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Literature summary for 2.4.1.17 extracted from
- Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases (2007), Drug Metab. Dispos., 35, 2006-2014.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| isozyme UGT1A3, DNA and amino acid sequence determination and analysis, overexpression of isozyme UGT1A3 in HEK-293 cells | Homo sapiens |
| isozyme UGT1A3, DNA and amino acid sequence determination and analysis, overexpression of isozymes UGT1A3 and UGT1A8 in HEK-293 cells | Homo sapiens |
| overexpression of isozyme UGT1A8 in HEK-293 cells | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.004 | - |
trans-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT2B7 | Homo sapiens |  |
| 0.0074 | - |
cis-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A7 | Homo sapiens | |
| 0.015 | - |
cis-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT2B7 | Homo sapiens | |
| 0.018 | - |
cis-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT2B17 | Homo sapiens | |
| 0.02 | - |
cis-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT2B15 | Homo sapiens | |
| 0.023 | - |
trans-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A8 | Homo sapiens | |
| 0.03 | - |
cis-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A10 | Homo sapiens | |
| 0.041 | - |
cis-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT2B17 | Homo sapiens | |
| 0.056 | - |
cis-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A8 | Homo sapiens | |
| 0.07 | - |
cis-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A9 | Homo sapiens | |
| 0.094 | - |
trans-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A3 | Homo sapiens | |
| 0.096 | - |
trans-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A10 | Homo sapiens | |
| 0.124 | - |
trans-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A1 | Homo sapiens | |
| 0.165 | - |
cis-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A3 | Homo sapiens | |
| 0.166 | - |
trans-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A7 | Homo sapiens | |
| 0.193 | - |
cis-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A1 | Homo sapiens | |
| 0.319 | - |
trans-4-hydroxytamoxifen | pH 7.4, 37°C, isozyme UGT1A9 | 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 + 4-hydroxy-N-desmethyl-tamoxifen | Homo sapiens | the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview | UDP + 4-hydroxy-N-desmethyl-tamoxifen beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + acceptor | Homo sapiens | the enzyme is involved in detoxification reactions | UDP + acceptor beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + cis-4-hydroxytamoxifen | Homo sapiens | the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview | UDP + 4-hydroxytamoxifen beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + tamoxifen + H+ | Homo sapiens | the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview | UDP + tamoxifen beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + trans-4-hydroxytamoxifen | Homo sapiens | the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview | UDP + 4-hydroxytamoxifen beta-D-glucuronoside | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | O75795 | isozyme UGT2B17; isozyme UGT2B17 | - |
| Homo sapiens | P22309 | isozyme UGT1A1; isozyme UGT1A1 | - |
| Homo sapiens | P22309 | isozyme UGT2B7; isozyme UGT2B7 | - |
| Homo sapiens | P35503 | isozyme UGT1A3; isozyme UGT1A3 | - |
| Homo sapiens | P54855 | isozyme UGT2B15; isozyme UGT2B15 | - |
| Homo sapiens | Q9HAW7 | isozyme UGT1A7; isozyme UGT1A7 | - |
| Homo sapiens | Q9HAW8 | isozyme UGT1A10; isozyme UGT1A10 | - |
| Homo sapiens | Q9HAW9 | isozyme UGT1A8; isozyme UGT1A8 | - |
| Homo sapiens | Q9HAW9 | isozyme UGT1A9; isozyme UGT1A9 | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | isozyme UGT1A10 exhibits high overall glucuronidating activities compared to other UGT isozymes | Homo sapiens | ? | - |
? | |
| additional information | isozyme UGT1A8 exhibits high overall glucuronidating activities compared to other UGT isozymes | Homo sapiens | ? | - |
? | |
| additional information | isozyme UGT2B7 exhibits high overall glucuronidating activities compared to other UGT isozymes | Homo sapiens | ? | - |
? | |
| additional information | isozymes UGT1A10, UGT1A8, and UGT2B7 exhibit the highest overall glucuronidating activities of the UGT isozymes | Homo sapiens | ? | - |
? | |
| additional information | no activity by isozyme UGT2B15 with trans-4-hydroxytamoxifen | Homo sapiens | ? | - |
? | |
| UDP-D-glucuronate + 4-hydroxy-N-desmethyl-tamoxifen | the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview | Homo sapiens | UDP + 4-hydroxy-N-desmethyl-tamoxifen beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + 4-hydroxy-N-desmethyl-tamoxifen | i.e. endoxifen, substrate synthesis, overview, O-glucuronidation by liver microsomes | Homo sapiens | UDP + 4-hydroxy-N-desmethyl-tamoxifen beta-D-glucuronoside | product identification by HPLC and mass spectrometry analysis | ? | |
| UDP-D-glucuronate + acceptor | - |
Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + acceptor | the enzyme is involved in detoxification reactions | Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + cis-4-hydroxytamoxifen | the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview | Homo sapiens | UDP + 4-hydroxytamoxifen beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + cis-4-hydroxytamoxifen | N- and O-glucuronidation by liver microsomes | Homo sapiens | UDP + 4-hydroxytamoxifen beta-D-glucuronoside | product identification by HPLC and mass spectrometry analysis | ? | |
| UDP-D-glucuronate + tamoxifen + H+ | the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview | Homo sapiens | UDP + tamoxifen beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + tamoxifen + H+ | N- and O-glucuronidation by liver microsomes | Homo sapiens | UDP + tamoxifen beta-D-glucuronoside | product identification by HPLC and mass spectrometry analysis | ? | |
| UDP-D-glucuronate + trans-4-hydroxytamoxifen | the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview | Homo sapiens | UDP + 4-hydroxytamoxifen beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + trans-4-hydroxytamoxifen | N- and O-glucuronidation by liver microsomes | Homo sapiens | UDP + 4-hydroxytamoxifen beta-D-glucuronoside | product identification by HPLC and mass spectrometry analysis | ? | |
| UDP-D-glucuronate + trans-4-hydroxytamoxifen | N- and O-glucuronidation by liver microsomes, no activity by isozyme UGT2B15 | Homo sapiens | UDP + 4-hydroxytamoxifen beta-D-glucuronoside | product identification by HPLC and mass spectrometry analysis | ? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| UDP glucuronosyltransferase | - |
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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