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Literature summary extracted from

  • Hanioka, N.; Tanabe, N.; Jinno, H.; Tanaka-Kagawa, T.; Nagaoka, K.; Naito, S.; Koeda, A.; Narimatsu, S.
    Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes (2010), Life Sci., 87, 261-268.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 expression in insect cell Homo sapiens
2.4.1.17 expression in insect cell Macaca fascicularis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 7-hydroxy-4-trifluoromethylcoumarin substrate inhibition Homo sapiens
2.4.1.17 7-hydroxy-4-trifluoromethylcoumarin substrate inhibition Macaca fascicularis

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.151
-
 7-hydroxy-4-trifluoromethylcoumarin recombinant isoform UGT1A1, pH 7.4, 37°C Macaca fascicularis
2.4.1.17 0.198
-
 7-hydroxy-4-trifluoromethylcoumarin recombinant isoform UGT1A1, pH 7.4, 37°C Homo sapiens

Localization

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

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens P22309 isoform UGT1A1
-
2.4.1.17 Macaca fascicularis Q9TSL7 isoform UGT1A1, with silent mutation 1401ANG, Arg467Arg
-

Source Tissue

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 7-ethyl-10-hydroxycamptothecin + UDP-alpha-D-glucuronate
-
 Homo sapiens 7-ethyl-10-hydroxycamptothecin 10-O-glucuronate + UDP
-
 ?
2.4.1.17 7-ethyl-10-hydroxycamptothecin + UDP-alpha-D-glucuronate
-
 Macaca fascicularis 7-ethyl-10-hydroxycamptothecin 10-O-glucuronate + UDP
-
 ?
2.4.1.17 7-hydroxy-4-trifluoromethylcoumarin + UDP-alpha-D-glucuronate
-
 Homo sapiens 7-hydroxy-4-trifluoromethylcoumarin 7-O-glucuronate + UDP
-
 ?
2.4.1.17 7-hydroxy-4-trifluoromethylcoumarin + UDP-alpha-D-glucuronate
-
 Macaca fascicularis 7-hydroxy-4-trifluoromethylcoumarin 7-O-glucuronate + UDP
-
 ?
2.4.1.17 estradiol + UDP-alpha-D-glucuronate sigmoidal kinetics with n of 1.7 Macaca fascicularis estradiol 3-O-glucuronate + UDP
-
 ?
2.4.1.17 estradiol + UDP-glucuronate sigmoidal kinetics with n of 1.7 Homo sapiens estradiol 3-O-glucuronate + UDP
-
 ?
2.4.1.17 additional information there are no significant differences in the levels of kinetic parameters for 7-hydroxy-4-trifluoromethylcoumarin, estradiol at 3-hydroxy position and 7-ethyl-10-hydroxycamptothecin glucuronidation between humans and cynomolgus monkeys in enzymes from liver microsomes and recombinant isoforms UGT1A1. 7-Hydroxy-4-trifluoromethylcoumarin and estradiol glucuronidation by cynomolgus monkey liver microsomes fits the typical Michaelis-Menten model. 7-Ethyl-10-hydroxycamptothecin glucuronidation by by cynomolgus monkey liver microsomes exhibits autoactivation kinetics Macaca fascicularis ?
-
 ?
2.4.1.17 additional information there are no significant differences in the levels of kinetic parameters for 7-hydroxy-4-trifluoromethylcoumarin, estradiol at 3-hydroxy position and 7-ethyl-10-hydroxycamptothecin glucuronidation between humans and cynomolgus monkeys in enzymes from liver microsomes and recombinant isoforms UGT1A1. 7-Hydroxy-4-trifluoromethylcoumarin and estradiol glucuronidation by human liver microsomes exhibits biphasic and sigmoidal kinetics, respectively. 7-Ethyl-10-hydroxycamptothecin glucuronidation by human liver microsomes exhibits autoactivation kinetics Homo sapiens ?
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 0.0996
-
 7-hydroxy-4-trifluoromethylcoumarin recombinant isoform UGT1A1, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.161
-
 7-hydroxy-4-trifluoromethylcoumarin recombinant isoform UGT1A1, pH 7.4, 37°C Macaca fascicularis