999..These data demonstrate that the DD ACE genotype in a young population is associated with a blunting of stimulated endothelial NO and donated NO responses but not to non-NO vasodilators or vasoconstrictors... - Identification of an A-to-G missense mutation in exon 2 of the UGT1 gene complex that causes Crigler-Najjar syndrome type 2N Moghrabi
Department of Biochemical Medicine, University of Dundee, Ninewells Hospital and Medical School, Scotland, United Kingdom
Genomics 18:171-3. 1993 - Expression of human liver epoxide hydrolase in Saccharomyces pombeM R Jackson
Department of Biochemistry, The University, Scotland, U K
Biochem J 251:931-3. 1988..This method will provide a useful source of human liver epoxide hydrolase, avoiding the problems of obtaining human tissue... - Cloning and characterization of a novel human olfactory UDP-glucuronosyltransferaseG Jedlitschky
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, University of Dundee, Dundee DD1 9SY, Scotland, UK
Biochem J 340:837-43. 1999..Furthermore, some steroids, especially androgens, some drugs and carcinogens were conjugated. The results support a role of the enzyme in olfactory perception and in protection of the neural system against airborne hazardous chemicals... - Isolation of a human YAC contig encompassing a cluster of UGT2 genes and its regional localization to chromosome 4q13G Monaghan
Department of Biochemical Medicine, University of Dundee, Ninewells Hospital Medical School, Scotland, United Kingdom
Genomics 23:496-9. 1994..These data permitted a provisional ordering of the genes as UGT2B9-UGT2B4-UGT2B15. Fluorescence in situ hybridization analysis, using the YAC DNA, permitted the regional localization of this gene cluster to chromosome 4q13... - Characterisation of glucuronidation and transport in V79 cells co-expressing UGT1A1 and MRP1R L Cuff
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, University of Dundee, Scotland DD1 9SY, Dundee, UK
Toxicol Lett 120:43-9. 2001..V79 cells expressing both UGT1A1 and MRP1 have been established. The ability of these cell lines to both glucuronidate and transport compounds was assessed ex vivo using estradiol and bilirubin as substrates... - Use of cloned and expressed human UDP-glucuronosyltransferases for the assessment of human drug conjugation and identification of potential drug interactionsB T Ethell
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, University of Dundee, Dundee, Scotland
Drug Metab Dispos 29:48-53. 2001..This study shows the utility of the expressed human UDP-glucuronosyltransferases in determining substrate structure-activity relationships and potential drug-drug interactions... - Merits and limitations of recombinant models for the study of human P450-mediated drug metabolism and toxicity: an intralaboratory comparisonT Friedberg
Biomedical Research Centre, University of Dundee, Ninewells Hospital and Medical School, Scotland, UK
Drug Metab Rev 31:523-44. 1999..For toxicological studies, however, expression of P450s in mammalian cells was most appropriate. This is exemplified here by studies into the role of human P450s in the activation and inactivation of chemotherapeutic drugs... - Cloning and functional expression of an apparent splice variant of the murine 5-HT3 receptor A subunitA G Hope
Department of Biochemical Medicine, Ninewells Hospital and Medical School, Dundee, UK
Eur J Pharmacol 245:187-92. 1993..Upon expression in Xenopus oocytes, the homo-oligomeric receptor displayed pharmacological properties which define it as a functional 5-HT3 receptor... - The UDP glucuronosyltransferase gene superfamily: suggested nomenclature based on evolutionary divergenceB Burchell
Department of Biochemical Medicine, Ninewells Hospital and Medical School, Dundee, Scotland
DNA Cell Biol 10:487-94. 1991..We suggest that the human nomenclature system be used for species other than the mouse. We anticipate that this UGT gene nomenclature system will require updating on a regular basis... - Chromosomal assignment of human phenol and bilirubin UDP-glucuronosyltransferase genes (UGT1A-subfamily)N Moghrabi
University Department of Biochemical Medicine, Ninewells Hospital and Medical School, Dundee, Scotland
Ann Hum Genet 56:81-91. 1992..The results obtained indicate that all four cDNA clones are encoded by gene(s) located on human chromosome 2... - Nucleotide and deduced amino acid sequence of human liver microsomal epoxide hydrolaseM R Jackson
Department of Biochemistry, University of Dundee, UK
Nucleic Acids Res 15:7188. 1987 - Farnesol is glucuronidated in human liver, kidney and intestine in vitro, and is a novel substrate for UGT2B7 and UGT1A1Adam G Staines
Division of Pathology and Neuroscience, Ninewells Hospital and Medical School, University of Dundee, Dundee DD1 9SY, Scotland, UK
Biochem J 384:637-45. 2004..Thus glucuronidation may modulate the physiological and/or pharmacological properties of this potent signalling molecule... - Glucuronidation of HMR1098 in human microsomes: evidence for the involvement of UGT1A1 in the formation of S-glucuronidesBrian T Ethell
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, University of Dendee, Dundee, Scotland, DD1 9SY, UK
Drug Metab Dispos 31:1027-34. 2003.... - The effect of valproic acid on drug and steroid glucuronidation by expressed human UDP-glucuronosyltransferasesBrian T Ethell
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, University of Dundee, DD1 9SY, Scotland, Dundee, UK
Biochem Pharmacol 65:1441-9. 2003..No significant inhibition of UGT1A1 or UGT1A6 by valproic acid was observed. These data indicate that valproic acid inhibition of glucuronidation reactions is not always due to simple competitive inhibition of substrates... - Cloning and characterisation of the first drug-metabolising canine UDP-glucuronosyltransferase of the 2B subfamilyMatthew G Soars
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, Dundee, DD1 9SY, Scotland, UK
Biochem Pharmacol 65:1251-9. 2003..The results suggest that UGT2B31 plays a crucial role in drug detoxification by the dog and may be the canine equivalent of human UGT2B7... - Substrate specificity of human hepatic udp-glucuronosyltransferasesBrian Burchell
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, University of Dundee, Scotland, United Kingdom
Methods Enzymol 400:46-57. 2005..Specific substrates for the five individual UGTs have been identified. These five probe substrates could be used to predict the drug clearance catalyzed by individual UGTs in vivo... - Quantitative structure activity relationships for the glucuronidation of simple phenols by expressed human UGT1A6 and UGT1A9Brian T Ethell
Department of Molecular and Cellular Pathology, Ninewells Hospital and Medical School, Dundee, United Kingdom
Drug Metab Dispos 30:734-8. 2002..The K(m) values for UGT1A9 showed a similar relationship to UGT1A6 but with much lower K(m) values and greater variability in range of this value... - N-glucuronidation of carbamazepine in human tissues is mediated by UGT2B7Adam G Staines
Division of Pathology and Neuroscience, Ninewells Hospital and Medical School, University of Dundee, Dundee DD1 9SY, Scotland, UK
J Pharmacol Exp Ther 311:1131-7. 2004..79 pmol/mg/min. In addition to revealing the isoform responsible for CBZ glucuronidation, this is the first example of primary amine glucuronidation by UGT2B7... - Molecular and functional characterization of microsomal UDP-glucuronic acid uptake by members of the nucleotide sugar transporter (NST) familyTsutomu Kobayashi
Division of Pathology and Neuroscience, University of Dundee, Ninewells Hospital and Medical School, Dundee DD1 9SY, Scotland, UK
Biochem J 400:281-9. 2006..The cell line H4IIE is a useful model for the study of UDPGA transporters for glucuronidation reactions... - Nomenclature update for the mammalian UDP glycosyltransferase (UGT) gene superfamilyPeter I Mackenzie
Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Center, Bedford Park, Australia
Pharmacogenet Genomics 15:677-85. 2005..Most UGT1 and UGT8 enzymes have been characterized in detail; however, the catalytic functions of the UGT3A enzymes and several UGT2 enzymes remain to be characterized... - Amino terminal domains of human UDP-glucuronosyltransferases (UGT) 2B7 and 2B15 associated with substrate selectivity and autoactivationBenjamin C Lewis
Department of Clinical Pharmacology, Flinders University and Flinders Medical Centre, Adelaide, Australia
Biochem Pharmacol 73:1463-73. 2007.... - Assessment of catechol induction and glucuronidation in rat liver microsomesEivor Elovaara
Department of Industrial Hygiene and Toxicology, Finnish Institute of Occupational Health, FIN 00250 Helsinki, Finland
Drug Metab Dispos 32:1426-33. 2004..6 nmol/min/mg). In conclusion, catechols are poor inducers of their own glucuronidation supported by several UGT isoforms. Their administration is unlikely to affect the glucuronidation of other drugs administered concomitantly... - Identification of the human liver UDP-glucuronosyltransferase involved in the metabolism of p-ethoxyphenylurea (dulcin)Yoshihiro Uesawa
Department of Pharmaceutics, Clinical Pharmaceutics Laboratory, Meiji Pharmaceutical University, 2 522 1 Noshio, Kiyose, Tokyo, 204 8588, Japan
Arch Toxicol 81:163-8. 2007..356 mM), but bilirubin, a substrate for UGT1A1, did not. These results suggest that UGT1A9 is a key enzyme catalyzing the glucuronidation of DL... - Identification of the rabbit liver UDP-glucuronosyltransferase catalyzing the glucuronidation of 4-ethoxyphenylurea (dulcin)Yoshihiro Uesawa
Clinical Pharmaceutics Laboratory, Department of Pharmaceutics, Meiji Pharmaceutical University, 2 522 1 Noshio, Kiyose, Tokyo 204 8588, Japan
Drug Metab Dispos 32:1476-81. 2004..Octylgallate was further shown to competitively inhibit DNG production by RabLM (Ki = 0.149 mM). These results demonstrate that UGT1A7 is the major isoform catalyzing the N-glucuronidation of DL in RabLM... - Glucuronidation of SN-38 and NU/ICRF 505 in human colon cancer and adjacent normal colonJeffrey Cummings
Cancer Research UK, Edinburgh Oncology Unit, Western General Hospital, Edinburgh, UK
Anticancer Res 26:2189-96. 2006..To safely reverse this mechanism in vivo, it is essential to identify which isoforms of UDP-glucuronosyltransferases are responsible for catalysing this drug metabolism in tumour tissue... - Glucuronidation as a mechanism of intrinsic drug resistance in human colon cancer: reversal of resistance by food additivesJeffrey Cummings
Cancer Research UK, Edinburgh Oncology Unit, Western General Hospital, Edinburgh, United Kingdom
Cancer Res 63:8443-50. 2003..Glucuronidation may represent a mechanism of intrinsic drug resistance in colon cancer open to modulation by a range of food additives and proprietary medicines... - Conjugation of catechols by recombinant human sulfotransferases, UDP-glucuronosyltransferases, and soluble catechol O-methyltransferase: structure-conjugation relationships and predictive modelsJyrki Taskinen
Department of Pharmacy, University of Helsinki, Helsinki, Finland
Drug Metab Dispos 31:1187-97. 2003..Several structural factors governing the conjugation of catechol hormones, metabolites, and drugs were identified. The results have significant implications for predicting the metabolic fate of catechols... - Glucuronidation of catechols by human hepatic, gastric, and intestinal microsomal UDP-glucuronosyltransferases (UGT) and recombinant UGT1A6, UGT1A9, and UGT2B7Laurence Antonio
UMR 7561 CNRS University Henri Poincaré Nancy I, Vandoeuvre les Nancy, France
Arch Biochem Biophys 411:251-61. 2003..51 to 64.0 nmol/mgprotein x min. These results demonstrate for the first time glucuronidation of catechols by gastric and intestinal microsomal UGTs and three human recombinant UGT isoforms... - Glucuronidation of dihydroartemisinin in vivo and by human liver microsomes and expressed UDP-glucuronosyltransferasesKenneth F Ilett
Department of Pharmacology, University of Western Australia, Crawley, Western Australia
Drug Metab Dispos 30:1005-12. 2002..There was no significant metabolism of DHA by cytochrome-P450 oxidation or by cytosolic sulfotransferases. We conclude that alpha-DHA-G is an important metabolite of DHA in humans and that its formation is catalyzed by UGT1A9 and UGT2B7... - Histone 2A stimulates glucose-6-phosphatase activity by permeabilization of liver microsomesAngelo Benedetti
Dipartimento di Fisiopatologia e Medicina Sperimentale, University of Siena, 53100 Siena, Italy
Biochem J 367:505-10. 2002..Finally, histone 2A renders microsomal vesicles permeable to non-permeant compounds. Taken together, the results demonstrate that histone 2A stimulates glucose-6-phosphatase activity by permeabilizing the microsomal membrane... - The importance of cysteine 126 in the human liver UDP-glucuronosyltransferase UGT1A6Claire Senay
UMR 7561 CNRS Université Henri Poincaré Nancy 1, Faculte de Medecine, 9, avenue de la Forêt de Haye, BP184 54505 Vandoeuvre lès Nancy Cedex, France
Biochim Biophys Acta 1597:90-6. 2002..These results support the conclusion that Cys126 is an essential residue for the integrity of the substrate binding site of UGT1A6... - Tissue-specific regulation of canine intestinal and hepatic phenol and morphine UDP-glucuronosyltransferases by beta-naphthoflavone in comparison with humansKarl Walter Bock
Institute of Toxicology, University of Tubingen, Tubingen, Germany
Biochem Pharmacol 63:1683-90. 2002..The results suggest marked differences in tissue-specific regulation of canine vs. human hepatic and intestinal phenol or morphine UGTs... - Ethanol-dependent induction of bilirubin UDP-glucuronosyl-transferase in rat liver is mediated by Kupffer cellsTamas Kardon
Department of Medical Chemistry, Semmelweis University, Budapest, Hungary
Life Sci 70:1205-12. 2002..These results suggest that Kupffer cells play a major role in the mediation of ethanol-stimulated induction of UGT1A1 in liver parenchymal cells... - Characterization of catechol glucuronidation in rat liverLaurence Antonio
, , France
Drug Metab Dispos 30:199-207. 2002..Hydrogen bonding and steric effects also were important to account for to predict the glucuronidation rates...