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Literature summary for 2.4.1.17 extracted from
- Regulation of UDP-glucuronosyltransferase (UGT) 1A1 by progesterone and its impact on labetalol elimination (2008), Xenobiotica, 38, 62-75.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| effect of female hormones progesterone, oestradiol, oestriol, or oestrone on the promoter activities of relevant UGTs in Hep-G2 cells, real-time reverse transcription-PCR analysis, transcriptional regulation of isozyme UGT1A1, overview | Homo sapiens |
| effect of female hormones progesterone, oestradiol, oestriol, or oestrone on the promoter activities of relevant UGTs in HepG2 cells, real-time reverse transcription-PCR analysis, overview | Homo sapiens |
| effect of female hormones progesterone, oestradiol, oestriol, or oestrone on the promoter activities of relevant UGTs in HepG2 cells, real-time reverse transcription-PCR analysis, transcriptional regulation of isozyme UGT2B7, overview | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.368 | - |
labetalol | pH 7.5, 37°C, recombinant isozyme UGT1A9 | Homo sapiens |  |
| 0.386 | - |
labetalol | pH 7.5, 37°C, recombinant isozyme UGT2B7 | Homo sapiens | |
| 0.956 | - |
labetalol | pH 7.5, 37°C, recombinant isozyme UGT1A1 | 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. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | regulation of isozyme UGT1A1 by progesterone and its impact on labetalol elimination, overview | ? | - |
? | |
| UDP-D-glucuronate + acceptor | Homo sapiens | UGT isozyme substrate specificity, overview | UDP + acceptor beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + labetalol | Homo sapiens | - |
UDP + ? | - |
? | |
| UDP-D-glucuronate + labetalol | Homo sapiens | the reaction is catalyzed mainly by isozymes UGT1A1 and UGT2B7, overview | UDP + ? | - |
? | |
| UDP-D-glucuronate + labetalol | Homo sapiens | the reaction is catalyzed mainly by isozymes UGT1A1 and UGT2B7, potential role for progesterone in regulating labetalol elimination by modulating the expression of UGT1A1, leading to enhanced drug metabolism during pregnancy, overview | UDP + ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | O60656 | isozyme UGT1A9; isozyme UGT1A9 | - |
| Homo sapiens | P06133 | isozyme UGT2B4; isozyme UGT2B4 | - |
| Homo sapiens | P16662 | isozyme UGT2B7; isozyme UGT2B7 | - |
| Homo sapiens | P19224 | isozyme UGT1A6; isozyme UGT1A6 | - |
| Homo sapiens | P22309 | isozyme UGT1A1; isozyme UGT1A1 | - |
| Homo sapiens | P22310 | isozyme UGT1A4; isozyme UGT1A4 | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | recombinant isozyme UGT1A1 | Homo sapiens | - |
| commercial preparation | recombinant isozyme UGT2B7 | Homo sapiens | - |
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | regulation of isozyme UGT1A1 by progesterone and its impact on labetalol elimination, overview | Homo sapiens | ? | - |
? | |
| UDP-D-glucuronate + acceptor | - |
Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + acceptor | UGT isozyme substrate specificity, overview | Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + labetalol | - |
Homo sapiens | UDP + ? | - |
? | |
| UDP-D-glucuronate + labetalol | the reaction is catalyzed mainly by isozymes UGT1A1 and UGT2B7, overview | Homo sapiens | UDP + ? | - |
? | |
| UDP-D-glucuronate + labetalol | the reaction is catalyzed mainly by isozymes UGT1A1 and UGT2B7, potential role for progesterone in regulating labetalol elimination by modulating the expression of UGT1A1, leading to enhanced drug metabolism during pregnancy, overview | Homo sapiens | UDP + ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| UDP-glucuronosyltransferase 1A1 | - |
Homo sapiens |
| UGT1A1 | - |
Homo sapiens |
| UGT1A4 | - |
Homo sapiens |
| UGT1A6 | - |
Homo sapiens |
| UGT1A9 | - |
Homo sapiens |
| UGT2B4 | - |
Homo sapiens |
| UGT2B7 | - |
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 |
|---|---|---|---|
| 7.5 | - |
assay at | Homo sapiens |
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