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Literature summary extracted from

  • Zhang, D.; Chando, T.J.; Everett, D.W.; Patten, C.J.; Dehal, S.S.; Humphreys, W.G.
    In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation (2005), Drug Metab. Dispos., 33, 1729-1739.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 2-hydroxy-estradiol 38.5% inhibition at 0.1 mM, UGT1A3 Homo sapiens
2.4.1.17 atazanavir a HIV protease inhibitor, linear mixed-type inhibition mechanism, UGT1A1, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7 Homo sapiens
2.4.1.17 beta-estradiol 61.5% inhibition at 0.2 mM, UGT1A1 Homo sapiens
2.4.1.17 eugenol UGT2B7, 54.5% inhibition at 0.1 mM Homo sapiens
2.4.1.17 hecogenin 48.0% inhibition at 0.05 mM, UGT1A4 Homo sapiens
2.4.1.17 indinavir a HIV protease inhibitor, linear mixed-type inhibition mechanism, UGT1A1, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7 Homo sapiens
2.4.1.17 lopinavir a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7 Homo sapiens
2.4.1.17 additional information IC50 values for HIV protease inhibitors with UGT isozymes, overview Homo sapiens
2.4.1.17 naphthol UGT1A6, 87.0% inhibition at 0.05 mM Homo sapiens
2.4.1.17 nelfinavir a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7 Homo sapiens
2.4.1.17 propofol UGT1A9, 37.0% inhibition at 0.05 mM Homo sapiens
2.4.1.17 ritonavir a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7 Homo sapiens
2.4.1.17 saquinavir a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.004
-
 bilirubin pH 7.5, 37°C, recombinant UGT1A1 Homo sapiens
2.4.1.17 0.0062
-
 bilirubin pH 7.5, 37°C, liver UGT1A1 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.4.1.17 microsome
-
 Homo sapiens
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.4.1.17 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.1.17 additional information Homo sapiens direct inhibition of UGT1A1-mediated bilirubin glucuronidation may provide a mechanism for the reversible hyperbilirubinemia associated with administration of atazanavir as well as indinavir ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens
-
 isozymes UGT1A1, 1A3, 1A4, 1A6, 1A9, and 2B7
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.17 commercial preparation human UGT supersomes, i.e. membranes of insect cells transfected with baculovirus containing human cDNA of UGTs or microsomes of lymphoblast cells heterologously expressing human cDNA of UGT1A1 Homo sapiens
-
2.4.1.17 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 additional information direct inhibition of UGT1A1-mediated bilirubin glucuronidation may provide a mechanism for the reversible hyperbilirubinemia associated with administration of atazanavir as well as indinavir Homo sapiens ?
-
 ?
2.4.1.17 UDP-glucuronic acid + 7-hydroxy-4-(trifluoromethyl)-coumarin UGT1A6, UGT1A9, and UGT2B7 Homo sapiens UDP + 7-hydroxy-4-(trifluoromethyl)-coumarin O-glucuronide
-
 ?
2.4.1.17 UDP-glucuronic acid + beta-estradiol UGT1A3 Homo sapiens UDP + beta-estradiol 3-O-beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronic acid + bilirubin UGT1A1 Homo sapiens UDP + bilirubin-glucuronoside
-
 ?
2.4.1.17 UDP-glucuronic acid + trifluoperazine UGT1A4 Homo sapiens UDP + ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UGT
-
 Homo sapiens
2.4.1.17 uridine 5'-diphospho-glucuronosyltransferase
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.1.17 37
-
 assay at, UGT1A1 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.1.17 7.5
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 additional information
-
 additional information inhibition kinetics Homo sapiens
2.4.1.17 0.0019
-
 atazanavir pH 7.5, 37°C, UGT1A1 Homo sapiens
2.4.1.17 0.0479
-
 indinavir pH 7.5, 37°C, UGT1A1 Homo sapiens