Activating Compound | Comment | Organism | Structure |
---|---|---|---|
Nicotine | slightly activating with substrate amitriptyline | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
gene UGT1A3, recombinant expression of His-tagged enzyme in Spodoptera frugiperda Sf9 cells via baculovirus transfection | Homo sapiens |
gene UGT1A4, recombinant expression of His-tagged enzyme in Spodoptera frugiperda Sf9 cells via baculovirus transfection | Homo sapiens |
gene UGT2B10, recombinant expression of His-tagged enzyme in Spodoptera frugiperda Sf9 cells via baculovirus transfection | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
amitriptyline | substrate inhibition | Homo sapiens | |
hecogenin | - |
Homo sapiens | |
imipramine | substrate inhibition | Homo sapiens | |
additional information | no inhibition by hecogenin; no inhibition by hecogenin; no inhibition by nicotine | Homo sapiens | |
Nicotine | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Michaelis-Menten and Hill kinetics | Homo sapiens | |
0.0072 | - |
imipramine | pH 7.4, 37°C | Homo sapiens | |
0.0075 | - |
amitriptyline | pH 7.4, 37°C | Homo sapiens | |
0.037 | - |
diphenhydramine | pH 7.4, 37°C | Homo sapiens | |
0.45 | - |
amitriptyline | pH 7.4, 37°C | Homo sapiens | |
0.47 | - |
diphenhydramine | pH 7.4, 37°C | Homo sapiens | |
0.49 | - |
amitriptyline | pH 7.4, 37°C | Homo sapiens | |
0.5 | - |
imipramine | pH 7.4, 37°C | Homo sapiens | |
0.76 | - |
imipramine | pH 7.4, 37°C | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Homo sapiens | |
Mg2+ | required | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P22310 | - |
- |
Homo sapiens | P35503 | - |
- |
Homo sapiens | P36537 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | UDP-glucuronosyltransferase 2B10 catalyzes N-glucuronidation of amine-containing compounds, substrate specificity overview. Enzyme UGT2B10 preferably conjugates tertiary amines, but not conjugate the tertiary cyclic amine in trifluoperazin, substrate specificity, overview. No activity with desipramine, nortriptyline, carbamazepine, and afloqualone, UGT2B10 does not conjugate the tertiary cyclic amine in trifluoperazine. The affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher | Homo sapiens | ? | - |
? | |
additional information | UDP-glucuronosyltransferase 2B10 catalyzes N-glucuronidation of amine-containing compounds, substrate specificity overview. Enzyme UGT2B10 preferably conjugates tertiary amines, but not conjugate the tertiary cyclic amine in trifluoperazine. The affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher | Homo sapiens | ? | - |
? | |
additional information | UDP-glucuronosyltransferase 2B10 catalyzes N-glucuronidation of amine-containing compounds, substrate specificity overview. Enzyme UGT2B10 preferably conjugates tertiary amines, but not conjugate the tertiary cyclic amine in trifluoperazine. The affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher. No activity with diphenhydramine | Homo sapiens | ? | - |
? | |
UDP-glucuronate + amitriptyline | - |
Homo sapiens | UDP + amitriptyline beta-D-glucuronoside | - |
? | |
UDP-glucuronate + diphenhydramine | - |
Homo sapiens | UDP + diphenhydramine beta-D-glucuronoside | - |
? | |
UDP-glucuronate + imipramine | - |
Homo sapiens | UDP + imipramine beta-D-glucuronoside | - |
? | |
UDP-glucuronate + ketoconazole | - |
Homo sapiens | UDP + ketoconazole beta-D-glucuronoside | - |
? | |
UDP-glucuronate + ketotifen | - |
Homo sapiens | UDP + ketotifen beta-D-glucuronoside | - |
? | |
UDP-glucuronate + midazolam | - |
Homo sapiens | UDP + midazolam beta-D-glucuronoside | - |
? | |
UDP-glucuronate + olanzapine | - |
Homo sapiens | UDP + olanzapine beta-D-glucuronoside | - |
? | |
UDP-glucuronate + pizotifen | - |
Homo sapiens | UDP + pizotifen beta-D-glucuronoside | - |
? | |
UDP-glucuronate + tamoxifen | - |
Homo sapiens | UDP + tamoxifen beta-D-glucuronoside | - |
? |
Synonyms | Comment | Organism |
---|---|---|
UDP-glucuronosyltransferase 1A3 | - |
Homo sapiens |
UDP-glucuronosyltransferase 1A4 | - |
Homo sapiens |
UDP-glucuronosyltransferase 2B10 | - |
Homo sapiens |
UGT1A3 | - |
Homo sapiens |
UGT1A4 | - |
Homo sapiens |
UGT2B10 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.13 | - |
amitriptyline | pH 7.4, 37°C | Homo sapiens | |
0.38 | - |
imipramine | pH 7.4, 37°C | Homo sapiens |