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 |
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 |
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 |
EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|---|
2.4.1.17 | microsome | - |
Homo sapiens | - |
- |
2.4.1.17 | microsome | - |
Macaca fascicularis | - |
- |
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 | - |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
2.4.1.17 | liver | - |
Homo sapiens | - |
2.4.1.17 | liver | - |
Macaca fascicularis | - |
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 | ? | - |
? |
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 |