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Literature summary for 2.4.1.17 extracted from
- In vitro characterisation of human renal and hepatic frusemide glucuronidation and identification of the UDP-glucuronosyltransferase enzymes involved in this pathway (2008), Biochem. Pharmacol., 76, 249-257.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| stable expression of isozymes UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A7, UGT1A8, UGT1A9, UGT1A10, UGT2B4, UGT2B7, UGT2B15, UGT2B17, and UGT2B28 in HEK-293 cells | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| fluconazole | a UGT2B7 selective inhibitor | Homo sapiens |  |
| Phenylbutazone | a UGT1A selective inhibitor | Homo sapiens | |
| sulfinpyrazone | a UGT1A selective inhibitor | Homo sapiens | |
| zidovudine | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | frusemide glucuronidation followed MichaelisMenten kinetics in all tissues, kinetics of different microsome types from liver and kidney, overview | Homo sapiens |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Homo sapiens | - |
- |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| UDP-D-glucuronate + acceptor | Homo sapiens | - |
UDP + acceptor beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + frusemide | Homo sapiens | - |
UDP + frusemide beta-D-glucuronoside | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
diverse isozymes | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| kidney | cortex and medulla | Homo sapiens | - |
| liver | - |
Homo sapiens | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
catalytic efficiency of frusemide glucuronidation of different microsome types from liver and kidney, overview | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| UDP-D-glucuronate + acceptor | - |
Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + frusemide | - |
Homo sapiens | UDP + frusemide beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + frusemide | substrate of isozymes UGT 1A1, UGT1A3, UGT1A6, UGT1A7, UGT1A9, UGT1A10 and UGT2B7, with a predominant role of UGT1A9 in liver and kidney | Homo sapiens | UDP + frusemide beta-D-glucuronoside | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| UDP-glucuronosyltransferase | - |
Homo sapiens |
| UGT | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
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Release 2023.1 (January 2023)
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