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Literature summary for 2.4.1.17 extracted from

  • Zhang, H.; Zhao, Z.; Wang, T.; Wang, Y.; Cui, X.; Zhang, H.; Fang, Z.Z.
    Inhibition of UDP-glucuronosyltransferase (UGT) isoforms by arctiin and arctigenin (2016), Phytother. Res., 30, 1189-1196 .
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
arctigenin about 210% activity of isoform UGT1A8 at 0.1 mM arctigenin Homo sapiens
arctiin about 225% activity of isoform UGT1A8 at 0.1 mM arctiin Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
arctigenin about 20% inhibition at 0.1 mM; about 35% inhibition at 0.1 mM; about 50% inhibition at 0.1 mM; about 50% inhibition at 0.1 mM; about 65% inhibition at 0.1 mM; about 80% inhibition at 0.1 mM; about 82% inhibition at 0.1 mM; about 90% inhibition at 0.1 mM; noncompetitive inhibition toward isoform UGT2B15 with more than 80% inhibition at 0.1 mM Homo sapiens
arctiin about 20% inhibition at 0.1 mM; about 35% inhibition at 0.1 mM; about 50% inhibition at 0.1 mM; about 50% inhibition at 0.1 mM; about 65% inhibition at 0.1 mM; about 80% inhibition at 0.1 mM; about 82% inhibition at 0.1 mM; about 85% inhibition at 0.1 mM; competitive inhibition toward isoform UGT2B15 with more than 80% inhibition at 0.1 mM Homo sapiens
atractylenolide I inhibitor of isoform UGT2B7 Homo sapiens
gomisin J inhibitor of isoform UGT1A9 Homo sapiens
schisandrin A inhibitor of isoform UGT1A1; inhibitor of isoform UGT1A3 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ 5 mM used in assay conditions Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O60656
-
-
Homo sapiens O75795
-
-
Homo sapiens P06133
-
-
Homo sapiens P16662
-
-
Homo sapiens P19224
-
-
Homo sapiens P22309
-
-
Homo sapiens P35503
-
-
Homo sapiens P54855
-
-
Homo sapiens Q9HAW7
-
-
Homo sapiens Q9HAW9
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-methylumbelliferone + UDP-glucuronate
-
Homo sapiens UDP + 4-methylumbelliferyl beta-D-glucuronide
-
?

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase
-
Homo sapiens
UGT1A1 isoform Homo sapiens
UGT1A3 isoform Homo sapiens
UGT1A6 isoform Homo sapiens
UGT1A7 isoform Homo sapiens
UGT1A8 isoform Homo sapiens
UGT1A9 isoform Homo sapiens
UGT2B15 isoform Homo sapiens
UGT2B17 isoform Homo sapiens
UGT2B4 isoform Homo sapiens
UGT2B7 isoform Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.016
-
arctiin isoform UGT2B15, at pH 7.4 and 37°C Homo sapiens
0.0767
-
arctigenin isoform UGT2B15, at pH 7.4 and 37°C Homo sapiens