Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.1.1.357 extracted from

  • Endo, S.; Matsunaga, T.; Ikari, A.; El-Kabbani, O.; Hara, A.; Kitade, Y.
    Identification of a determinant for strict NADP(H)-specificity and high sensitivity to mixed-type steroid inhibitor of rabbit aldo-keto reductase 1C33 by site-directed mutagenesis (2015), Arch. Biochem. Biophys., 569, 19-25.
    View publication on PubMed

Protein Variants

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

Inhibitors Comment Organism Structure
NADPH inhibition pattern is competitive Oryctolagus cuniculus

KM Value [mM]

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

Organism UniProt Comment Textmining
Oryctolagus cuniculus T2HVB4
-
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
AKR1C33
-
Oryctolagus cuniculus
Naloxone reductase 2
-
Oryctolagus cuniculus

Turnover Number [1/s]

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 [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 [mM/s]

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