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Literature summary for 2.4.1.17 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
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 3-demethyltranilast | - |
Homo sapiens |  |
| 4-demethyltranilast | bilirubin glucuronosyltransferase activity, tranilast glucuronosyltransferase activity | Homo sapiens | |
| bilirubin | tranilast glucuronosyltransferase activity, activity in human jejunum microsomes is strongly inhibited (IC50: 0.0811 mM) | Homo sapiens | |
| tranilast | bilirubin glucuronosyltransferase activity, activity in human jejunum microsomes is strongly inhibited (0.0753 mM) | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0506 | - |
tranilast | activity in human jejunum microsomes | Homo sapiens | |
| 0.0515 | - |
tranilast | activity in human liver microsomes | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Homo sapiens | - |
- |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P22309 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| jejunum | - |
Homo sapiens | - |
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| bilirubin + UDP-glucuronate | UGT1A1 exhibits the highest tranilast glucuronosyltransferase activity (13.5 pmol/min/mg protein) | Homo sapiens | bilirubin glucuronoside + UDP | - |
? | |
| tranilast + UDP-glucuronate | - |
Homo sapiens | tranilast glucuronoside + UDP | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| UGT1A1 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0811 | - |
tranilast glucuronosyltransferase activity, activity in human jejunum microsomes is strongly inhibited (IC50: 0.0811 mM) | Homo sapiens | bilirubin | |
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