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Literature summary extracted from

  • Zhou, J.; Tracy, T.; Remmel, R.
    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.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 expression of isoform UGT1A4 in HEK-293 cell Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 lamotrigen low-affinity substrate of isoform UGT1A4, noncompetitively inhibits dihydrotestosterone and trans-androsterone glucuronidation Homo sapiens
2.4.1.17 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
2.4.1.17 trans-androsterone uncompetitive substrate inhibition Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.0009
-
 tamoxifen isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.0196
-
 dihydrotestosterone isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.0236
-
 trans-androsterone isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 1.564
-
 lamotrigine isoform UGT1A4, pH 7.4, 37°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 dihydrotestosterone + UDP-alpha-D-glucuronate
-
 Homo sapiens dihydrotestosterone D-glucuronate + UDP
-
 ?
2.4.1.17 lamotrigine + UDP-alpha-D-glucuronate
-
 Homo sapiens lamotrigine D-glucuronate + UDP
-
 ?
2.4.1.17 tamoxifen + UDP-alpha-D-glucuronate
-
 Homo sapiens tamoxifen-N-glucuronate + UDP
-
 ?
2.4.1.17 trans-androsterone + UDP-alpha-D-glucuronate
-
 Homo sapiens trans-androsterone D-glucuronate + UDP
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 0.0046
-
 tamoxifen isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.514
-
 trans-androsterone isoform UGT1A4, pH 7.4, 37°C Homo sapiens