Any feedback?
Literature summary extracted from
- Glucuronidation of antiallergic drug, tranilast: identification of human UDP-glucuronosyltransferase isoforms and effect of its phase I metabolite (2007), Drug Metab. Dispos., 35, 583-589.
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 2.4.1.17 | 3-demethyltranilast | - |
Homo sapiens |  |
| 2.4.1.17 | 4-demethyltranilast | bilirubin glucuronosyltransferase activity, tranilast glucuronosyltransferase activity | Homo sapiens | |
| 2.4.1.17 | bilirubin | tranilast glucuronosyltransferase activity, activity in human jejunum microsomes is strongly inhibited (IC50: 0.0811 mM) | Homo sapiens | |
| 2.4.1.17 | tranilast | bilirubin glucuronosyltransferase activity, activity in human jejunum microsomes is strongly inhibited (0.0753 mM) | Homo sapiens | |
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 2.4.1.17 | 0.0506 | - |
tranilast | activity in human jejunum microsomes | Homo sapiens | |
| 2.4.1.17 | 0.0515 | - |
tranilast | activity in human liver microsomes | Homo sapiens | |
Localization
| EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|---|
| 2.4.1.17 | microsome | - |
Homo sapiens | - |
- |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 2.4.1.17 | Homo sapiens | P22309 | - |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 2.4.1.17 | jejunum | - |
Homo sapiens | - |
| 2.4.1.17 | liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 2.4.1.17 | bilirubin + UDP-glucuronate | UGT1A1 exhibits the highest tranilast glucuronosyltransferase activity (13.5 pmol/min/mg protein) | Homo sapiens | bilirubin glucuronoside + UDP | - |
? | |
| 2.4.1.17 | tranilast + UDP-glucuronate | - |
Homo sapiens | tranilast glucuronoside + UDP | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 2.4.1.17 | UGT1A1 | - |
Homo sapiens |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 2.4.1.17 | 0.0811 | - |
tranilast glucuronosyltransferase activity, activity in human jejunum microsomes is strongly inhibited (IC50: 0.0811 mM) | Homo sapiens | bilirubin | |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
