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Literature summary for 2.4.1.17 extracted from

  • Kaivosaari, S.; Toivonen, P.; Aitio, O.; Sipilae, J.; Koskinen, M.; Salonen, J.S.; Finel, M.
    Regio- and stereospecific N-glucuronidation of medetomidine: the differences between UDP glucuronosyltransferase (UGT) 1A4 and UGT2B10 account for the complex kinetics of human liver microsomes (2008), Drug Metab. Dispos., 36, 1529-1537.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
alamethicin a pore-forming peptide, activates the activity of liver microsomes, but not of purified recombinant isozyme, with substrates dexmedetomidine and levomedetomidine Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetic analysis, recombinant isozyme UGT1A4, and liver microsomes, with substrates dexmedetomidine and levomedetomidine, overview Homo sapiens
additional information
-
additional information kinetic analysis, recombinant isozyme UGT2B10, and liver microsomes, with substrates dexmedetomidine and levomedetomidine, overview Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2 UDP-D-glucuronate + 2 dexmedetomidine Homo sapiens the major metabolic pathway of dexmedetomidine, i.e. (4S)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, in humans is N-glucuronidation at the imidazolate nitrogens to N3- and N1-glucuronides 2 UDP + dexmedetomidine N1-beta-D-glucuronoside + dexmedetomidine N3-beta-D-glucuronoside
-
?
2 UDP-D-glucuronate + 2 levomedetomidine Homo sapiens the major metabolic pathway of levomedetomidine, i.e. (4R)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, in humans is N-glucuronidation at the imidazolate nitrogens to N3-glucuronide 2 UDP + levomedetomidine N1-beta-D-glucuronoside + dexmedetomidine N3-beta-D-glucuronoside
-
?
UDP-D-glucuronate + acceptor Homo sapiens
-
UDP + acceptor beta-D-glucuronoside
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozyme UGT1A4
-
Homo sapiens P36537 isozyme UGT2B10
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2 UDP-D-glucuronate + 2 dexmedetomidine the major metabolic pathway of dexmedetomidine, i.e. (4S)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, in humans is N-glucuronidation at the imidazolate nitrogens to N3- and N1-glucuronides Homo sapiens 2 UDP + dexmedetomidine N1-beta-D-glucuronoside + dexmedetomidine N3-beta-D-glucuronoside
-
?
2 UDP-D-glucuronate + 2 dexmedetomidine i.e. (+)-4-(S)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, NMR product structure analysis, product ratios of isozyme UGT1A4, overview Homo sapiens 2 UDP + dexmedetomidine N1-beta-D-glucuronoside + dexmedetomidine N3-beta-D-glucuronoside
-
?
2 UDP-D-glucuronate + 2 dexmedetomidine i.e. (+)-4-(S)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, NMR product structure analysis, product ratios of isozyme UGT2B10, overview Homo sapiens 2 UDP + dexmedetomidine N1-beta-D-glucuronoside + dexmedetomidine N3-beta-D-glucuronoside
-
?
2 UDP-D-glucuronate + 2 levomedetomidine the major metabolic pathway of levomedetomidine, i.e. (4R)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, in humans is N-glucuronidation at the imidazolate nitrogens to N3-glucuronide Homo sapiens 2 UDP + levomedetomidine N1-beta-D-glucuronoside + dexmedetomidine N3-beta-D-glucuronoside
-
?
2 UDP-D-glucuronate + 2 levomedetomidine i.e. (4R)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, NMR product structure analysis, product ratios of isozyme UGT1A4, isozyme UGT1A4 shows low activity producing N1- and N3-glucuronides, overview Homo sapiens 2 UDP + levomedetomidine N1-beta-D-glucuronoside + dexmedetomidine N3-beta-D-glucuronoside
-
?
2 UDP-D-glucuronate + 2 levomedetomidine i.e. (4R)-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, NMR product structure analysis, product ratios of isozyme UGT2B10, isozyme UGT2B10 exclusively produces N3-glucuronides, overview Homo sapiens 2 UDP + levomedetomidine N1-beta-D-glucuronoside + dexmedetomidine N3-beta-D-glucuronoside
-
?
additional information regioselectivity of recombinant isozymes and liver microsomes, overview Homo sapiens ?
-
?
UDP-D-glucuronate + acceptor
-
Homo sapiens UDP + acceptor beta-D-glucuronoside
-
?

Synonyms

Synonyms Comment Organism
UDP glucuronosyltransferase 1A4
-
Homo sapiens
UDP glucuronosyltransferase 2B10
-
Homo sapiens
UGT1A4
-
Homo sapiens
UGT2B10
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens