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Literature summary extracted from

  • Patana, A.; Kurkela, M.; Finel, M.; Goldman, A.
    Mutation analysis in UGT1A9 suggests a relationship between substrate and catalytic residues in UDP-glucuronosyltransferases (2008), Protein Eng. Des. Sel., 21, 537-543.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
2.4.1.17 D143A increase in substrate inhibition with 4-methylumbelliferone, large decrease in Vmax Homo sapiens
2.4.1.17 D148A large decrease in Vmax Homo sapiens
2.4.1.17 H37A H37 is not critical in N-glucuronidation, but in O-glucuronidation. 99% decrease in Vmax with substrate UDP-glucuronate Homo sapiens
2.4.1.17 H37D H37 is not critical in N-glucuronidation, but in O-glucuronidation Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 4-Methylumbelliferone substrate inhibition Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.015
-
 4-Methylumbelliferone mutant D143A Homo sapiens
2.4.1.17 0.021
-
 4-Methylumbelliferone wild-type Homo sapiens
2.4.1.17 0.058
-
 retigabine mutant H37A Homo sapiens
2.4.1.17 0.062
-
 scopoletin mutant D143A Homo sapiens
2.4.1.17 0.083
-
 scopoletin wild-type Homo sapiens
2.4.1.17 0.09
-
 retigabine wild-type Homo sapiens
2.4.1.17 0.138
-
 UDP-glucuronate mutant D143A Homo sapiens
2.4.1.17 0.173
-
 UDP-glucuronate mutant H37A Homo sapiens
2.4.1.17 0.179
-
 UDP-glucuronate wild-type Homo sapiens
2.4.1.17 0.184
-
 UDP-glucuronate mutant D148A Homo sapiens
2.4.1.17 0.251
-
 4-aminobiphenyl mutant D148A Homo sapiens
2.4.1.17 0.269
-
 4-aminobiphenyl wild-type Homo sapiens
2.4.1.17 0.286
-
 4-aminobiphenyl mutant H37A Homo sapiens
2.4.1.17 0.629
-
 scopoletin mutant D148A Homo sapiens
2.4.1.17 0.954
-
 scopoletin mutant H37A Homo sapiens
2.4.1.17 0.967
-
 4-Methylumbelliferone mutant D148A Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens
-
 isoform UGT1A9
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 4-aminobiphenyl + UDP-glucuronate
-
 Homo sapiens UDP + 4-aminobiphenyl N-glucuronide
-
 ?
2.4.1.17 4-methylumbelliferone + UDP-glucuronate
-
 Homo sapiens UDP + 4-methylumbelliferyl-7-O-beta-D-glucuronide
-
 ?
2.4.1.17 retigabine + UDP-glucuronate
-
 Homo sapiens UDP + retigabine N-glucuronide
-
 ?
2.4.1.17 scopoletin + UDP-glucuronate
-
 Homo sapiens UDP + scopoletin O-glucuronide
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 1.2
-
 4-Methylumbelliferone mutant D143A Homo sapiens
2.4.1.17 3.73
-
 4-Methylumbelliferone wild-type Homo sapiens