Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.4.1.17 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)

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

Inhibitors

Inhibitors Comment Organism Structure
monobenzyl phthalate isoform UGT1A9 shows 92.49% inhibition at 0.1 mM Homo sapiens
monobutyl phthalate
-
Homo sapiens
monocyclohexyl phthalate isoform UGT1A9 shows 95.9% inhibition at 0.1 mM Homo sapiens
monoethyl phthalate
-
Homo sapiens
monoethylhexyl phthalate isoform UGT1A7 shows 85.26% inhibition at 0.1 mM, isoform UGT1A9 shows 97.61% inhibition at 0.1 mM Homo sapiens
monohexyl phthalate isoform UGT1A9 shows 85.83% inhibition at 0.1 mM Homo sapiens
monomethyl phthalate
-
Homo sapiens
monooctyl phthalate isoform UGT1A9 shows 91.21% inhibition at 0.1 mM Homo sapiens
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

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

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
UGT1A10 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
0.00009
-
monocyclohexyl phthalate isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
0.00016
-
monooctyl phthalate isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
0.00117
-
monoethylhexyl phthalate isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
0.00213
-
monobenzyl phthalate isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
0.00746
-
monohexyl phthalate isoform UGT1A9, at pH 7.4 and 37°C Homo sapiens
0.01125
-
monoethylhexyl phthalate isoform UGT1A7, at pH 7.4 and 37°C Homo sapiens

IC50 Value

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