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Literature summary for 1.14.14.55 extracted from
- Inhibition of CYP3A4 and CYP3A5 catalyzed metabolism of alprazolam and quinine by ketoconazole as racemate and four different enantiomers (2007), Eur. J. Clin. Pharmacol., 63, 173-179.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| ketoconazole | i.e. KTZ, is a antifungal drug, known as an inhibitor of, especially, the CYP3A subfamily, KTZ racemate and four separate enantiomers are evaluated for their selectivity in inhibiting quinine metabolism | Homo sapiens |  |
| ketoconazole 2R,4R enantiomer | - |
Homo sapiens | |
| ketoconazole 2R,4S enantiomer | - |
Homo sapiens | |
| ketoconazole 2S,4R enantiomer | - |
Homo sapiens | |
| ketoconazole 2S,4S enantiomer | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetics | Homo sapiens |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Homo sapiens | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| quinine + [reduced NADPH-hemoprotein reductase] + O2 | Homo sapiens | - |
3-hydroxyquinine + [oxidized NADPH-hemoprotein reductase] + H2O | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| native enzyme partially by microsome preparation | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| quinine + [reduced NADPH-hemoprotein reductase] + O2 | - |
Homo sapiens | 3-hydroxyquinine + [oxidized NADPH-hemoprotein reductase] + H2O | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| CYP3A4 | - |
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 |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| NADPH | - |
Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.004 | - |
pH 7.4, 37°C | Homo sapiens | ketoconazole 2S,4S enantiomer | |
| 0.01 | - |
pH 7.4, 37°C | Homo sapiens | ketoconazole racemate | |
| 0.011 | - |
pH 7.4, 37°C | Homo sapiens | ketoconazole 2S,4R enantiomer | |
| 0.014 | - |
pH 7.4, 37°C | Homo sapiens | ketoconazole 2R,4S enantiomer | |
| 0.023 | - |
pH 7.4, 37°C | Homo sapiens | ketoconazole 2R,4R enantiomer | |
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