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Literature summary for 2.4.1.17 extracted from
- Contribution of UDP-glucuronosyltransferase 1A1 and 1A8 to morphine-6-glucuronidation and its kinetic properties (2008), Drug Metab. Dispos., 36, 688-694.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of isozyme UGT1A1 in baculovirus-infected insect cells | Homo sapiens |
| expression of isozyme UGT1A8 in baculovirus-infected insect cells | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| morphine | - |
Homo sapiens |  |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetic analysis, isozyme UGT1A1 shows biphasic Michaelis-Menten kinetic behavior with substrate morphine, overview | Homo sapiens | |
| additional information | - |
additional information | kinetic analysis, isozyme UGT1A8 shows biphasic Michaelis-Menten kinetic behavior with substrate morphine, overview | Homo sapiens | |
| 0.0355 | - |
morphine | pH 7.5, 37°C, isozyme UGT1A8, at 0.05 mM morphine | Homo sapiens | |
| 0.0404 | - |
morphine | pH 7.5, 37°C, isozyme UGT1A1, at 0.05 mM morphine | Homo sapiens | |
| 0.0679 | - |
morphine | pH 7.5, 37°C, isozyme UGT1A1, at 2.5 mM morphine | Homo sapiens | |
| 0.0681 | - |
morphine | pH 7.5, 37°C, isozyme UGT1A8, at 2.5 mM morphine | 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 + morphine | Homo sapiens | the metabolic conversion of morphine to morphine-6-glucuronide plays a significant role in mediation of the clinical effect of morphine because of the superior analgesic effect of morphine-6-glucuronide | UDP + morphine 6-beta-D-glucuronoside | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
isozyme UGT1A8 | - |
| Homo sapiens | P22309 | isozyme UGT1A1; isozyme UGT1A1 | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| intestine | - |
Homo sapiens | - |
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | substrate specificity of UGT isozymes with morphine, overview, no or poor activity with isozymes UGT1A3, UGT1A4, UGT1A6, UGT1A7, UGT1A9, UGT1A10, UGT2B15, and UGT2B17 | Homo sapiens | ? | - |
? | |
| UDP-D-glucuronate + acceptor | - |
Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + morphine | the metabolic conversion of morphine to morphine-6-glucuronide plays a significant role in mediation of the clinical effect of morphine because of the superior analgesic effect of morphine-6-glucuronide | Homo sapiens | UDP + morphine 6-beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + morphine | isozyme UGT1A1, as the morphine concentration approaches 0.1 mM, morphine-6-glucuronidation activity gradually decreases, and the kinetics closely resemble substrate inhibition Michaelis-Menten kinetic behavior | Homo sapiens | UDP + morphine 6-beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + morphine | isozyme UGT1A8, as the morphine concentration approaches 0.1 mM, morphine-6-glucuronidation activity gradually decreases, and the kinetics closely resemble substrate inhibition Michaelis-Menten kinetic behavior | Homo sapiens | UDP + morphine 6-beta-D-glucuronoside | - |
? | |
| UDP-D-glucuronate + morphine | activity of isozyme UGT1A8 | Homo sapiens | UDP + morphine 3-beta-D-glucuronoside | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| UDP-glucuronosyltransferase 1A1 | - |
Homo sapiens |
| UDP-glucuronosyltransferase 1A8 | - |
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 |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.088 | - |
morphine | pH 7.5, 37°C, isozyme UGT1A8 | Homo sapiens | |
| 0.219 | - |
morphine | pH 7.5, 37°C, isozyme UGT1A1 | Homo sapiens | |
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