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Meeting ReportSYMPOSIUM

Glucuronidation of Amine Substrates by Purified and Expressed UDP-Glucuronosyltransferase Proteins

1996 ASPET N-Glucuronidation of Xenobiotics Symposium

Mitchell D. Green and Thomas R. Tephly
Drug Metabolism and Disposition September 1998, 26 (9) 860-867;
Mitchell D. Green
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Thomas R. Tephly
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1996 ASPET N-Glucuronidation of Xenobiotics Symposium

Abstract

Conjugation of many primary, secondary, and tertiary amine–containing xenobiotics with glucuronic acid can result in the formation of N-glucuronide metabolites. For carcinogenic arylamines and their N-hydroxylated metabolites,N-glucuronidation can result in the formation of either inactive metabolites or labile conjugates, which can be transported to their target tissue (urinary bladder) where they may be converted to reactive metabolites. Drugs with primary amine (e.g.dapsone) or secondary amine moieties (e.g. sulfadimethoxine and clozapine) can also be metabolized to N-glucuronides. The metabolism of a number of tertiary amine–containing pharmacological agents to quaternary ammonium–linked glucuronides represents a unique and important metabolic pathway for these compounds that is highly species-dependent. This review summarizes our present knowledge of the uridine diphosphate (UDP)-glucuronosyltransferase enzymes involved in catalyzing N-glucuronide formation. Of the more than 30 UDP-glucuronosyltransferases that have been purified or cloned and expressed, many catalyze N-glucuronide formation for primary and secondary amine substrates. In contrast, only human UDP-glucuronosyltransferases 1A3 and 1A4 have been shown to catalyze quaternary ammonium–linked glucuronide formation for aliphatic tertiary amines. The structure of the UGT1 gene complex is highly conserved across species, and it appears that a mutation in the first exon encoding UDP-glucuronosyltransferase 1A4, resulting in a pseudo-gene, may explain the inability of some species to form quaternary ammonium–linked glucuronides.

Footnotes

  • Send reprint requests to: Mitchell D. Green, M.S., Department of Pharmacology, 2-459 Bowen Science Building, The University of Iowa, Iowa City, IA 52242.

  • This work was supported by National Institutes of Health Grant GM 26221.

  • Abbreviations used are::
    α-NA
    α-naphthylamine
    β-NA
    β-naphthylamine
    4-ABP
    4-aminobiphenyl
    UDP
    uridine diphosphate
    2-ABP
    2-aminobiphenyl
    OH
    hydroxy
    LA Wistar rats
    strain of Wistar rats deficient in UGT2B2
    HA Wistar rats
    strain of Wistar rats with normal UGT2B2
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition
Vol. 26, Issue 9
1 Sep 1998
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Meeting ReportSYMPOSIUM

Glucuronidation of Amine Substrates by Purified and Expressed UDP-Glucuronosyltransferase Proteins

Mitchell D. Green and Thomas R. Tephly
Drug Metabolism and Disposition September 1, 1998, 26 (9) 860-867;

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Meeting ReportSYMPOSIUM

Glucuronidation of Amine Substrates by Purified and Expressed UDP-Glucuronosyltransferase Proteins

Mitchell D. Green and Thomas R. Tephly
Drug Metabolism and Disposition September 1, 1998, 26 (9) 860-867;
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  • The N-Glucuronidation of Xenobiotics
  • N +-Glucuronidation, a Common Pathway in Human Metabolism of Drugs With a Tertiary Amine Group
  • Species Differences in N-Glucuronidation
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