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Literature summary for 1.3.1.3 extracted from
- Substrate specificity and inhibitor analyses of human steroid 5beta-reductase (AKR1D1) (2011), Steroids, 76, 484-490.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4-benzoylbenzoic acid | - |
Homo sapiens |  |
| chenodeoxycholic acid | - |
Homo sapiens | |
| indomethacin | - |
Homo sapiens | |
| Mefenamic acid | - |
Homo sapiens | |
| additional information | substrate inhibition is observed with C18 to C21 steroids provided that the C11 position is unsubstituted | Homo sapiens | |
| Ursodeoxycholic acid | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0003 | - |
cholestenone | pH 6.0, 37°C | Homo sapiens | |
| 0.0008 | - |
4-cholesten-7alpha-ol-3-one | pH 6.0, 37°C | Homo sapiens | |
| 0.0009 | - |
4-androstene-3,17-dione | pH 6.0, 37°C | Homo sapiens | |
| 0.0022 | - |
corticosterone | pH 6.0, 37°C | Homo sapiens | |
| 0.0025 | - |
aldosterone | pH 6.0, 37°C | Homo sapiens | |
| 0.0027 | - |
testosterone | pH 6.0, 37°C | Homo sapiens | |
| 0.0029 | - |
Epitestosterone | pH 6.0, 37°C | Homo sapiens | |
| 0.003 | - |
4-estren-17beta-ol-3-one | pH 6.0, 37°C | Homo sapiens | |
| 0.0032 | - |
1,4-androstadien-17beta-ol-3-one | pH 6.0, 37°C | Homo sapiens | |
| 0.0131 | - |
cortisol | pH 6.0, 37°C | Homo sapiens | |
| 0.0151 | - |
cortisone | pH 6.0, 37°C | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 1,4-androstadien-17beta-ol-3-one + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 4-androstene-3,17-dione + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 4-cholesten-7alpha-ol-3-one + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 4-estren-17beta-ol-3-one + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| aldosterone + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| cholestenone + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| corticosterone + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| cortisol + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| cortisone + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| epitestosterone + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| additional information | substrate specificity of homogeneous human recombinant AKR1D1 using C18, C19, C21, and C27 DELTA4-ketosteroids, AKR1D1 proficiently reduces all the steroids tested at physiological pH, overview | Homo sapiens | ? | - |
? | |
| testosterone + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| AKR1D1 | - |
Homo sapiens |
| aldo-keto reductase 1D1 | - |
Homo sapiens |
| steroid 5beta-reductase | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.01 | - |
cholestenone | pH 6.0, 37°C | Homo sapiens | |
| 0.032 | - |
corticosterone | pH 6.0, 37°C | Homo sapiens | |
| 0.033 | - |
4-cholesten-7alpha-ol-3-one | pH 6.0, 37°C | Homo sapiens | |
| 0.035 | - |
1,4-androstadien-17beta-ol-3-one | pH 6.0, 37°C | Homo sapiens | |
| 0.045 | - |
cortisol | pH 6.0, 37°C | Homo sapiens | |
| 0.045 | - |
4-estren-17beta-ol-3-one | pH 6.0, 37°C | Homo sapiens | |
| 0.1 | - |
4-androstene-3,17-dione | pH 6.0, 37°C | Homo sapiens | |
| 0.1 | - |
Epitestosterone | pH 6.0, 37°C | Homo sapiens | |
| 0.14 | - |
testosterone | pH 6.0, 37°C | Homo sapiens | |
| 0.15 | - |
aldosterone | pH 6.0, 37°C | Homo sapiens | |
| 0.195 | - |
cortisone | pH 6.0, 37°C | Homo sapiens | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 6 | - |
- |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| NADPH | - |
Homo sapiens | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| additional information | existence of a small alternative substrate binding pocket, structure-activity relationship, overview | Homo sapiens |
| physiological function | human steroid 5beta-reductase, i.e. aldo-keto reductase 1D1, catalyzes the stereospecific NADPH-dependent reduction of the C4-C5 double bond of DELTA4-ketosteroids to yield an A/B cis-ring junction. This cis configuration is crucial for bile acid biosynthesis and plays important roles in steroid metabolism. AKR1D1 is the only enzyme necessary for all the 5-steroid metabolites present in humans | Homo sapiens |
kcat/KM [mM/s]
| kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 2.77 | - |
4-androstene-3,17-dione | pH 6.0, 37°C | Homo sapiens | |
| 3.44 | - |
cortisol | pH 6.0, 37°C | Homo sapiens | |
| 10.94 | - |
1,4-androstadien-17beta-ol-3-one | pH 6.0, 37°C | Homo sapiens | |
| 12.91 | - |
cortisone | pH 6.0, 37°C | Homo sapiens | |
| 14.54 | - |
corticosterone | pH 6.0, 37°C | Homo sapiens | |
| 15 | - |
4-estren-17beta-ol-3-one | pH 6.0, 37°C | Homo sapiens | |
| 33.33 | - |
cholestenone | pH 6.0, 37°C | Homo sapiens | |
| 34.48 | - |
Epitestosterone | pH 6.0, 37°C | Homo sapiens | |
| 41.25 | - |
4-cholesten-7alpha-ol-3-one | pH 6.0, 37°C | Homo sapiens | |
| 51.85 | - |
testosterone | pH 6.0, 37°C | Homo sapiens | |
| 60 | - |
aldosterone | pH 6.0, 37°C | Homo sapiens | |
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