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Literature summary for 2.4.1.17 extracted from
- Glucuronidation of dihydrotestosterone and trans-androsterone by recombinant UDP-glucuronosyltransferase (UGT) 1A4: Evidence for multiple UGT1A4 aglycone binding sites (2010), Drug Metab. Dispos., 38, 431-440.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of isoform UGT1A4 in HEK-293 cell | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| lamotrigen | low-affinity substrate of isoform UGT1A4, noncompetitively inhibits dihydrotestosterone and trans-androsterone glucuronidation | Homo sapiens |  |
| tamoxifen | uncompetitive substrate inhibition. Coincubation with tamoxifen, a high-affinity substrate of isoform UGT1A4, results in a concentration-dependent activation/inhibition effect on dihydrotestosterone and trans-androsterone glucuronidation | Homo sapiens | |
| trans-androsterone | uncompetitive substrate inhibition | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0009 | - |
tamoxifen | isoform UGT1A4, pH 7.4, 37°C | Homo sapiens | |
| 0.0196 | - |
dihydrotestosterone | isoform UGT1A4, pH 7.4, 37°C | Homo sapiens | |
| 0.0236 | - |
trans-androsterone | isoform UGT1A4, pH 7.4, 37°C | Homo sapiens | |
| 1.564 | - |
lamotrigine | isoform UGT1A4, pH 7.4, 37°C | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| dihydrotestosterone + UDP-alpha-D-glucuronate | - |
Homo sapiens | dihydrotestosterone D-glucuronate + UDP | - |
? | |
| lamotrigine + UDP-alpha-D-glucuronate | - |
Homo sapiens | lamotrigine D-glucuronate + UDP | - |
? | |
| tamoxifen + UDP-alpha-D-glucuronate | - |
Homo sapiens | tamoxifen-N-glucuronate + UDP | - |
? | |
| trans-androsterone + UDP-alpha-D-glucuronate | - |
Homo sapiens | trans-androsterone D-glucuronate + UDP | - |
? | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0046 | - |
tamoxifen | isoform UGT1A4, pH 7.4, 37°C | Homo sapiens | |
| 0.514 | - |
trans-androsterone | isoform UGT1A4, pH 7.4, 37°C | Homo sapiens | |
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