Cloned (Comment) | Organism |
---|---|
expression of isoform UGT1A4 in HEK-293 cell | Homo sapiens |
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 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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
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 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 |