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Literature summary for 2.4.1.17 extracted from

  • Kaji, H.; Kume, T.
    Regioselective glucuronidation of denopamine: marked species differences and identification of human UDP-glucuronosyltransferase isoform (2005), Drug Metab. Dispos., 33, 403-412.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of isozyme UGT1A1 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT1A10 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT1A3 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT1A4 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT1A6 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT1A7 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT1A8 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT1A9 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT2B15 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT2B17 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT2B4 in insect cells using the baculovirus infection system Homo sapiens
expression of isozyme UGT2B7 in insect cells using the baculovirus infection system Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
diclofenac inhibition of denopamine glucuroniation Homo sapiens
DMSO 2% v/v reduces enzyme activity in liver microsomes Canis lupus familiaris
DMSO 2% v/v reduces enzyme activity in liver microsomes; 2% v/v reduces enzyme activity in liver microsomes; 2% v/v reduces enzyme activity in liver microsomes; 2% v/v reduces enzyme activity in liver microsomes; 2% v/v reduces enzyme activity in liver microsomes; 2% v/v reduces enzyme activity in liver microsomes; 2% v/v reduces enzyme activity in liver microsomes; 2% v/v reduces enzyme activity in liver microsomes; 2% v/v reduces enzyme activity in liver microsomes; 2% v/v reduces enzyme activity in liver microsomes; 2% v/v reduces enzyme activity in liver microsomes Homo sapiens
additional information no effect by 1% v/v DMSO and 2% v/v methanol on denopamine glucuronidation Canis lupus familiaris
additional information no effect by 1% v/v DMSO and 2% v/v methanol on denopamine glucuronidation Homo sapiens
additional information no effect by 1% v/v DMSO and 2% v/v methanol on denopamine glucuronidation Macaca fascicularis
additional information no effect by 1% v/v DMSO and 2% v/v methanol on denopamine glucuronidation Oryctolagus cuniculus
additional information no effect by 1% v/v DMSO and 2% v/v methanol on denopamine glucuronidation Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0018
-
denopamine liver microsomes, substrate denopamine, pH 7.5, 37°C Oryctolagus cuniculus
0.0022
-
denopamine liver microsomes, substrate denopamine, pH 7.5, 37°C Rattus norvegicus
1.48
-
denopamine recombinant isozyme UGT2B7, substrate denopamine, pH 7.5, 37°C Homo sapiens
1.84
-
denopamine liver microsomes, substrate denopamine, formation of G2 product, pH 7.5, 37°C Macaca fascicularis
2.87
-
denopamine liver micosomes, substrate denopamine, pH 7.5, 37°C Homo sapiens
2.99
-
denopamine jejunum microsomes, substrate denopamine, pH 7.5, 37°C Homo sapiens
3.51
-
denopamine liver microsomes, substrate denopamine, formation of G2 product, pH 7.5, 37°C Canis lupus familiaris
3.91
-
denopamine liver microsomes, substrate denopamine, formation of G1 product, pH 7.5, 37°C Macaca fascicularis
10.18
-
denopamine liver microsomes, substrate denopamine, formation of G1 product, pH 7.5, 37°C Canis lupus familiaris

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-
microsome
-
Rattus norvegicus
-
-
microsome
-
Oryctolagus cuniculus
-
-
microsome
-
Canis lupus familiaris
-
-
microsome
-
Macaca fascicularis
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens
Mg2+
-
Rattus norvegicus
Mg2+
-
Oryctolagus cuniculus
Mg2+
-
Canis lupus familiaris
Mg2+
-
Macaca fascicularis

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris
-
male beagles
-
Homo sapiens
-
isozyme UGT1A6
-
Homo sapiens
-
isozyme UGT2B4
-
Homo sapiens O60656 isozyme UGT1A9; isozyme UGT1A9
-
Homo sapiens O75795 isozyme UGT2B17
-
Homo sapiens P16662 isozyme UGT2B7; isozyme UGT2B7
-
Homo sapiens P22309 isozyme UGT1A1; isozyme UGT1A1
-
Homo sapiens P22310 isozyme UGT1A4; isozyme UGT1A4
-
Homo sapiens P35503 isozyme UGT1A3; isozyme UGT1A3
-
Homo sapiens P54855 isozyme UGT2B15; isozyme UGT2B15
-
Homo sapiens Q9HAW7 isozyme UGT1A7; isozyme UGT1A7
-
Homo sapiens Q9HAW8 isozyme UGT1A10; isozyme UGT1A10
-
Homo sapiens Q9HAW9 isozyme UGT1A8; isozyme UGT1A8
-
Macaca fascicularis
-
cynomolgus monkey
-
Oryctolagus cuniculus
-
male New Zealand White
-
Rattus norvegicus
-
male Sprague-Dawley
-

Source Tissue

Source Tissue Comment Organism Textmining
jejunum
-
Homo sapiens
-
liver
-
Homo sapiens
-
liver
-
Rattus norvegicus
-
liver
-
Oryctolagus cuniculus
-
liver
-
Canis lupus familiaris
-
liver
-
Macaca fascicularis
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
Rattus norvegicus
additional information
-
-
Oryctolagus cuniculus
additional information
-
-
Canis lupus familiaris
additional information
-
-
Macaca fascicularis
0.00011
-
recombinant isozyme UGT2B17, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0002
-
recombinant isozyme UGT1A10, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0005
-
recombinant isozyme UGT2B4, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0007
-
recombinant isozyme UGT1A8, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0014
-
recombinant isozyme UGT1A4, substrate trifluoperazine, pH 7.5, 37°C Homo sapiens
0.0015
-
recombinant isozyme UGT1A1, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0022
-
recombinant isozyme UGT1A3, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0037
-
recombinant isozyme UGT2B15, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0037
-
recombinant isozyme UGT2B7, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0044
-
recombinant isozyme UGT1A6, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0065
-
recombinant isozyme UGT1A9, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0126
-
recombinant isozyme UGT1A7, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0191
-
jejunum microsomes, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens
0.0622
-
liver microsomes, substrate 7-hydroxy-4-trifluoromethylcoumarin, pH 7.5, 37°C Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-alpha-D-glucuronate + diclofenac
-
Homo sapiens UDP + diclofenac O-beta-D-glucuronide
-
?
UDP-glucuronate + 7-hydroxy-4-trifluoromethylcoumarin
-
Homo sapiens UDP + 4-trifluoromethylcoumarin 7-O-beta-D-glucuronide
-
?
UDP-glucuronate + denopamine
-
Rattus norvegicus UDP + denopamine beta-D-glucuronide formation of 1 product metabolite termed G1 ?
UDP-glucuronate + denopamine
-
Oryctolagus cuniculus UDP + denopamine beta-D-glucuronide formation of 1 product metabolite termed G1 ?
UDP-glucuronate + denopamine
-
Homo sapiens UDP + denopamine beta-D-glucuronide formation of 1 product metabolite termed G2 ?
UDP-glucuronate + denopamine
-
Canis lupus familiaris UDP + denopamine beta-D-glucuronide formation of 2 product metabolites termed G1 and G2 ?
UDP-glucuronate + denopamine
-
Macaca fascicularis UDP + denopamine beta-D-glucuronide formation of 2 product metabolites termed G1 and G2 ?
UDP-glucuronate + trifluoperazine isozyme UGT1A4 Homo sapiens UDP + trifluoperazine beta-D-glucuronide
-
?

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase
-
Homo sapiens
UDP-glucuronosyltransferase
-
Rattus norvegicus
UDP-glucuronosyltransferase
-
Oryctolagus cuniculus
UDP-glucuronosyltransferase
-
Canis lupus familiaris
UDP-glucuronosyltransferase
-
Macaca fascicularis
UGT
-
Homo sapiens
UGT
-
Rattus norvegicus
UGT
-
Oryctolagus cuniculus
UGT
-
Canis lupus familiaris
UGT
-
Macaca fascicularis

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens
37
-
assay at Rattus norvegicus
37
-
assay at Oryctolagus cuniculus
37
-
assay at Canis lupus familiaris
37
-
assay at Macaca fascicularis

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens
7.5
-
assay at Rattus norvegicus
7.5
-
assay at Oryctolagus cuniculus
7.5
-
assay at Canis lupus familiaris
7.5
-
assay at Macaca fascicularis