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Literature summary for 2.4.1.17 extracted from
- UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics (2007), Drug Metab. Dispos., 35, 371-380.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 17alpha-ethinylestradiol | strongly inhibits the formation of etoposide alcoholic glucuronide EAG2 (IC50: 0.0 42 mM) but shows very similar and moderate inhibition on etoposide phenolic glucuronide (IC50: 0.2 mM) and etoposide alcoholic glucuronide EAG1 (IC50: 0.21 mM) | Homo sapiens |  |
| beta-estradiol | exhibits strong inhibition on etoposide phenolic glucuronide (IC50: 0.068 mM) and etoposide alcoholic glucuronide EAG2 (IC50: 0.086 mM). The inhibitory effect of beta-estradiol on the formation of etoposide alcoholic glucuronide EAG1 is not so significant in comparison with the other two etoposide glucuronide isomers, even at very high concentration of beta-estradiol (about 80% at 2 mM) | Homo sapiens | |
| bilirubin | strongly inhibits the formation of etoposide phenolic glucuronide (IC50: 0.075 mM) and EAG1 (I50: 0.054 mM), and significantly inhibits the formation of etoposide alcoholic glucuronide EAG2 (IC50: 0.140 mM) | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Homo sapiens | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| etoposide + UDP-glucuronate | Homo sapiens | UGT1A1 is principally responsible for the formation of etoposide glucuronides, mainly in the form of phenolic glucuronide | UDP + etoposide glucuronide | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P22309 | - |
- |
| Homo sapiens | P35503 | - |
- |
| Homo sapiens | Q9HAW9 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| intestine | - |
Homo sapiens | - |
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| etoposide + UDP-glucuronate | - |
Homo sapiens | UDP + etoposide glucuronide | - |
? | |
| etoposide + UDP-glucuronate | UGT1A1 is principally responsible for the formation of etoposide glucuronides, mainly in the form of phenolic glucuronide | Homo sapiens | UDP + etoposide glucuronide | - |
? | |
| etoposide + UDP-glucuronate | activity with UGT1A3 is much lower than activity with UGT1A1 | Homo sapiens | UDP + etoposide glucuronide | - |
? | |
| etoposide + UDP-glucuronate | activity with UGT1A8 is much lower than activity with UGT1A1 | Homo sapiens | UDP + etoposide glucuronide | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| UDP-glucuronosyltransferase 1A1 | - |
Homo sapiens |
| UDP-glucuronosyltransferase 1A3 | - |
Homo sapiens |
| UDP-glucuronosyltransferase 1A8 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.042 | - |
strongly inhibits the formation of etoposide alcoholic glucuronide EAG2 (IC50: 0.042 mM) | Homo sapiens | 17alpha-ethinylestradiol | |
| 0.054 | - |
strongly inhibits EAG1 (I50: 0.054 mM) | Homo sapiens | bilirubin | |
| 0.068 | 0.086 | exhibits strong inhibition on etoposide phenolic glucuronide (IC50: 0.068 mM) and etoposide alcoholic glucuronide EAG2 (IC50: 0.086 mM). The inhibitory effect of beta-estradiol on the formation of etoposide alcoholic glucuronide EAG1 is not so significant | Homo sapiens | beta-estradiol | |
| 0.075 | - |
strongly inhibits the formation of etoposide phenolic glucuronide (IC50: 0.075 mM) | Homo sapiens | bilirubin | |
| 0.14 | - |
significantly inhibits the formation of etoposide alcoholic glucuronide EAG2 (IC50: 0.140 mM) | Homo sapiens | bilirubin | |
| 0.2 | - |
shows very similar and moderate inhibition on etoposide phenolic glucuronide (IC50: 0.2 mM) | Homo sapiens | 17alpha-ethinylestradiol | |
| 0.21 | - |
shows very similar and moderate inhibition on etoposide alcoholic glucuronide EAG1 (IC50: 0.21 mM) | Homo sapiens | 17alpha-ethinylestradiol | |
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