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Research ArticleCELLULAR AND MOLECULAR

Human UDP-Glucuronosyltransferase 1A5: Identification, Expression, and Activity

Moshe Finel, Xin Li, Dione Gardner-Stephen, Stacie Bratton, Peter I. Mackenzie and Anna Radominska-Pandya
Journal of Pharmacology and Experimental Therapeutics December 2005, 315 (3) 1143-1149; DOI: https://doi.org/10.1124/jpet.105.091900
Moshe Finel
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Xin Li
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Dione Gardner-Stephen
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Stacie Bratton
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Peter I. Mackenzie
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Anna Radominska-Pandya
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Abstract

The human UDP-glucuronosyltransferase (UGT) subfamily 1A includes nine genes. The expression of all the UGT1A isoforms, apart from UGT1A5, has been reported previously. We have now detected a low basal level of UGT1A5 expression in cultured human hepatocytes, and treatment with rifampicin or 3-methylcholanthrene increased the level of UGT1A5 mRNA. Low-level UGT1A5 expression was also found in HepG2 and Caco-2 cells as well as human liver. Furthermore, UGT1A5 expression has been detected in various segments of the intestine from human donors, revealing high interindividual variability in its level and distribution along the intestine. Full-length UGT1A5 cDNA was isolated from Caco-2 cells that had been transfected with the pregnane X receptor and treated with rifampicin. Recombinant UGT1A5, expressed in baculovirus-infected insect cells, exhibited very low rates of 4-methylumbelliferone and scopoletin glucuronidation, whereas 1-hydroxypyrene was a much better substrate for it. UGT1A5 did not glucuronidate 4-aminobiphenyl, a good substrate for the highly homologous enzymes UGT1A4 and UGT1A3. However, replacing the first 110 amino acids of UGT1A5, a region that may be involved in substrate binding, with the counterpart segment from UGT1A4 did not increase the 4-aminobiphenyl glucuronidation activity. Collectively, this work demonstrates for the first time that the human UGT1A5 is expressed in several tissues, is inducible, and is catalytically active.

Footnotes

  • This work was supported in part by the Academy of Finland, Project 207535 (to M.F.), National Institutes of Health Grants DK51971 and DK49715 (to A.R.-P.), tobacco settlement funds (to A.R.-P.), and the Australian National Health and Medical Research Council (to P.I.M.).

  • doi:10.1124/jpet.105.091900.

  • ABBREVIATIONS: UGT, UDP-glucuronosyltransferase; HMM, hepatocyte maintenance medium; Dex, dexamethasone; Rif, rifampicin; 3-MC, 3-methylcholanthrene; RT-PCR, reverse transcription-polymerase chain reaction; GAPDH, glyceraldehyde-3-phosphate dehydrogenase; PCR, polymerase chain reaction; PXR, pregnane X receptor; 4-MU, 4-methylumbelliferone; 4-ABP, 4-aminobiphenyl; 1-HP, 1-hydroxypyrene; GI, gastrointestinal.

    • Received July 1, 2005.
    • Accepted August 19, 2005.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 387 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 387, Issue 1
1 Oct 2023
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Research ArticleCELLULAR AND MOLECULAR

Human UDP-Glucuronosyltransferase 1A5: Identification, Expression, and Activity

Moshe Finel, Xin Li, Dione Gardner-Stephen, Stacie Bratton, Peter I. Mackenzie and Anna Radominska-Pandya
Journal of Pharmacology and Experimental Therapeutics December 1, 2005, 315 (3) 1143-1149; DOI: https://doi.org/10.1124/jpet.105.091900

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Research ArticleCELLULAR AND MOLECULAR

Human UDP-Glucuronosyltransferase 1A5: Identification, Expression, and Activity

Moshe Finel, Xin Li, Dione Gardner-Stephen, Stacie Bratton, Peter I. Mackenzie and Anna Radominska-Pandya
Journal of Pharmacology and Experimental Therapeutics December 1, 2005, 315 (3) 1143-1149; DOI: https://doi.org/10.1124/jpet.105.091900
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