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Literature summary for 2.4.1.17 extracted from

  • Mori, A.; Maruo, Y.; Iwai, M.; Sato, H.; Takeuchi, Y.
    UDP-glucuronosyltransferase 1A4 polymorphisms in a Japanese population and kinetics of clozapine glucuronidation (2005), Drug Metab. Dispos., 33, 672-675.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
isozyme UGT1A4, DNA and amino acid sequence determination and analysis, expression of isozyme UGT1A4 in COS-7 cells, analysis of polymorphisms naturally occuring in a Japanese population Homo sapiens

Protein Variants

Protein Variants Comment Organism
L48V naturally occuring polymorphism, increased activity with trans-androsterone, imipramine, and cyproheptadine, less active with tigogenin as compared to the wild-type enzyme Homo sapiens
additional information isozyme UGT1A4 polymorphisms in a Japanese population, identification of 3 single nucleotides polymorphisms in exon 1, 1 in intron 1, and of 3 types of alleles with distinct SNP combinations, overview Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.007
-
tigogenin recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C Homo sapiens
0.008
-
trans-androsterone recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C Homo sapiens
0.008
-
tigogenin recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C Homo sapiens
0.025
-
clozapine recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C Homo sapiens
0.049
-
clozapine recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C Homo sapiens
0.086
-
cyproheptadine recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C Homo sapiens
0.228
-
cyproheptadine recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C Homo sapiens
0.255
-
trans-androsterone recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C Homo sapiens
0.276
-
imipramine recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C Homo sapiens
1.442
-
imipramine recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
55000
-
x * 55000, recombinant isozyme UGT1A4, SDS-PAGE Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P22310 isozyme UGT1A4; isozyme UGT1A4
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-glucuronate + clozapine
-
Homo sapiens UDP + clozapine beta-D-glucuronide
-
?
UDP-glucuronate + cyproheptadine
-
Homo sapiens UDP + cyproheptadine beta-D-glucuronide
-
?
UDP-glucuronate + imipramine
-
Homo sapiens UDP + imipramine beta-D-glucuronide
-
?
UDP-glucuronate + tigogenin
-
Homo sapiens UDP + tigogenin beta-D-glucuronide
-
?
UDP-glucuronate + trans-androsterone
-
Homo sapiens UDP + trans-androsterone beta-D-glucuronide
-
?

Subunits

Subunits Comment Organism
? x * 55000, recombinant isozyme UGT1A4, SDS-PAGE Homo sapiens

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase 1A4
-
Homo sapiens
UGT1A4
-
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
8.4
-
assay at Homo sapiens