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Literature summary for 1.14.99.38 extracted from
- Cholesterol 25-hydroxylation activity of CYP3A (2011), J. Lipid Res., 52, 1509-1516.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| recombinant expression in insect cell microsomes via baculovirus transfection | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| additional information | in cells overexpressing human recombinant CYP3A4, the activity of cholesterol 25-hydroxylation is higher than that of cholesterol 4beta-hydroxylation, a known marker activity of CYP3A4 | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| desmosterol | a potent inhibitor of CH25H; a potent inhibitor of CH25H; a potent inhibitor of CH25H | Homo sapiens |  |
| desmosterol | a potent inhibitor of CH25H | Mus musculus | |
| troleandomycin | specific inhibitor of CYP3A | Homo sapiens | |
| troleandomycin | specific inhibitor of CYP3A | Mus musculus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Mus musculus | - |
- |
| microsome | - |
Homo sapiens | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| cholesterol + AH2 + O2 | Mus musculus | - |
25-hydroxycholesterol + A + H2O | - |
? | |
| cholesterol + AH2 + O2 | Homo sapiens | lower 25-hydroxylation enzyme activity by CYP1A2 compared to marker enzyme CYP3A4 | 25-hydroxycholesterol + A + H2O | - |
? | |
| cholesterol + AH2 + O2 | Homo sapiens | lower 25-hydroxylation enzyme activity by CYP2C9 compared to marker enzyme CYP3A4 | 25-hydroxycholesterol + A + H2O | - |
? | |
| cholesterol + AH2 + O2 | Homo sapiens | lower 25-hydroxylation enzyme activity by CYP2D6 compared to marker enzyme CYP3A4 | 25-hydroxycholesterol + A + H2O | - |
? | |
| cholesterol + AH2 + O2 | Homo sapiens | production of 25-hydroxycholesterol by intact CYP3A4, most significant activity is 25-hydroxylation, which is higher than that of 4beta-hydroxylation, a marker activity of CYP3A4 | 25-hydroxycholesterol + A + H2O | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P05177 | gene Ch25h | - |
| Homo sapiens | P08684 | gene Ch25h | - |
| Homo sapiens | P10635 | gene Ch25h | - |
| Homo sapiens | P11712 | gene Ch25h | - |
| Mus musculus | Q9Z0F5 | gene Ch25h | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| AML-12 cell | - |
Mus musculus | - |
| liver | - |
Mus musculus | - |
| liver | - |
Homo sapiens | - |
| additional information | 25-hydroxycholesterol concentrations in normal human sera correlates positively with the levels of 4beta-hydroxycholesterol, but does not significantly correlate with the levels of 27-hydroxycholesterol or (24S)-hydroxycholesterol | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| cholesterol + AH2 + O2 | - |
Mus musculus | 25-hydroxycholesterol + A + H2O | - |
? | |
| cholesterol + AH2 + O2 | - |
Homo sapiens | 25-hydroxycholesterol + A + H2O | - |
? | |
| cholesterol + AH2 + O2 | lower 25-hydroxylation enzyme activity by CYP1A2 compared to marker enzyme CYP3A4 | Homo sapiens | 25-hydroxycholesterol + A + H2O | - |
? | |
| cholesterol + AH2 + O2 | lower 25-hydroxylation enzyme activity by CYP2C9 compared to marker enzyme CYP3A4 | Homo sapiens | 25-hydroxycholesterol + A + H2O | - |
? | |
| cholesterol + AH2 + O2 | lower 25-hydroxylation enzyme activity by CYP2D6 compared to marker enzyme CYP3A4 | Homo sapiens | 25-hydroxycholesterol + A + H2O | - |
? | |
| cholesterol + AH2 + O2 | production of 25-hydroxycholesterol by intact CYP3A4, most significant activity is 25-hydroxylation, which is higher than that of 4beta-hydroxylation, a marker activity of CYP3A4 | Homo sapiens | 25-hydroxycholesterol + A + H2O | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| CH25H | - |
Mus musculus |
| CH25H | - |
Homo sapiens |
| CYP1A2 | - |
Homo sapiens |
| CYP2C9 | - |
Homo sapiens |
| CYP2D6 | - |
Homo sapiens |
| CYP3A | - |
Mus musculus |
| CYP3A4 | - |
Homo sapiens |
Expression
| Organism | Comment | Expression |
|---|---|---|
| Mus musculus | induction of CYP3A by pregnenolone-16 alpha-carbonitrile causes accumulation of 25-hydroxycholesterol in cell line AML12 derived from mouse liver, the induction is not suppressed by the addition of desmosterol. Although the transcription of Ch25h is also upregulated by addition of pregnenolone-16 alpha-carbonitrile, the protein level of CH25H is not elevated. Desmosterol does not affect the expression of cellular CYP3A protein, but CH25H protein level is obviously decreased by desmosterol treatment | up |
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