Protein Variants | Comment | Organism |
---|---|---|
F217S | mutation converts AKR1C33 into a dually coenzyme-specific form and abolishes the activity towards 3-keto-5beta-cholestanes that are substrates specific to AKR1C33, and markedly decreases the sensitivity to 4-pregnenes | Oryctolagus cuniculus |
N272T | mutation does not influence cofactor specificity | Oryctolagus cuniculus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
NADPH | inhibition pattern is competitive | Oryctolagus cuniculus |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0001 | - |
5alpha-androstan-17-beta-ol-3-one | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0002 | - |
NADP+ | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0002 | - |
5alpha-pregnan-20alpha-ol-3-one | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0003 | - |
5alpha-pregnan-20alpha-ol-3-one | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0004 | - |
NADPH | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0005 | - |
5beta-pregnane-3,20-dione | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0006 | - |
5beta-androstan-3,17-dione | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0006 | - |
5beta-Androstan-3alpha-ol-17-one | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0009 | - |
Dehydrolithocholic acid | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0021 | - |
5beta-Androstan-3alpha-ol-17-one | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0023 | - |
5beta-pregnane-3,20-dione | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.003 | - |
5beta-androstan-3,17-dione | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.003 | - |
5alpha-androstan-17-beta-ol-3-one | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.004 | - |
Dehydrolithocholic acid | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0084 | - |
NADPH | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.009 | - |
NADPH | mutant N272T, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.017 | - |
NADP+ | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.017 | - |
NADP+ | mutant N272T, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.033 | - |
NADH | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.081 | - |
NAD+ | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.97 | - |
NAD+ | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
1 | - |
NAD+ | mutant N272T, pH 7.4, 25°C | Oryctolagus cuniculus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Oryctolagus cuniculus | T2HVB4 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
5alpha-androstan-17-beta-ol-3-one + NADH + H+ | NADH is not a substrate for wild-type | Oryctolagus cuniculus | 5alpha-androstane-3alpha,17beta-diol + NAD+ | - |
r | |
5alpha-androstan-17-beta-ol-3-one + NADPH + H+ | - |
Oryctolagus cuniculus | 5alpha-androstane-3alpha,17beta-diol + NADP+ | - |
r | |
5alpha-androstane-3alpha,17beta-diol + NAD+ | - |
Oryctolagus cuniculus | 5alpha-androstan-17-beta-ol-3-one + NADH + H+ | - |
r | |
5alpha-androstane-3alpha,17beta-diol + NADP+ | - |
Oryctolagus cuniculus | 5alpha-androstan-17-beta-ol-3-one + NADPH + H+ | - |
r | |
5alpha-pregnan-20alpha-ol-3-one + NADP+ | - |
Oryctolagus cuniculus | 5alpha-pregnane-3,20-dione + NADPH + H+ | - |
r | |
5beta-androstan-3,17-dione + NADPH + H+ | - |
Oryctolagus cuniculus | 5beta-androstan-3alpha-ol-17-one + NADP+ | - |
r | |
5beta-androstan-3alpha-ol-17-one + NADP+ | - |
Oryctolagus cuniculus | 5beta-androstan-3,17-dione + NADPH + H+ | - |
r | |
5beta-pregnane-3,20-dione + NADPH + H+ | - |
Oryctolagus cuniculus | 5beta-pregnan-20alpha-ol-3-one + NADP+ | - |
r | |
dehydrolithocholic acid + NADPH + H+ | - |
Oryctolagus cuniculus | ? | - |
r | |
additional information | enzyme is strictly NADPH-specific | Oryctolagus cuniculus | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
AKR1C33 | - |
Oryctolagus cuniculus |
Naloxone reductase 2 | - |
Oryctolagus cuniculus |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0025 | - |
5alpha-pregnan-20alpha-ol-3-one | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.004 | - |
5beta-Androstan-3alpha-ol-17-one | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.004 | - |
5alpha-androstan-17-beta-ol-3-one | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.006 | - |
NADP+ | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.006 | - |
Dehydrolithocholic acid | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.007 | - |
5beta-pregnane-3,20-dione | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.009 | - |
5beta-androstan-3,17-dione | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.01 | - |
NADPH | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.037 | - |
Dehydrolithocholic acid | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.05 | - |
5alpha-pregnan-20alpha-ol-3-one | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.053 | - |
5beta-pregnane-3,20-dione | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.077 | - |
NADPH | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.1 | - |
NADPH | mutant N272T, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.113 | - |
5beta-Androstan-3alpha-ol-17-one | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.14 | - |
5beta-androstan-3,17-dione | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.367 | - |
5alpha-androstan-17-beta-ol-3-one | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.72 | - |
NADP+ | mutant N272T, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.85 | - |
NADP+ | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000015 | - |
NADPH | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
0.0046 | - |
NADPH | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
9 | - |
NADPH | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus | |
11 | - |
NADPH | mutant N272T, pH 7.4, 25°C | Oryctolagus cuniculus | |
27 | - |
NADPH | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
28 | - |
NADP+ | mutant F217S, pH 7.4, 25°C | Oryctolagus cuniculus | |
42 | - |
NADP+ | mutant N272T, pH 7.4, 25°C | Oryctolagus cuniculus | |
50 | - |
NADP+ | wild-type, pH 7.4, 25°C | Oryctolagus cuniculus |