Peter Mackenzie

Summary

Affiliation: Flinders University
Country: Australia

Publications

  1. ncbi request reprint Nomenclature update for the mammalian UDP glycosyltransferase (UGT) gene superfamily
    Peter I Mackenzie
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Center, Bedford Park, Australia
    Pharmacogenet Genomics 15:677-85. 2005
  2. ncbi request reprint Polymorphisms in UDP glucuronosyltransferase genes: functional consequences and clinical relevance
    P I Mackenzie
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Adelaide, SA, Australia
    Clin Chem Lab Med 38:889-92. 2000
  3. ncbi request reprint Polymorphic variations in the expression of the chemical detoxifying UDP glucuronosyltransferases
    P I Mackenzie
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Toxicol Appl Pharmacol 207:77-83. 2005
  4. doi request reprint The novel UDP glycosyltransferase 3A2: cloning, catalytic properties, and tissue distribution
    Peter I Mackenzie
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, SA, Australia
    Mol Pharmacol 79:472-8. 2011
  5. pmc Identification of UDP glycosyltransferase 3A1 as a UDP N-acetylglucosaminyltransferase
    Peter I Mackenzie
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    J Biol Chem 283:36205-10. 2008
  6. ncbi request reprint Regulation of UDP glucuronosyltransferase genes
    P I Mackenzie
    Department of Clinical Pharmacology, Flinders Medical Research Institute, Flinders University, Bedford Park, SA 5042, Australia
    Curr Drug Metab 4:249-57. 2003
  7. ncbi request reprint Glucosidation of hyodeoxycholic acid by UDP-glucuronosyltransferase 2B7
    Peter Mackenzie
    Department of Clinical Pharmacology, Flinders University and Flinders Medical Center, Bedford Park, SA 5042, Australia
    Biochem Pharmacol 65:417-21. 2003
  8. doi request reprint The regulation of UDP-glucuronosyltransferase genes by tissue-specific and ligand-activated transcription factors
    Peter I Mackenzie
    Department of Clinical Pharmacology, Flinders Medical Science and Technology, Flinders University, Adelaide, South Australia, Australia
    Drug Metab Rev 42:99-109. 2010
  9. pmc Human PXR variants and their differential effects on the regulation of human UDP-glucuronosyltransferase gene expression
    Dione Gardner-Stephen
    Department of Clinical Pharmacology, Flinders University, Flinders Medical Centre, South Australia, Australia
    Drug Metab Dispos 32:340-7. 2004
  10. doi request reprint Kinetic modeling of the interactions between 4-methylumbelliferone, 1-naphthol, and zidovudine glucuronidation by udp-glucuronosyltransferase 2B7 (UGT2B7) provides evidence for multiple substrate binding and effector sites
    Verawan Uchaipichat
    Department of Clinical Pharmacology, Flinders University, Flinders Medical Centre, Adelaide, Australia
    Mol Pharmacol 74:1152-62. 2008

Collaborators

Detail Information

Publications54

  1. ncbi request reprint Nomenclature update for the mammalian UDP glycosyltransferase (UGT) gene superfamily
    Peter 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...
  2. ncbi request reprint Polymorphisms in UDP glucuronosyltransferase genes: functional consequences and clinical relevance
    P I Mackenzie
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Adelaide, SA, Australia
    Clin Chem Lab Med 38:889-92. 2000
    ..g. UGT1A1 and bilirubin) or is the predominant or only UGT present in the cell, it is unlikely that these polymorphisms will be of major clinical significance...
  3. ncbi request reprint Polymorphic variations in the expression of the chemical detoxifying UDP glucuronosyltransferases
    P I Mackenzie
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Toxicol Appl Pharmacol 207:77-83. 2005
    ....
  4. doi request reprint The novel UDP glycosyltransferase 3A2: cloning, catalytic properties, and tissue distribution
    Peter I Mackenzie
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, SA, Australia
    Mol Pharmacol 79:472-8. 2011
    ..The broad substrate and novel UDP sugar specificity of UGT3A2 would be advantageous for such a function...
  5. pmc Identification of UDP glycosyltransferase 3A1 as a UDP N-acetylglucosaminyltransferase
    Peter I Mackenzie
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    J Biol Chem 283:36205-10. 2008
    ..Its activity and distribution suggest that UGT3A1 may have an important role in the metabolism and elimination of ursodeoxycholic acid in therapies for ameliorating the symptoms of cholestasis or for dissolving gallstones...
  6. ncbi request reprint Regulation of UDP glucuronosyltransferase genes
    P I Mackenzie
    Department of Clinical Pharmacology, Flinders Medical Research Institute, Flinders University, Bedford Park, SA 5042, Australia
    Curr Drug Metab 4:249-57. 2003
    ..These proteins include the Ah receptor, members of the nuclear receptor superfamily, such as CAR and PXR and transcription factors that respond to stress...
  7. ncbi request reprint Glucosidation of hyodeoxycholic acid by UDP-glucuronosyltransferase 2B7
    Peter Mackenzie
    Department of Clinical Pharmacology, Flinders University and Flinders Medical Center, Bedford Park, SA 5042, Australia
    Biochem Pharmacol 65:417-21. 2003
    ..The two polymorphic variants of UGT2B7, UGT2B7(*)1 and UGT2B7(*)2 could both glucosidate HDCA. This is the first report that identifies UGT2B7 as the enzyme responsible for the glucosidation of the bile acid, HDCA...
  8. doi request reprint The regulation of UDP-glucuronosyltransferase genes by tissue-specific and ligand-activated transcription factors
    Peter I Mackenzie
    Department of Clinical Pharmacology, Flinders Medical Science and Technology, Flinders University, Adelaide, South Australia, Australia
    Drug Metab Rev 42:99-109. 2010
    ....
  9. pmc Human PXR variants and their differential effects on the regulation of human UDP-glucuronosyltransferase gene expression
    Dione Gardner-Stephen
    Department of Clinical Pharmacology, Flinders University, Flinders Medical Centre, South Australia, Australia
    Drug Metab Dispos 32:340-7. 2004
    ..The data suggest that individual variation in PXR expression may account for differential expression of some UGT isoforms between subjects...
  10. doi request reprint Kinetic modeling of the interactions between 4-methylumbelliferone, 1-naphthol, and zidovudine glucuronidation by udp-glucuronosyltransferase 2B7 (UGT2B7) provides evidence for multiple substrate binding and effector sites
    Verawan Uchaipichat
    Department of Clinical Pharmacology, Flinders University, Flinders Medical Centre, Adelaide, Australia
    Mol Pharmacol 74:1152-62. 2008
    ..The multiplicity of binding and effector sites results in complex kinetic interactions between UGT2B7 substrates, which potentially complicates inhibition screening studies...
  11. ncbi request reprint Influence of mutations associated with Gilbert and Crigler-Najjar type II syndromes on the glucuronidation kinetics of bilirubin and other UDP-glucuronosyltransferase 1A substrates
    Wandee Udomuksorn
    Department of Clinical Pharmacology, Flinders University and Flinders Medical Centre, Adelaide, South Australia, Australia
    Pharmacogenet Genomics 17:1017-29. 2007
    ....
  12. doi request reprint 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
    ....
  13. ncbi request reprint Binding of inhibitory fatty acids is responsible for the enhancement of UDP-glucuronosyltransferase 2B7 activity by albumin: implications for in vitro-in vivo extrapolation
    Andrew Rowland
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    J Pharmacol Exp Ther 321:137-47. 2007
    ..It is postulated that BSA and HSA-FAF sequester inhibitory fatty acids released during incubations, and the apparent high Km values observed for UGT2B7 substrates arise from the presence of these endogenous inhibitors...
  14. ncbi request reprint In vitro-in vivo correlation for drugs and other compounds eliminated by glucuronidation in humans: pitfalls and promises
    John O Miners
    Department of Clinical Pharmacology, Flinders University and Flinders Medical Centre, Adelaide, Australia
    Biochem Pharmacol 71:1531-9. 2006
    ....
  15. ncbi request reprint In vitro characterization of lamotrigine N2-glucuronidation and the lamotrigine-valproic acid interaction
    Andrew Rowland
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Drug Metab Dispos 34:1055-62. 2006
    ..These data indicate that UGT2B7 and UGT1A4 are responsible for the Hill and Michaelis-Menten components, respectively, of microsomal LTG N2-glucuronidation, and the LTG-VPA interaction in vivo arises from inhibition of UGT2B7...
  16. ncbi request reprint Recent advances in the in silico modelling of UDP glucuronosyltransferase substrates
    Michael J Sorich
    Sansom Institute, University of South Australia, Adelaide, SA 5000, Australia
    Curr Drug Metab 9:60-9. 2008
    ..Furthermore, improved protein structure data on UGTs will enable the application of structural modelling techniques likely leading to greater insight into the binding and reactive processes of UGT catalysed glucuronidation...
  17. doi request reprint The prediction of drug-glucuronidation parameters in humans: UDP-glucuronosyltransferase enzyme-selective substrate and inhibitor probes for reaction phenotyping and in vitro-in vivo extrapolation of drug clearance and drug-drug interaction potential
    John O Miners
    Department of Clinical Pharmacology, Flinders University School of Medicine, Adelaide, Australia
    Drug Metab Rev 42:196-208. 2010
    ..Additionally, in vitro experimental approaches and scaling strategies have been successfully applied to the quantitative prediction of in vivo clearance via glucuronidation and drug-drug interaction potential...
  18. doi request reprint UGT3A: novel UDP-glycosyltransferases of the UGT superfamily
    Robyn Meech
    Department of Clinical Pharmacology, Flinders University of South Australia, Bedford Park, South Australia, Australia
    Drug Metab Rev 42:45-54. 2010
    ..We also review recently published work that has revealed that one member of this family, UGT3A1, has a unique enzymatic function: N-acetylglucosaminidation. Finally, we discuss the possible biological significance of the UGT3A enzymes...
  19. ncbi request reprint Critical roles of residues 36 and 40 in the phenol and tertiary amine aglycone substrate selectivities of UDP-glucuronosyltransferases 1A3 and 1A4
    Takahiro Kubota
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Mol Pharmacol 72:1054-62. 2007
    ..Thus, residues 36 and 40 of UGT1A3 and UGT1A4 are pivotal for the respective selectivities of these enzymes toward planar phenols and tertiary amines, although other regions of the proteins influence binding affinity and/or turnover...
  20. ncbi request reprint Coordinate regulation of the human UDP-glucuronosyltransferase 1A8, 1A9, and 1A10 genes by hepatocyte nuclear factor 1alpha and the caudal-related homeodomain protein 2
    Philip A Gregory
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, South Australia 5042, Australia
    Mol Pharmacol 65:953-63. 2004
    ..These studies provide insight into the mechanisms controlling the extrahepatic expression of the UGT1A8, -1A9, and -1A10 genes...
  21. ncbi request reprint Predicting human drug glucuronidation parameters: application of in vitro and in silico modeling approaches
    John O Miners
    Department of Clinical Pharmacology, Flinders University and Flinders Medical Center, Bedford Park, Adelaide, SA 5042, Australia
    Annu Rev Pharmacol Toxicol 44:1-25. 2004
    ..This review assesses the utility of in vitro and in silico approaches for the qualitative and quantitative prediction of drug glucuronidation parameters and the challenges facing the development of generalizable models...
  22. ncbi request reprint Cloning and characterization of the human UDP-glucuronosyltransferase 1A8, 1A9, and 1A10 gene promoters: differential regulation through an interior-like region
    Philip A Gregory
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Bedford Park, South Australia 5042, Australia
    J Biol Chem 278:36107-14. 2003
    ..These results provide evidence that the UGT1A8, 1A9, and 1A10 genes are differentially regulated through an initiator element in their 5'-flanking regions...
  23. ncbi request reprint Isoform selectivity and kinetics of morphine 3- and 6-glucuronidation by human udp-glucuronosyltransferases: evidence for atypical glucuronidation kinetics by UGT2B7
    Andrew N Stone
    Department of Clinical Pharmacology, Flinders Medical Centre, Adelaide, Australia
    Drug Metab Dispos 31:1086-9. 2003
    ....
  24. ncbi request reprint Genetic polymorphisms of UDP-glucuronosyltransferases and their functional significance
    John O Miners
    Department of Clinical Pharmacology, Flinders Medical Centre and Flinders University School of Medicine, Bedford Park, Adelaide, SA, Australia
    Toxicology 181:453-6. 2002
    ..It has been proposed on the basis of altered catalytic activity of mutants of UGT 1A6, 1A7 and 2B15 that genetic polymorphism of these forms may be of toxicological significance, but this is yet to be proven...
  25. ncbi request reprint Human udp-glucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid
    Verawan Uchaipichat
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Drug Metab Dispos 32:413-23. 2004
    ..Overall, the results emphasize the need for the careful design and interpretation of kinetic and inhibition studies with human UGTs...
  26. doi request reprint 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
    ..Only BSA caused a similar effect on 4MU glucuronidation by UGT1A1. It is concluded that BSA and HSAFAF reduce the K(m) values of only those enzymes inhibited by long-chain unsaturated fatty acids...
  27. ncbi request reprint Selectivity of substrate (trifluoperazine) and inhibitor (amitriptyline, androsterone, canrenoic acid, hecogenin, phenylbutazone, quinidine, quinine, and sulfinpyrazone) "probes" for human udp-glucuronosyltransferases
    Verawan Uchaipichat
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Drug Metab Dispos 34:449-56. 2006
    ..Amitriptyline, androsterone, canrenoic acid, hecogenin, phenylbutazone, quinidine, quinine, and sulfinpyrazone are nonselective UGT inhibitors...
  28. ncbi request reprint Hepatocyte nuclear factor1 transcription factors are essential for the UDP-glucuronosyltransferase 1A9 promoter response to hepatocyte nuclear factor 4alpha
    Dione A Gardner-Stephen
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, South Australia, Australia
    Pharmacogenet Genomics 17:25-36. 2007
    ..The discovery of two unique and cooperative liver-enriched transcription factor binding sites in the UGT1A9 promoter is a significant step towards understanding the unique hepatic expression of UGT1A9 amongst the UGT1A7-10 gene cluster...
  29. ncbi request reprint Sulfinpyrazone C-glucuronidation is catalyzed selectively by human UDP-glucuronosyltransferase 1A9
    Oranun Kerdpin
    Department of Clinical Pharmacology, Flinders University and Flinders Medical Centre, Bedford Park, Adelaide, Australia
    Drug Metab Dispos 34:1950-3. 2006
    ..The data indicate that UGT1A9 is the enzyme responsible for hepatic SFZ C-glucuronidation and that SFZ may be used as a substrate "probe" for UGT1A9 activity in HLMs...
  30. ncbi request reprint Amino terminal domains of human UDP-glucuronosyltransferases (UGT) 2B7 and 2B15 associated with substrate selectivity and autoactivation
    Benjamin C Lewis
    Department of Clinical Pharmacology, Flinders University and Flinders Medical Centre, Adelaide, Australia
    Biochem Pharmacol 73:1463-73. 2007
    ....
  31. ncbi request reprint Carboxylic acid drug-induced DNA nicking in HEK293 cells expressing human UDP-glucuronosyltransferases: role of acyl glucuronide metabolites and glycation pathways
    Hamish T Southwood
    Department of Cardiology and Clinical Pharmacology, The Queen Elizabeth Hospital, and Discipline of Pharmacology, School of Medical Sciences, University of Adelaide, Adelaide, SA 5000, Australia
    Chem Res Toxicol 20:1520-7. 2007
    ..This study demonstrates the substrate-dependent role of human UGTs in the bioactivation of carboxylic acid drugs to genotoxic acyl glucuronide metabolites that are able to damage nuclear DNA via glycation and/or glycoxidation mechanisms...
  32. ncbi request reprint Regulation of UDP glucuronosyltransferases in the gastrointestinal tract
    Philip A Gregory
    Department of Clinical Pharmacology, Flinders Medical Centre, Flinders University School of Medicine, Bedford Park, South Australia, 5042
    Toxicol Appl Pharmacol 199:354-63. 2004
    ..In turn, this will lead to further understanding of interindividual variation in the capacity of the GI tract to metabolize lipophilic chemicals and to act as a barrier to dietary toxins and orally administered drugs...
  33. pmc Quantitative prediction of in vivo inhibitory interactions involving glucuronidated drugs from in vitro data: the effect of fluconazole on zidovudine glucuronidation
    Verawan Uchaipichat
    Department of Clinical Pharmacology, Flinders University and Flinders Medical Centre, Adelaide, SA, Australia
    Br J Clin Pharmacol 61:427-39. 2006
    ....
  34. ncbi request reprint Identification and characterization of functional hepatocyte nuclear factor 1-binding sites in UDP-glucuronosyltransferase genes
    Dione A Gardner-Stephen
    Department of Clinical Oncology, Flinders University School of Medicine, Flinders Medical Center, Adelaide, Australia
    Methods Enzymol 400:22-46. 2005
    ..Finally, possible scenarios in which HNF1-mediated regulation of UGT expression may be clinically relevant are suggested...
  35. ncbi request reprint The homeodomain Pbx2-Prep1 complex modulates hepatocyte nuclear factor 1alpha-mediated activation of the UDP-glucuronosyltransferase 2B17 gene
    Philip A Gregory
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Adelaide, Australia
    Mol Pharmacol 62:154-61. 2002
    ..Modulation of transcription by restricting the binding of transcriptional effectors to their target site is a novel role for Pbx2-Prep1 complexes...
  36. doi request reprint A novel polymorphism in a forkhead box A1 (FOXA1) binding site of the human UDP glucuronosyltransferase 2B17 gene modulates promoter activity and is associated with altered levels of circulating androstane-3α,17β-diol glucuronide
    Dong Gui Hu
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Bedford Park SA 5042, Australia
    Mol Pharmacol 78:714-22. 2010
    ..In summary, this work identifies FOXA1 as an important regulator of UGT2B17 expression in prostate cancer LNCaP cells and identifies a polymorphism that alters this regulation...
  37. doi request reprint Characterization of the binding of drugs to human intestinal fatty acid binding protein (IFABP): potential role of IFABP as an alternative to albumin for in vitro-in vivo extrapolation of drug kinetic parameters
    Andrew Rowland
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Drug Metab Dispos 37:1395-403. 2009
    ..5 versus 1-1.5% for BSA) was necessary for a 10-fold reduction in this parameter. The results indicate that IFABP is likely to have advantages over BSA in microsomal kinetic studies with drugs that bind extensively to albumin...
  38. ncbi request reprint The caudal-related homeodomain protein Cdx2 and hepatocyte nuclear factor 1alpha cooperatively regulate the UDP-glucuronosyltransferase 2B7 gene promoter
    Philip A Gregory
    Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Pharmacogenet Genomics 16:527-36. 2006
    ..The demonstration that Cdx2 and HNF1alpha are important regulators of UGT2B7 expression will aid in defining pathways for coordinate control of drug metabolism in the gastrointestinal tract...
  39. pmc S-Naproxen and desmethylnaproxen glucuronidation by human liver microsomes and recombinant human UDP-glucuronosyltransferases (UGT): role of UGT2B7 in the elimination of naproxen
    Kushari Bowalgaha
    Department of Clinical Pharmacology, Flinders University and Flinders Medical Centre, Bedford Park, Adelaide, Australia
    Br J Clin Pharmacol 60:423-33. 2005
    ..To characterize the kinetics of S-naproxen ('naproxen') acyl glucuronidation and desmethylnaproxen acyl and phenolic glucuronidation by human liver microsomes and identify the human UGT isoform(s) catalysing these reactions...
  40. ncbi request reprint Isolation of the UDP-glucuronosyltransferase 1A3 and 1A4 proximal promoters and characterization of their dependence on the transcription factor hepatocyte nuclear factor 1alpha
    Dione A Gardner-Stephen
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, South Australia 5042, Australia
    Drug Metab Dispos 35:116-20. 2007
    ..This study suggests an important role for HNF1alpha in the transcriptional regulation of the human UGT1A3 and UGT1A4 genes...
  41. doi request reprint Estrogen receptor alpha, fos-related antigen-2, and c-Jun coordinately regulate human UDP glucuronosyltransferase 2B15 and 2B17 expression in response to 17beta-estradiol in MCF-7 cells
    Dong Gui Hu
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, SA, Australia
    Mol Pharmacol 76:425-39. 2009
    ..Because UGT2B15 and UGT2B17 inactivate steroid hormones by glucuronidation, the regulation of their genes by 17beta-estradiol may maintain steroid hormone homeostasis and prevent excessive estrogen signaling activity...
  42. doi request reprint The "albumin effect" and in vitro-in vivo extrapolation: sequestration of long-chain unsaturated fatty acids enhances phenytoin hydroxylation by human liver microsomal and recombinant cytochrome P450 2C9
    Andrew Rowland
    Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, SA 5042, Australia
    Drug Metab Dispos 36:870-7. 2008
    ..The results indicate that previously determined in vitro K(m) values for CYP2C9 substrates are almost certainly overestimates, and accurate in vitro-in vivo extrapolation of kinetic data for CYP2C9 substrates is achievable...
  43. ncbi request reprint Inhibition of UDP-glucuronosyltransferase 2b7-catalyzed morphine glucuronidation by ketoconazole: dual mechanisms involving a novel noncompetitive mode
    Shuso Takeda
    Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Drug Metab Dispos 34:1277-82. 2006
    ....
  44. ncbi request reprint Interactions with other human UDP-glucuronosyltransferases attenuate the consequences of the Y485D mutation on the activity and substrate affinity of UGT1A6
    Mika Kurkela
    Drug Discovery and Development Technology Center DDTC and Division of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland
    Pharmacogenet Genomics 17:115-26. 2007
    ..It is unknown, however, if this mutation results in clinical conditions, other than impaired bilirubin conjugation by UGT1A1...
  45. ncbi request reprint Protein-protein interactions between rat hepatic cytochromes P450 (P450s) and UDP-glucuronosyltransferases (UGTs): evidence for the functionally active UGT in P450-UGT complex
    Yuji Ishii
    Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Drug Metab Pharmacokinet 22:367-76. 2007
    ..Thus, CYP2C11/13 could associate with UGTs, but the affinity is assumed to be weaker than that of CYP2B/3As. These results suggest that there is isoform specificity in the interaction between P450s and UGTs...
  46. ncbi request reprint Fatty acyl-CoA as an endogenous activator of UDP-glucuronosyltransferases
    Kazuharu Okamura
    Graduate School of Pharmaceutical Sciences, Kyushu University, Higashi ku, Fukuoka, Japan
    Biochem Biophys Res Commun 345:1649-56. 2006
    ..These results suggest that: (1) acyl-CoAs play a role as an endogenous activator of UGTs, and (2) a sulfhydryl group is required for the activation of UGT by physiological concentrations of acyl-CoAs...
  47. ncbi request reprint Modulation of UDP-glucuronosyltransferase 2B7 function by cytochrome P450s in vitro: differential effects of CYP1A2, CYP2C9 and CYP3A4
    Shuso Takeda
    Graduate School of Pharmaceutical Sciences, Kyushu University Fukuoka 812 8582, Japan
    Biol Pharm Bull 28:2026-7. 2005
    ..These results suggest that CYP1A2 and CYP2C9 have ability to modify UGT2B7 function. However, the mechanism(s) underlying the modulation of UGT2B7 function by these P450s seems to differ from that by CYP3A4...
  48. ncbi request reprint Human UDP-glucuronosyltransferase 1A5: identification, expression, and activity
    Moshe Finel
    Viikki DDTC, Faculty of Pharmacy, University of Helsinki, P O Box 56 Viikinkaari 5E, 00014 University of Helsinki, Finland
    J Pharmacol Exp Ther 315:1143-9. 2005
    ..Collectively, this work demonstrates for the first time that the human UGT1A5 is expressed in several tissues, is inducible, and is catalytically active...
  49. ncbi request reprint Modulation of UDP-glucuronosyltransferase function by cytochrome P450: evidence for the alteration of UGT2B7-catalyzed glucuronidation of morphine by CYP3A4
    Shuso Takeda
    Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Mol Pharmacol 67:665-72. 2005
    ..This study provides the first evidence that P450 is not only involved in oxidation of drugs but also modulates the function of UGTs...
  50. ncbi request reprint Glucuronidation and the UDP-glucuronosyltransferases in health and disease
    Peter G Wells
    Faculty of Pharmacy and Department of Pharmacology, University of Toronto, Ontario, Canada
    Drug Metab Dispos 32:281-90. 2004
    ....
  51. ncbi request reprint Pharmacogenomics of human UDP-glucuronosyltransferases and irinotecan toxicity
    Robert H Tukey
    Department of Pharmacology, Chemistry and Biochemistry, University of California, San Diego, La Jolla, California 92093, USA
    Mol Pharmacol 62:446-50. 2002
  52. ncbi request reprint UGT1A10 is responsible for SN-38 glucuronidation and its expression in human lung cancers
    Tetsuya Oguri
    Department of Internal Medicine and Molecular Science, Nagoya City University Graduate School of Medical Sciences, Nagoya, Japan
    Anticancer Res 24:2893-6. 2004
    ..In order to extend this result to the clinical setting, it is important to elucidate the role of SN-38 glucuronidation by UGT1A isoforms in CPT-11/SN-38 resistance in vivo...
  53. ncbi request reprint Relationship between hyperbilirubinaemia and UDP-glucuronosyltransferase 1A1 (UGT1A1) polymorphism in adult HIV-infected Thai patients treated with indinavir
    Mark A Boyd
    The HIV Netherlands Australia Thailand Research Collaboration HIV NAT, Thai Red Cross AIDS Research Centre, Bangkok, Thailand
    Pharmacogenet Genomics 16:321-9. 2006
    ..To investigate the association between the UGT1A1*6 (G71R) and UGT1A1*28 (promoter (TA)7-repeat) genotypes and hyperbilirubinaemia in Thai patients treated with indinavir, and characterize the inhibition of human UGTs by indinavir in vitro...
  54. ncbi request reprint Inhibitory effects of adenine nucleotides and related substances on UDP-glucuronosyltransferase: structure-effect relationships and evidence for an allosteric mechanism
    Yoshio Nishimura
    Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Biochim Biophys Acta 1770:1557-66. 2007
    ..These results suggest that (1) a number of cellular nucleotides present within the endoplasmic reticulum regulate UGT function; and (2) these substances bind to a common allosteric site on UGT to reduce catalytic function...