Cloned (Comment) | Organism |
---|---|
overexpression of isozymes AKR1C1-AKR1C4 in Escherichia coli | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
Flufenamic acid | nonsteroidal anti-inflammatory drug, inhibits all 4 isozymes, binding mode | Homo sapiens | |
NADPH | strongly inhibits the 3alpha-hydroxysteroid oxidase activity | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
cytosol | - |
Homo sapiens | 5829 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
4-pregnen-3alpha,20beta-diol + NAD+ | Homo sapiens | - |
(20beta)-20-hydroxypregn-4-en-3-one + NADH + H+ | - |
ir | |
5alpha-dihydroprogesterone + 2 NADPH + 2 H+ | Homo sapiens | - |
pregnan-3alpha,20beta-diol + 2 NADP+ | - |
? | |
5alpha-dihydroprogesterone + 2 NADPH + 2 H+ | Homo sapiens | inactivation of the potent androgen, 3alpha(beta)-hydroxysteroid oxidoreductase activity | pregnan-3alpha,20beta-diol + 2 NADP+ | - |
ir | |
additional information | Homo sapiens | in vivo the isozymes act predominantly as 3-ketosteroid reductases due to inhibition by NADPH, but significantly produce 3beta-tetrahydrosteroids physiologically important in steroid metabolim, androgen metabolism, overview | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q04828 | 4 isozymes AKR1C1-AKR1C4 | - |
Purification (Comment) | Organism |
---|---|
recombinant enzymes from Escherichia coli by DE52 and Blue Sepharose chromatography | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
Hep-G2 cell | hepatoma cell, expresses isozymes AKR1C1-AKR1C3 | Homo sapiens | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
0.0037 | - |
purified recombinant isozyme AKR1C3, substrate 4-pregnen-3alpha,20beta-diol | Homo sapiens |
0.0039 | - |
purified recombinant isozyme AKR1C1, substrate 4-pregnen-3alpha,20beta-diol | Homo sapiens |
0.119 | - |
purified recombinant isozyme AKR1C4, substrate 4-pregnen-3alpha,20beta-diol | Homo sapiens |
76.1 | - |
purified recombinant isozyme AKR1C2, substrate 4-pregnen-3alpha,20beta-diol | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
4-pregnen-3alpha,20beta-diol + NAD+ | - |
Homo sapiens | (20beta)-20-hydroxypregn-4-en-3-one + NADH + H+ | - |
? | |
4-pregnen-3alpha,20beta-diol + NAD+ | - |
Homo sapiens | (20beta)-20-hydroxypregn-4-en-3-one + NADH + H+ | - |
ir | |
5alpha-dihydroprogesterone + 2 NADPH + 2 H+ | - |
Homo sapiens | pregnan-3alpha,20beta-diol + 2 NADP+ | - |
? | |
5alpha-dihydroprogesterone + 2 NADPH + 2 H+ | inactivation of the potent androgen, 3alpha(beta)-hydroxysteroid oxidoreductase activity | Homo sapiens | pregnan-3alpha,20beta-diol + 2 NADP+ | - |
ir | |
additional information | in vivo the isozymes act predominantly as 3-ketosteroid reductases due to inhibition by NADPH, but significantly produce 3beta-tetrahydrosteroids physiologically important in steroid metabolim, androgen metabolism, overview | Homo sapiens | ? | - |
? | |
additional information | stereospecificity differs between the isozymes, the enzyme also exhibits in vitro 3alpha[17beta]-hydroxysteroid axidase activity with 3alpha-diol as the substrate | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
3alpha-HSD | - |
Homo sapiens |
3alpha-hydroxysteroid dehydrogenase | - |
Homo sapiens |
AKR1C | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0023 | - |
4-pregnen-3alpha,20beta-diol | pH 7.0, 25°C, isozyme AKR1C3 | Homo sapiens | |
0.0025 | - |
4-pregnen-3alpha,20beta-diol | pH 7.0, 25°C, isozyme AKR1C1 | Homo sapiens | |
0.046 | - |
4-pregnen-3alpha,20beta-diol | pH 7.0, 25°C, isozyme AKR1C2 | Homo sapiens | |
0.0735 | - |
4-pregnen-3alpha,20beta-diol | pH 7.0, 25°C, isozyme AKR1C4 | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NAD+ | - |
Homo sapiens | |
NADP+ | - |
Homo sapiens | |
NADPH | dependent on | Homo sapiens |