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Literature summary for 1.1.1.213 extracted from
- Purification and properties of a 3alpha-hydroxysteroid dehydrogenase of rat liver cytosol and its inhibition by anti-inflammatory drugs (1984), Biochem. J., 222, 601-611.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 6alpha-Methylprednisolone | - |
Rattus norvegicus |  |
| acetaminophen | non-competitive, only androsterone oxidation, pH 7.0 | Rattus norvegicus | |
| arachidonic acid | - |
Rattus norvegicus | |
| aspirin | salicylate, non-competitive, only androsterone oxidation, pH 7.0 | Rattus norvegicus | |
| Betamethasone | non-competitive | Rattus norvegicus | |
| cortisol | competitive | Rattus norvegicus | |
| cortisone | competitive | Rattus norvegicus | |
| dexamethasone | non-competitive | Rattus norvegicus | |
| Ibuprofen | competitive | Rattus norvegicus | |
| indomethacin | competitive, IC50 for reduction of 9,10-phenanthrenequinone is 0.000735 mM and of androsterone 0.00333 mM | Rattus norvegicus | |
| Meclofenamic acid | competitive | Rattus norvegicus | |
| additional information | not inhibited by dicoumarol, disulfiram and barbiturates. Inhibitory potency of non-steroidal anti-inflamatory drugs and salicylates falls sharply as the pH is increased from 6 to 9 | Rattus norvegicus | |
| non-steroidal anti-inflamatory drug | competitive | Rattus norvegicus | |
| Oxyphenybutazone | competitive | Rattus norvegicus | |
| Prednisolone | competitive | Rattus norvegicus | |
| Prednisone | competitive | Rattus norvegicus | |
| Prostaglandin | A1, B1, E1, F1, F1alpha, A2, B2, E2 and F2alpha, inhibit 9,10-phenanthrenequinone reduction and androsterone oxidation, the order of inhibitory potency is related to their lipophilicity | Rattus norvegicus | |
| prostaglandin A1 | - |
Rattus norvegicus | |
| Prostaglandin B1 | - |
Rattus norvegicus | |
| prostaglandin E1 | - |
Rattus norvegicus | |
| prostaglandin F1alpha | - |
Rattus norvegicus | |
| pyrazole | 10% at 0.4 mM | Rattus norvegicus | |
| salicylate | non-competitive | Rattus norvegicus | |
| Tolmetin | competitive, only androsterone oxidation, pH 7.0 | Rattus norvegicus | |
| Zomepirac | competitive, only androsterone oxidation, pH 7.0 | Rattus norvegicus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytosol | - |
Rattus norvegicus | 5829 | - |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 33000 | - |
1 * 33000 gel filtration | Rattus norvegicus |
| 34000 | - |
1 * 34000 SDS-PAGE | Rattus norvegicus |
Natural Substrates/ Products (Substrates)
| 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 | conversion in animal tissues | 3alpha,17beta-dihydroxy-5alpha-androstan + NAD(P)+ | - |
? | |
| 5beta-pregnane-17alpha,20beta,21-triol-3,11-dione + NAD(P)H | Rattus norvegicus | hepatic reduction in animal tissues | 5beta-pregnane-3alpha,17alpha,20beta,21-tetraol-11-one + NAD(P)+ | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Rattus norvegicus | - |
male, adult | - |
| Rattus norvegicus | - |
Sprangue-Dawley | - |
| Rattus norvegicus Sprangue-Dawley | - |
Sprangue-Dawley | - |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| CaCl2 and ammonium sulfate fractionation, DEAE-cellulose- and hydroxyapatite chromatography, chromatofocusing, Sephadex G-100 | Rattus norvegicus |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | - |
Rattus norvegicus | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 0.008 | 4 | determined for several substrates,with best activities for 9,10-phenanthrenequinone, 4-nitrobezaldehyde and androsterone | Rattus norvegicus |
| 3.19 | - |
- |
Rattus norvegicus |
Storage Stability
| Storage Stability | Organism |
|---|---|
| -80°C, 20 mM potassium phosphate buffer, pH 7.0, 1 mM EDTA, 1 mM DTT, 30% glycerol | Rattus norvegicus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 1-acenaphthenol + NAD(P)+ | pH 9.0 | Rattus norvegicus | 1-acenaphthenone + NAD(P)H + H+ | - |
? | |
| 1-acenaphthenol + NAD(P)+ | pH 9.0 | Rattus norvegicus Sprangue-Dawley | 1-acenaphthenone + NAD(P)H + H+ | - |
? | |
| 17beta-hydroxy-5alpha-androstan-3-one + NAD(P)H + H+ | conversion in animal tissues | Rattus norvegicus | 3alpha,17beta-dihydroxy-5alpha-androstan + NAD(P)+ | - |
? | |
| 3alpha-hydroxy-5alpha-androstan-17-one + NAD+ | pH 9.0 | Rattus norvegicus | 5alpha-androstan-3,17-dione + NADH | - |
? | |
| 3alpha-hydroxy-5alpha-androstan-17-one + NAD+ | pH 9.0 | Rattus norvegicus Sprangue-Dawley | 5alpha-androstan-3,17-dione + NADH | - |
? | |
| 4-nitroacetophenone + NAD(P)H | pH 6.0 | Rattus norvegicus | 1-(4-nitrophenyl)ethanol + NAD(P)+ | - |
? | |
| 4-nitrobenzaldehyde + NAD(P)H | pH 6.0 | Rattus norvegicus | (4-nitrophenyl)methanol + NAD(P)+ | - |
? | |
| 5alpha-androstan-3,17-dione + NAD(P)H | pH 6.0 for reduction, pH 7.0 and 9.0 for androsterone oxidation | Rattus norvegicus | 3alpha-hydroxy-5alpha-androstan-17-one + NAD(P)+ | - |
r | |
| 5alpha-androstan-3,17-dione + NAD(P)H | pH 6.0 for reduction, pH 7.0 and 9.0 for androsterone oxidation | Rattus norvegicus Sprangue-Dawley | 3alpha-hydroxy-5alpha-androstan-17-one + NAD(P)+ | - |
r | |
| 5beta-pregnane-17alpha,20beta,21-triol-3,11-dione + NAD(P)H | hepatic reduction in animal tissues | Rattus norvegicus | 5beta-pregnane-3alpha,17alpha,20beta,21-tetraol-11-one + NAD(P)+ | - |
? | |
| 9,10-phenanthrenequinone + NAD(P)H | pH 6.0 | Rattus norvegicus | ? + NAD(P)+ | - |
? | |
| benzenedihydrodiol + NAD(P)+ | pH 9.0 | Rattus norvegicus | ? | - |
? | |
| benzenedihydrodiol + NAD(P)+ | pH 9.0 | Rattus norvegicus Sprangue-Dawley | ? | - |
? | |
| additional information | the enzyme displays a distinct preference for the reduction of quinones, e.g. 9,10-phenanthrenequinone, and 3-oxo steroids, e.g. androstane, pregnane and cholane, over aromatic aldehydes and ketones, whereas 3alpha-hydroxy steroids are overwhelmingly more efficiently oxidized than are 1-acenaphthenol or benzenedihydrodiol. Ethanol and 3beta-hydroxy steroids no substrates | Rattus norvegicus | ? | - |
? | |
| additional information | the enzyme displays a distinct preference for the reduction of quinones, e.g. 9,10-phenanthrenequinone, and 3-oxo steroids, e.g. androstane, pregnane and cholane, over aromatic aldehydes and ketones, whereas 3alpha-hydroxy steroids are overwhelmingly more efficiently oxidized than are 1-acenaphthenol or benzenedihydrodiol. Ethanol and 3beta-hydroxy steroids no substrates | Rattus norvegicus Sprangue-Dawley | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| monomer | 1 * 34000 SDS-PAGE | Rattus norvegicus |
| monomer | 1 * 33000 gel filtration | Rattus norvegicus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 25 | - |
assay at | Rattus norvegicus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| additional information | for a number of substrates the reactions are more efficient in the presence of NADPH and NADP+ | Rattus norvegicus | |
| NAD+ | - |
Rattus norvegicus | |
| NADH | - |
Rattus norvegicus | |
| NADP+ | - |
Rattus norvegicus | |
| NADPH | - |
Rattus norvegicus | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | more Ki values given for different inhibitors of androsterone oxidation, 9,10-phenanthrenequinone- and 5alpha-androstane-3,17-dione reduction | Rattus norvegicus | |
| 0.0002 | - |
indomethacin | competitive, for 9,10-phenanthrenequinone and 5alpha-androstane-3,17-dione reduction at pH 6.0 | Rattus norvegicus | |
| 0.0008 | - |
Prostaglandin B1 | androsterone oxidation | Rattus norvegicus | |
| 0.000835 | - |
indomethacin | competitive for androstene oxidation at pH 7.0. IC50 is 0.003 mM at H 7.0, 0.045 at pH 9.0 | Rattus norvegicus | |
| 0.0031 | - |
prostaglandin A1 | androsterone oxidation | Rattus norvegicus | |
| 0.0045 | - |
Betamethasone | androsterone oxidation | Rattus norvegicus | |
| 0.006 | - |
arachidonic acid | androsterone oxidation | Rattus norvegicus | |
| 0.0075 | - |
prostaglandin E1 | androsterone oxidation | Rattus norvegicus | |
| 0.0075 | - |
6alpha-Methylprednisolone | androsterone oxidation | Rattus norvegicus | |
| 0.01 | - |
dexamethasone | androsterone oxidation | Rattus norvegicus | |
| 0.012 | - |
prostaglandin F1alpha | androsterone oxidation | Rattus norvegicus | |
| 0.0175 | - |
Prednisolone | androsterone oxidation | Rattus norvegicus | |
| 0.0175 | - |
Prednisone | androsterone oxidation | Rattus norvegicus | |
| 0.115 | 0.75 | salicylate | - |
Rattus norvegicus | |
| 0.19 | - |
cortisol | androsterone oxidation | Rattus norvegicus | |
| 0.285 | - |
cortisone | androsterone oxidation | Rattus norvegicus | |
| 0.65 | - |
aspirin | for androsterone oxidation | Rattus norvegicus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000735 | - |
competitive, IC50 for reduction of 9,10-phenanthrenequinone by NADPH at pH6.0 is 0.000735 mM | Rattus norvegicus | indomethacin | |
| 0.00333 | - |
competitive, IC50 for oxidation of androsterone by NAD+ at pH 7.0 0.00333 mM | Rattus norvegicus | indomethacin | |
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