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Literature summary extracted from
- Crystal structures of substrate-bound and substrate-free cytochrome P450 46A1, the principal cholesterol hydroxylase in the brain (2008), Proc. Natl. Acad. Sci. USA, 105, 9546-9551.
Activating Compound
| EC Number | Activating Compound | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.14.14.25 | cholesterol 3-sulfate | i.e. CH-35 | Homo sapiens |  |
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 1.14.14.25 | His-tagged enzyme | Homo sapiens |
Crystallization (Commentary)
| EC Number | Crystallization (Comment) | Organism |
|---|---|---|
| 1.14.14.25 | a recombinant C-terminally His4-tagged CYP46A1 lacking the first 50 N-terminal amino acid residues, substrate-free enzyme or enzyme in complex with cholesterol 3-sulfate, X-ray diffraction structure determination and analysis at 2.4 A and 1.9 A resolution, respectively, structure modeling | Homo sapiens |
Protein Variants
| EC Number | Protein Variants | Comment | Organism |
|---|---|---|---|
| 1.14.14.25 | additional information | construction of an mutant CYP46A1, in which the first 50 N-terminal amino acid residues are deleted, and a His4 tag is added at the C-terminus. The truncation removed a 23-residue transmembrane-anchoring domain and renders this membrane P450 more soluble compared to the wild-type, overview | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.14.14.25 | clobenpropit | complete inhibition | Homo sapiens | |
| 1.14.14.25 | thioperamide | 66% inhibition | Homo sapiens | |
| 1.14.14.25 | tranylcypromine | complete inhibition | Homo sapiens | |
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 1.14.14.25 | 0.0015 | - |
(24S)-24-hydroxycholesterol | recombinant truncation mutant enzyme | Homo sapiens | |
| 1.14.14.25 | 0.0033 | - |
cholesterol 3-sulfate | recombinant truncation mutant enzyme | Homo sapiens | |
| 1.14.14.25 | 0.0039 | - |
(24S)-24-hydroxycholesterol | recombinant wild-type enzyme | Homo sapiens | |
| 1.14.14.25 | 0.0049 | - |
cholesterol 3-sulfate | recombinant wild-type enzyme | Homo sapiens | |
| 1.14.14.25 | 0.0054 | - |
cholesterol | recombinant wild-type enzyme | Homo sapiens | |
| 1.14.14.25 | 0.0077 | - |
cholesterol | recombinant truncation mutant enzyme | Homo sapiens | |
Metals/Ions
| EC Number | Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.14.14.25 | Fe2+ | a heme-containing cytochrome P450 enzyme | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.14.14.25 | cholesterol + [reduced NADPH-hemoprotein reductase] + H+ + O2 | Homo sapiens | - |
(24S)-24-hydroxycholesterol + [oxidized NADPH-hemoprotein reductase] + H2O | - |
r | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.14.14.25 | Homo sapiens | Q9Y6A2 | - |
- |
Purification (Commentary)
| EC Number | Purification (Comment) | Organism |
|---|---|---|
| 1.14.14.25 | recombinant His-tagged enzyme by nickel affinity chromatography | Homo sapiens |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 1.14.14.25 | brain | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.14.14.25 | cholesterol + [reduced NADPH-hemoprotein reductase] + H+ + O2 | - |
Homo sapiens | (24S)-24-hydroxycholesterol + [oxidized NADPH-hemoprotein reductase] + H2O | - |
r | |
| 1.14.14.25 | cholesterol 3-sulfate + [reduced NADPH-hemoprotein reductase] + H+ + O2 | - |
Homo sapiens | (24S)-24-hydroxycholesterol 3-sulfate + [oxidized NADPH-hemoprotein reductase] + H2O | - |
? | |
| 1.14.14.25 | additional information | active site structure and substrate binding, overview | Homo sapiens | ? | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 1.14.14.25 | CYP46A1 | - |
Homo sapiens |
| 1.14.14.25 | cytochrome P450 46A1 | - |
Homo sapiens |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 1.14.14.25 | 37 | - |
assay at | Homo sapiens |
Turnover Number [1/s]
| EC Number | Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 1.14.14.25 | 0.0018 | - |
cholesterol | recombinant wild-type enzyme | Homo sapiens | |
| 1.14.14.25 | 0.0072 | - |
cholesterol | recombinant truncation mutant enzyme | Homo sapiens | |
| 1.14.14.25 | 0.0076 | - |
cholesterol 3-sulfate | recombinant wild-type enzyme | Homo sapiens | |
| 1.14.14.25 | 0.0142 | - |
(24S)-24-hydroxycholesterol | recombinant truncation mutant enzyme | Homo sapiens | |
| 1.14.14.25 | 0.0153 | - |
(24S)-24-hydroxycholesterol | recombinant wild-type enzyme | Homo sapiens | |
| 1.14.14.25 | 0.042 | - |
cholesterol 3-sulfate | recombinant truncation mutant enzyme | Homo sapiens | |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 1.14.14.25 | 7.2 | - |
assay at | Homo sapiens |
Cofactor
| EC Number | Cofactor | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.14.14.25 | cytochrome P450 | - |
Homo sapiens | |
| 1.14.14.25 | heme | - |
Homo sapiens | |
| 1.14.14.25 | NADPH | - |
Homo sapiens | |
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