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Literature summary for 2.4.1.17 extracted from

  • Fujiwara, R.; Nakajima, M.; Yamanaka, H.; Katoh, M.; Yokoi, T.
    Interactions between human UGT1A1, UGT1A4, and UGT1A6 affect their enzymatic activities (2007), Drug Metab. Dispos., 35, 1781-1787.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK293 cells Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information co-expression of both UGT1A1 and UGT1A4 increases the Vmax values of UGT1A6-catalyzed serotonin and diclofenac O-glucuronide formation Homo sapiens
additional information
-
additional information coexpression of UGT1A1 decreases the Vmax value of UGT1A4-catalyzed imipramine N-glucuronide formation but has no effect on UGT1A4-catalyzed trifluoperazine N-glucuronide formation. Coexpression of UGT1A6 has no effect on UGT1A4-catalyzed imipramine N-glucuronide formation but increases the Km and Vmax of UGT1A4-catalyzed trifluoperazine N-glucuronide formation Homo sapiens
additional information
-
additional information imipramine N-glucuronide formation: Vmax (pmol/min/unit): 134.9, 110.4 (1A4 co-expressed with isoform 1A1), 126 (1A4 co-expressed with isoform 1A6). Trifluoperazine N-glucuronide formation: 2.1, 2.0 (1A4 co-expressed with isoform 1A1), 5.1 (1A4 co-expressed with isoform 1A6) Homo sapiens
additional information
-
additional information serotonin O-glucuronide formation: Vmax (nmol/min/unit): 1.5, 2.1 (1A6 co-expressed with isoform 1A1), 6.1 (1A6 co-expressed with isoform 1A4). Diclofenac O-glucuronide formation: 0.0284, 0.088 (1A6 co-expressed with isoform 1A1), 0.0758 (1A6 co-expressed with isoform 1A4) Homo sapiens
0.0197
-
Trifluoperazine trifluoperazine N-glucuronide formation Homo sapiens
0.0198
-
Trifluoperazine trifluoperazine N-glucuronide formation, 1A4 co-expressed with isoform 1A4 Homo sapiens
0.048
-
Trifluoperazine trifluoperazine N-glucuronide formation, 1A4 co-expressed with isoform 1A6 Homo sapiens
1.1
-
imipramine imipramine N-glucuronide formation Homo sapiens
1.4
-
imipramine imipramine N-glucuronide formation, 1A4 co-expressed with isoform 1A4 Homo sapiens
1.4
-
imipramine imipramine N-glucuronide formation, 1A4 co-expressed with isoform 1A6 Homo sapiens
3.7
-
serotonin serotonin O-glucuronide formation, 1A4 co-expressed with isoform 1A6 Homo sapiens
4.4
-
serotonin serotonin O-glucuronide formation, 1A4 co-expressed with isoform 1A4 Homo sapiens
4.6
-
serotonin serotonin O-glucuronide formation Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
50000
-
SDS-PAGE, each UGT1A isoform shows a single band at 50 to 55 kDa, owing to the differences in the levels of glycosylation Homo sapiens

Organism

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-glucuronic acid + diclofenac
-
Homo sapiens UDP + diclofenac O-glucuronide
-
?
UDP-glucuronic acid + imipramine
-
Homo sapiens UDP + imipramine N-glucuronide
-
?
UDP-glucuronic acid + serotonin
-
Homo sapiens UDP + serotonin O-glucuronide
-
?
UDP-glucuronic acid + trifluoperazine
-
Homo sapiens UDP + trifluoperazine N-glucuronide
-
?

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase
-
Homo sapiens
UGT 1A4
-
Homo sapiens
UGT 1A6
-
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