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Literature summary extracted from

  • Kato, Y.; Izukawa, T.; Oda, S.; Fukami, T.; Finel, M.; Yokoi, T.; Nakajima, M.
    Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4 (2013), Drug Metab. Dispos., 41, 1389-1397.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.4.1.17 Nicotine slightly activating with substrate amitriptyline Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 gene UGT1A3, recombinant expression of His-tagged enzyme in Spodoptera frugiperda Sf9 cells via baculovirus transfection Homo sapiens
2.4.1.17 gene UGT1A4, recombinant expression of His-tagged enzyme in Spodoptera frugiperda Sf9 cells via baculovirus transfection Homo sapiens
2.4.1.17 gene UGT2B10, recombinant expression of His-tagged enzyme in Spodoptera frugiperda Sf9 cells via baculovirus transfection Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 amitriptyline substrate inhibition Homo sapiens
2.4.1.17 hecogenin
-
 Homo sapiens
2.4.1.17 imipramine substrate inhibition Homo sapiens
2.4.1.17 additional information no inhibition by hecogenin; no inhibition by hecogenin; no inhibition by nicotine Homo sapiens
2.4.1.17 Nicotine
-
 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 Michaelis-Menten and Hill kinetics Homo sapiens
2.4.1.17 0.0072
-
 imipramine pH 7.4, 37°C Homo sapiens
2.4.1.17 0.0075
-
 amitriptyline pH 7.4, 37°C Homo sapiens
2.4.1.17 0.037
-
 diphenhydramine pH 7.4, 37°C Homo sapiens
2.4.1.17 0.45
-
 amitriptyline pH 7.4, 37°C Homo sapiens
2.4.1.17 0.47
-
 diphenhydramine pH 7.4, 37°C Homo sapiens
2.4.1.17 0.49
-
 amitriptyline pH 7.4, 37°C Homo sapiens
2.4.1.17 0.5
-
 imipramine pH 7.4, 37°C Homo sapiens
2.4.1.17 0.76
-
 imipramine pH 7.4, 37°C Homo sapiens

Metals/Ions

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

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens P22310
-
-
2.4.1.17 Homo sapiens P35503
-
-
2.4.1.17 Homo sapiens P36537
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 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 ?
-
 ?
2.4.1.17 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 ?
-
 ?
2.4.1.17 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 ?
-
 ?
2.4.1.17 UDP-glucuronate + amitriptyline
-
 Homo sapiens UDP + amitriptyline beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-glucuronate + diphenhydramine
-
 Homo sapiens UDP + diphenhydramine beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-glucuronate + imipramine
-
 Homo sapiens UDP + imipramine beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-glucuronate + ketoconazole
-
 Homo sapiens UDP + ketoconazole beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-glucuronate + ketotifen
-
 Homo sapiens UDP + ketotifen beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-glucuronate + midazolam
-
 Homo sapiens UDP + midazolam beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-glucuronate + olanzapine
-
 Homo sapiens UDP + olanzapine beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-glucuronate + pizotifen
-
 Homo sapiens UDP + pizotifen beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-glucuronate + tamoxifen
-
 Homo sapiens UDP + tamoxifen beta-D-glucuronoside
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UDP-glucuronosyltransferase 1A3
-
 Homo sapiens
2.4.1.17 UDP-glucuronosyltransferase 1A4
-
 Homo sapiens
2.4.1.17 UDP-glucuronosyltransferase 2B10
-
 Homo sapiens
2.4.1.17 UGT1A3
-
 Homo sapiens
2.4.1.17 UGT1A4
-
 Homo sapiens
2.4.1.17 UGT2B10
-
 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 7.4
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 0.13
-
 amitriptyline pH 7.4, 37°C Homo sapiens
2.4.1.17 0.38
-
 imipramine pH 7.4, 37°C Homo sapiens