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Literature summary for 2.4.1.17 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
Search for more literature for 2.4.1.17

Activating Compound

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

Cloned(Commentary)

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

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 [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

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P22310
-
-
Homo sapiens P35503
-
-
Homo sapiens P36537
-
-

Substrates and Products (Substrate)

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

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens

Ki Value [mM]

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