Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-hydroxy-estradiol | 38.5% inhibition at 0.1 mM, UGT1A3 | Homo sapiens | |
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 | |
beta-estradiol | 61.5% inhibition at 0.2 mM, UGT1A1 | Homo sapiens | |
eugenol | UGT2B7, 54.5% inhibition at 0.1 mM | Homo sapiens | |
hecogenin | 48.0% inhibition at 0.05 mM, UGT1A4 | Homo sapiens | |
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 | |
lopinavir | a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7 | Homo sapiens | |
additional information | IC50 values for HIV protease inhibitors with UGT isozymes, overview | Homo sapiens | |
naphthol | UGT1A6, 87.0% inhibition at 0.05 mM | Homo sapiens | |
nelfinavir | a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7 | Homo sapiens | |
propofol | UGT1A9, 37.0% inhibition at 0.05 mM | Homo sapiens | |
ritonavir | a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7 | Homo sapiens | |
saquinavir | a HIV protease inhibitor, inhibition of isozymes UGT1A1, 1A3, 1A4, low inhibition of isozymes UGT1A6, 1A9, and 2B7 | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.004 | - |
bilirubin | pH 7.5, 37°C, recombinant UGT1A1 | Homo sapiens | |
0.0062 | - |
bilirubin | pH 7.5, 37°C, liver UGT1A1 | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isozymes UGT1A1, 1A3, 1A4, 1A6, 1A9, and 2B7 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
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 | - |
liver | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
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 | ? | - |
? | |
UDP-glucuronic acid + 7-hydroxy-4-(trifluoromethyl)-coumarin | UGT1A6, UGT1A9, and UGT2B7 | Homo sapiens | UDP + 7-hydroxy-4-(trifluoromethyl)-coumarin O-glucuronide | - |
? | |
UDP-glucuronic acid + beta-estradiol | UGT1A3 | Homo sapiens | UDP + beta-estradiol 3-O-beta-D-glucuronide | - |
? | |
UDP-glucuronic acid + bilirubin | UGT1A1 | Homo sapiens | UDP + bilirubin-glucuronoside | - |
? | |
UDP-glucuronic acid + trifluoperazine | UGT1A4 | Homo sapiens | UDP + ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
UGT | - |
Homo sapiens |
uridine 5'-diphospho-glucuronosyltransferase | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at, UGT1A1 | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics | Homo sapiens | |
0.0019 | - |
atazanavir | pH 7.5, 37°C, UGT1A1 | Homo sapiens | |
0.0479 | - |
indinavir | pH 7.5, 37°C, UGT1A1 | Homo sapiens |