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Literature summary extracted from

  • Du, Z.; Cao, Y.F.; Li, S.N.; Hu, C.M.; Fu, Z.W.; Huang, C.T.; Sun, X.Y.; Liu, Y.Z.; Yang, K.; Fang, Z.Z.
    Inhibition of UDP-glucuronosyltransferases (UGTs) by phthalate monoesters (2018), Chemosphere, 197, 7-13 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 expressed in baculovirus-infected insect cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 monobenzyl phthalate isoform UGT1A9 shows 92.49% inhibition at 0.1 mM Homo sapiens
2.4.1.17 monobutyl phthalate
-
 Homo sapiens
2.4.1.17 monocyclohexyl phthalate isoform UGT1A9 shows 95.9% inhibition at 0.1 mM Homo sapiens
2.4.1.17 monoethyl phthalate
-
 Homo sapiens
2.4.1.17 monoethylhexyl phthalate isoform UGT1A7 shows 85.26% inhibition at 0.1 mM, isoform UGT1A9 shows 97.61% inhibition at 0.1 mM Homo sapiens
2.4.1.17 monohexyl phthalate isoform UGT1A9 shows 85.83% inhibition at 0.1 mM Homo sapiens
2.4.1.17 monomethyl phthalate
-
 Homo sapiens
2.4.1.17 monooctyl phthalate isoform UGT1A9 shows 91.21% inhibition at 0.1 mM Homo sapiens
2.4.1.17 additional information 0.1 mM phthalate monoesters exhibit weak inhibition towards isoforms UGT1A10, UGT2B4, UGT2B7, UGT2B15 and UGT2B17 by reducing the glucuronidation less than 80% Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.4.1.17 Mg2+ 5 mM used in assay conditions 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 4-methylumbelliferone + UDP-glucuronate
-
 Homo sapiens UDP + 4-methylumbelliferyl beta-D-glucuronide
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UDP-glucuronosyltransferase
-
 Homo sapiens
2.4.1.17 UGT1A1 isoform Homo sapiens
2.4.1.17 UGT1A10 isoform Homo sapiens
2.4.1.17 UGT1A3 isoform Homo sapiens
2.4.1.17 UGT1A6 isoform Homo sapiens
2.4.1.17 UGT1A7 isoform Homo sapiens
2.4.1.17 UGT1A8 isoform Homo sapiens
2.4.1.17 UGT1A9 isoform Homo sapiens
2.4.1.17 UGT2B15 isoform Homo sapiens
2.4.1.17 UGT2B17 isoform Homo sapiens
2.4.1.17 UGT2B4 isoform Homo sapiens
2.4.1.17 UGT2B7 isoform Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 0.00009
-
 monocyclohexyl phthalate isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
2.4.1.17 0.00016
-
 monooctyl phthalate isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
2.4.1.17 0.00117
-
 monoethylhexyl phthalate isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
2.4.1.17 0.00213
-
 monobenzyl phthalate isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
2.4.1.17 0.00746
-
 monohexyl phthalate isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
2.4.1.17 0.01125
-
 monoethylhexyl phthalate isoform UGT1A7, at pH 7.4 and 37°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.17 0.00157
-
 isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens monoethylhexyl phthalate
2.4.1.17 0.00329
-
 isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens monocyclohexyl phthalate
2.4.1.17 0.00758
-
 isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens monooctyl phthalate
2.4.1.17 0.00936
-
 isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens monobenzyl phthalate
2.4.1.17 0.01071
-
 isoform UGT1A7, at pH 7.4 and 37°C Homo sapiens monoethylhexyl phthalate
2.4.1.17 0.01246
-
 isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens monohexyl phthalate