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Literature summary extracted from

  • Ohno, S.; Kawana, K.; Nakajin, S.
    Contribution of UDP-glucuronosyltransferase 1A1 and 1A8 to morphine-6-glucuronidation and its kinetic properties (2008), Drug Metab. Dispos., 36, 688-694.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 expression of isozyme UGT1A1 in baculovirus-infected insect cells Homo sapiens
2.4.1.17 expression of isozyme UGT1A8 in baculovirus-infected insect cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 morphine
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 additional information
-
 additional information kinetic analysis, isozyme UGT1A1 shows biphasic Michaelis-Menten kinetic behavior with substrate morphine, overview Homo sapiens
2.4.1.17 additional information
-
 additional information kinetic analysis, isozyme UGT1A8 shows biphasic Michaelis-Menten kinetic behavior with substrate morphine, overview Homo sapiens
2.4.1.17 0.0355
-
 morphine pH 7.5, 37°C, isozyme UGT1A8, at 0.05 mM morphine Homo sapiens
2.4.1.17 0.0404
-
 morphine pH 7.5, 37°C, isozyme UGT1A1, at 0.05 mM morphine Homo sapiens
2.4.1.17 0.0679
-
 morphine pH 7.5, 37°C, isozyme UGT1A1, at 2.5 mM morphine Homo sapiens
2.4.1.17 0.0681
-
 morphine pH 7.5, 37°C, isozyme UGT1A8, at 2.5 mM morphine Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.4.1.17 microsome
-
 Homo sapiens
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.4.1.17 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.1.17 UDP-D-glucuronate + acceptor Homo sapiens
-
 UDP + acceptor beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + morphine Homo sapiens the metabolic conversion of morphine to morphine-6-glucuronide plays a significant role in mediation of the clinical effect of morphine because of the superior analgesic effect of morphine-6-glucuronide UDP + morphine 6-beta-D-glucuronoside
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens
-
 isozyme UGT1A8
-
2.4.1.17 Homo sapiens P22309 isozyme UGT1A1; isozyme UGT1A1
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.17 intestine
-
 Homo sapiens
-
2.4.1.17 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 additional information substrate specificity of UGT isozymes with morphine, overview, no or poor activity with isozymes UGT1A3, UGT1A4, UGT1A6, UGT1A7, UGT1A9, UGT1A10, UGT2B15, and UGT2B17 Homo sapiens ?
-
 ?
2.4.1.17 UDP-D-glucuronate + acceptor
-
 Homo sapiens UDP + acceptor beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + morphine the metabolic conversion of morphine to morphine-6-glucuronide plays a significant role in mediation of the clinical effect of morphine because of the superior analgesic effect of morphine-6-glucuronide Homo sapiens UDP + morphine 6-beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + morphine isozyme UGT1A1, as the morphine concentration approaches 0.1 mM, morphine-6-glucuronidation activity gradually decreases, and the kinetics closely resemble substrate inhibition Michaelis-Menten kinetic behavior Homo sapiens UDP + morphine 6-beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + morphine isozyme UGT1A8, as the morphine concentration approaches 0.1 mM, morphine-6-glucuronidation activity gradually decreases, and the kinetics closely resemble substrate inhibition Michaelis-Menten kinetic behavior Homo sapiens UDP + morphine 6-beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + morphine activity of isozyme UGT1A8 Homo sapiens UDP + morphine 3-beta-D-glucuronoside
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UDP-glucuronosyltransferase 1A1
-
 Homo sapiens
2.4.1.17 UDP-glucuronosyltransferase 1A8
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.1.17 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.1.17 7.5
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 0.088
-
 morphine pH 7.5, 37°C, isozyme UGT1A8 Homo sapiens
2.4.1.17 0.219
-
 morphine pH 7.5, 37°C, isozyme UGT1A1 Homo sapiens