Activating Compound | Comment | Organism | Structure |
---|---|---|---|
cholesterol 3-sulfate | i.e. CH-35 | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
His-tagged enzyme | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
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 | Comment | Organism |
---|---|---|
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 | Comment | Organism | Structure |
---|---|---|---|
clobenpropit | complete inhibition | Homo sapiens | |
thioperamide | 66% inhibition | Homo sapiens | |
tranylcypromine | complete inhibition | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0015 | - |
(24S)-24-hydroxycholesterol | recombinant truncation mutant enzyme | Homo sapiens | |
0.0033 | - |
cholesterol 3-sulfate | recombinant truncation mutant enzyme | Homo sapiens | |
0.0039 | - |
(24S)-24-hydroxycholesterol | recombinant wild-type enzyme | Homo sapiens | |
0.0049 | - |
cholesterol 3-sulfate | recombinant wild-type enzyme | Homo sapiens | |
0.0054 | - |
cholesterol | recombinant wild-type enzyme | Homo sapiens | |
0.0077 | - |
cholesterol | recombinant truncation mutant enzyme | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Fe2+ | a heme-containing cytochrome P450 enzyme | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
cholesterol + [reduced NADPH-hemoprotein reductase] + H+ + O2 | Homo sapiens | - |
(24S)-24-hydroxycholesterol + [oxidized NADPH-hemoprotein reductase] + H2O | - |
r |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q9Y6A2 | - |
- |
Purification (Comment) | Organism |
---|---|
recombinant His-tagged enzyme by nickel affinity chromatography | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
brain | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
cholesterol + [reduced NADPH-hemoprotein reductase] + H+ + O2 | - |
Homo sapiens | (24S)-24-hydroxycholesterol + [oxidized NADPH-hemoprotein reductase] + H2O | - |
r | |
cholesterol 3-sulfate + [reduced NADPH-hemoprotein reductase] + H+ + O2 | - |
Homo sapiens | (24S)-24-hydroxycholesterol 3-sulfate + [oxidized NADPH-hemoprotein reductase] + H2O | - |
? | |
additional information | active site structure and substrate binding, overview | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
CYP46A1 | - |
Homo sapiens |
cytochrome P450 46A1 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0018 | - |
cholesterol | recombinant wild-type enzyme | Homo sapiens | |
0.0072 | - |
cholesterol | recombinant truncation mutant enzyme | Homo sapiens | |
0.0076 | - |
cholesterol 3-sulfate | recombinant wild-type enzyme | Homo sapiens | |
0.0142 | - |
(24S)-24-hydroxycholesterol | recombinant truncation mutant enzyme | Homo sapiens | |
0.0153 | - |
(24S)-24-hydroxycholesterol | recombinant wild-type enzyme | Homo sapiens | |
0.042 | - |
cholesterol 3-sulfate | recombinant truncation mutant enzyme | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.2 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
cytochrome P450 | - |
Homo sapiens | |
heme | - |
Homo sapiens | |
NADPH | - |
Homo sapiens |