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Literature summary 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)

EC Number Cloned (Comment) Organism
2.4.1.17 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

EC Number Protein Variants Comment Organism
2.4.1.17 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
2.4.1.17 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]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.007
-
 tigogenin recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C Homo sapiens
2.4.1.17 0.008
-
 trans-androsterone recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C Homo sapiens
2.4.1.17 0.008
-
 tigogenin recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C Homo sapiens
2.4.1.17 0.025
-
 clozapine recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C Homo sapiens
2.4.1.17 0.049
-
 clozapine recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C Homo sapiens
2.4.1.17 0.086
-
 cyproheptadine recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C Homo sapiens
2.4.1.17 0.228
-
 cyproheptadine recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C Homo sapiens
2.4.1.17 0.255
-
 trans-androsterone recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C Homo sapiens
2.4.1.17 0.276
-
 imipramine recombinant mutant isozyme UGT1A4 L48V, pH 8.4, 37°C Homo sapiens
2.4.1.17 1.442
-
 imipramine recombinant wild-type isozyme UGT1A4, pH 8.4, 37°C Homo sapiens

Metals/Ions

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

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.4.1.17 55000
-
 x * 55000, recombinant isozyme UGT1A4, SDS-PAGE Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens P22310 isozyme UGT1A4; isozyme UGT1A4
-

Specific Activity [micromol/min/mg]

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

Substrates and Products (Substrate)

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

Subunits

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

Synonyms

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