Cloned (Comment) | Organism |
---|---|
wild-type enzyme and mutants are overexpressed in Escherichia coli DH5alpha | Rattus norvegicus |
Protein Variants | Comment | Organism |
---|---|---|
W148Y | site-directed mutagenesis, kinetically similar to wild type enzyme, no function in ligand binding | Rattus norvegicus |
W227Y | site-directed mutagenesis, important role in binding steroid hormones, but not small substrates or inhibitors, interacts with the C and/or D-rings of steroid ligand | Rattus norvegicus |
W86Y | site-directed mutagenesis, important in binding steroids and non-steroidal anti-inflamatory drugs, region in which it resides is part of the substrate/inhibitor binding pocket, near the A-, and B-rings of bound steroid | Rattus norvegicus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(E/Z)-sulfindac | wild-type, W86Y and W227Y | Rattus norvegicus | |
1,10-phenanthroline | wild-type, W86Y and W227Y | Rattus norvegicus | |
1,7-phenanthroline | wild-type, W86Y and W227Y | Rattus norvegicus | |
Flufenamic acid | wild-type, W86Y and W227Y | Rattus norvegicus | |
Hexestrol | - |
Rattus norvegicus | |
indomethacin | wild-type, W86Y and W227Y | Rattus norvegicus | |
Meclofenamic acid | wild-type, W86Y and W227Y | Rattus norvegicus | |
Mefenamic acid | wild-type, W86Y and W227Y | Rattus norvegicus | |
non-steroidal anti-inflamatory drug | - |
Rattus norvegicus | |
ponalrestat | wild-type, W86Y and W227Y, weak inhibitor | Rattus norvegicus | |
zopolrestat | wild-type, W86Y and W227Y, weak inhibitor | Rattus norvegicus |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00122 | 0.0051 | 9,10-phenanthrenequinone | - |
Rattus norvegicus | |
0.042 | 0.408 | 3alpha-hydroxy-5alpha-androstan-17-one | - |
Rattus norvegicus | |
0.163 | 0.211 | 4-nitrobenzaldehyde | - |
Rattus norvegicus | |
3.54 | 33.7 | 2-decalone | - |
Rattus norvegicus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
17beta-hydroxy-5alpha-androstan-3-one + NAD(P)H + H+ | Rattus norvegicus | - |
3alpha,17beta-dihydroxy-5alpha-androstan + NAD(P)+ | - |
? | |
additional information | Rattus norvegicus | inactivating circulating androgens, progestins and glucocorticoids. Regulation of hormone levels in endocrine target tissues and in carcinogen actibation | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
- |
- |
Purification (Comment) | Organism |
---|---|
anion exchange and Blue Sepharose column | Rattus norvegicus |
Reaction | Comment | Organism | Reaction ID |
---|---|---|---|
a 3alpha-hydroxysteroid + NAD(P)+ = a 3-oxosteroid + NAD(P)H + H+ | aldoketoreductase superfamily | Rattus norvegicus | |
a 3alpha-hydroxysteroid + NAD(P)+ = a 3-oxosteroid + NAD(P)H + H+ | bi bi mechanism, pyridine nucleotide binds before substrate | Rattus norvegicus |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Rattus norvegicus | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
0.059 | - |
W86Y mutant | Rattus norvegicus |
0.08 | - |
W227Y mutant | Rattus norvegicus |
0.674 | - |
W148Y mutant | Rattus norvegicus |
1.5 | - |
native enzyme | Rattus norvegicus |
Storage Stability | Organism |
---|---|
-70°C, 20 mM potassium phosphate buffer, pH 7.0, 1 mM EDTA, 1 mM beta-mercaptoethanol, 30% glycerol | Rattus norvegicus |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
17beta-hydroxy-5alpha-androstan-3-one + NAD(P)H + H+ | - |
Rattus norvegicus | 3alpha,17beta-dihydroxy-5alpha-androstan + NAD(P)+ | - |
? | |
2-decalone + NADH | pH 6.0 | Rattus norvegicus | ? + NAD+ | - |
? | |
3alpha-hydroxy-5alpha-androstan-17-one + NAD+ | - |
Rattus norvegicus | 5alpha-androstan-3,17-dione + NADH | - |
r | |
4-nitrobenzaldehyde + NAD(P)H | pH 6.0 | Rattus norvegicus | (4-nitrophenyl)methanol + NAD(P)+ | - |
? | |
4-nitrobenzaldehyde + NAD(P)H | NADH as cofactor | Rattus norvegicus | (4-nitrophenyl)methanol + NAD(P)+ | - |
? | |
9,10-phenanthrenequinone + NAD(P)H | NADPH | Rattus norvegicus | ? + NAD(P)+ | - |
? | |
9,10-phenanthrenequinone + NAD(P)H | pH 6.0 | Rattus norvegicus | ? + NAD(P)+ | - |
? | |
additional information | inactivating circulating androgens, progestins and glucocorticoids. Regulation of hormone levels in endocrine target tissues and in carcinogen actibation | Rattus norvegicus | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
More | (alpha/beta)8-barrel fold | Rattus norvegicus |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
1.17 | 3.93 | 9,10-phenanthrenequinone | - |
Rattus norvegicus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
additional information | 4-pro-R-hydride transfer of the nicotinamide cofactor | Rattus norvegicus | |
NAD+ | - |
Rattus norvegicus | |
NADH | - |
Rattus norvegicus | |
NADPH | - |
Rattus norvegicus |