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Literature summary for 2.4.1.17 extracted from
- Glucuronidation of etoposide in human liver microsomes is specifically catalyzed by UDP-glucuronosyltransferase 1A1 (2003), Drug Metab. Dispos., 31, 589-595.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4-nitrophenol | inhibits the etoposide glucuronosyltransferase activity in liver microsomes | Homo sapiens |  |
| beta-estradiol | completely inhibits the etoposide glucuronosyltransferase activity in liver microsomes at 0.5 mM | Homo sapiens | |
| bilirubin | completely inhibits the etoposide glucuronosyltransferase activity in liver microsomes at 0.5 mM | Homo sapiens | |
| imipramine | inhibits the etoposide glucuronosyltransferase activity in liver microsomes | Homo sapiens | |
| morphine | inhibits the etoposide glucuronosyltransferase activity in liver microsomes | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.44 | - |
etoposide | liver microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.5 | - |
etoposide | recombinant isozyme UGT1A1, pH 7.4, 37°C | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Homo sapiens | - |
- |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P22309 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | - |
Homo sapiens | - |
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 + etoposide | isozyme UGT1A1 is specific for etoposide | Homo sapiens | UDP + etoposide beta-D-glucuronide | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| UDP-glucuronosyltransferase | - |
Homo sapiens |
| UDP-glucuronosyltransferase 1A1 | - |
Homo sapiens |
| UGT | - |
Homo sapiens |
| UGT1A1 | - |
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 |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | - |
Homo sapiens |
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Release 2023.1 (January 2023)
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