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Literature summary extracted from

  • Penning, T.M.; Mukharji, I.; Barrows, S.; Talalay, P.
    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.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.213 6alpha-Methylprednisolone
-
 Rattus norvegicus
1.1.1.213 acetaminophen non-competitive, only androsterone oxidation, pH 7.0 Rattus norvegicus
1.1.1.213 arachidonic acid
-
 Rattus norvegicus
1.1.1.213 aspirin salicylate, non-competitive, only androsterone oxidation, pH 7.0 Rattus norvegicus
1.1.1.213 Betamethasone non-competitive Rattus norvegicus
1.1.1.213 cortisol competitive Rattus norvegicus
1.1.1.213 cortisone competitive Rattus norvegicus
1.1.1.213 dexamethasone non-competitive Rattus norvegicus
1.1.1.213 Ibuprofen competitive Rattus norvegicus
1.1.1.213 indomethacin competitive, IC50 for reduction of 9,10-phenanthrenequinone is 0.000735 mM and of androsterone 0.00333 mM Rattus norvegicus
1.1.1.213 Meclofenamic acid competitive Rattus norvegicus
1.1.1.213 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
1.1.1.213 non-steroidal anti-inflamatory drug competitive Rattus norvegicus
1.1.1.213 Oxyphenybutazone competitive Rattus norvegicus
1.1.1.213 Prednisolone competitive Rattus norvegicus
1.1.1.213 Prednisone competitive Rattus norvegicus
1.1.1.213 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
1.1.1.213 prostaglandin A1
-
 Rattus norvegicus
1.1.1.213 Prostaglandin B1
-
 Rattus norvegicus
1.1.1.213 prostaglandin E1
-
 Rattus norvegicus
1.1.1.213 prostaglandin F1alpha
-
 Rattus norvegicus
1.1.1.213 pyrazole 10% at 0.4 mM Rattus norvegicus
1.1.1.213 salicylate non-competitive Rattus norvegicus
1.1.1.213 Tolmetin competitive, only androsterone oxidation, pH 7.0 Rattus norvegicus
1.1.1.213 Zomepirac competitive, only androsterone oxidation, pH 7.0 Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.213 cytosol
-
 Rattus norvegicus 5829
-

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
1.1.1.213 33000
-
 1 * 33000 gel filtration Rattus norvegicus
1.1.1.213 34000
-
 1 * 34000 SDS-PAGE Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.213 17beta-hydroxy-5alpha-androstan-3-one + NAD(P)H + H+ Rattus norvegicus conversion in animal tissues 3alpha,17beta-dihydroxy-5alpha-androstan + NAD(P)+
-
 ?
1.1.1.213 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

EC Number Organism UniProt Comment Textmining
1.1.1.213 Rattus norvegicus
-
 male, adult
-
1.1.1.213 Rattus norvegicus
-
 Sprangue-Dawley
-
1.1.1.213 Rattus norvegicus Sprangue-Dawley
-
 Sprangue-Dawley
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.213 CaCl2 and ammonium sulfate fractionation, DEAE-cellulose- and hydroxyapatite chromatography, chromatofocusing, Sephadex G-100 Rattus norvegicus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.213 liver
-
 Rattus norvegicus
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.1.1.213 0.008 4 determined for several substrates,with best activities for 9,10-phenanthrenequinone, 4-nitrobezaldehyde and androsterone Rattus norvegicus
1.1.1.213 3.19
-
-
 Rattus norvegicus

Storage Stability

EC Number Storage Stability Organism
1.1.1.213 -80°C, 20 mM potassium phosphate buffer, pH 7.0, 1 mM EDTA, 1 mM DTT, 30% glycerol Rattus norvegicus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.213 1-acenaphthenol + NAD(P)+ pH 9.0 Rattus norvegicus 1-acenaphthenone + NAD(P)H + H+
-
 ?
1.1.1.213 1-acenaphthenol + NAD(P)+ pH 9.0 Rattus norvegicus Sprangue-Dawley 1-acenaphthenone + NAD(P)H + H+
-
 ?
1.1.1.213 17beta-hydroxy-5alpha-androstan-3-one + NAD(P)H + H+ conversion in animal tissues Rattus norvegicus 3alpha,17beta-dihydroxy-5alpha-androstan + NAD(P)+
-
 ?
1.1.1.213 3alpha-hydroxy-5alpha-androstan-17-one + NAD+ pH 9.0 Rattus norvegicus 5alpha-androstan-3,17-dione + NADH
-
 ?
1.1.1.213 3alpha-hydroxy-5alpha-androstan-17-one + NAD+ pH 9.0 Rattus norvegicus Sprangue-Dawley 5alpha-androstan-3,17-dione + NADH
-
 ?
1.1.1.213 4-nitroacetophenone + NAD(P)H pH 6.0 Rattus norvegicus 1-(4-nitrophenyl)ethanol + NAD(P)+
-
 ?
1.1.1.213 4-nitrobenzaldehyde + NAD(P)H pH 6.0 Rattus norvegicus (4-nitrophenyl)methanol + NAD(P)+
-
 ?
1.1.1.213 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
1.1.1.213 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
1.1.1.213 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)+
-
 ?
1.1.1.213 9,10-phenanthrenequinone + NAD(P)H pH 6.0 Rattus norvegicus ? + NAD(P)+
-
 ?
1.1.1.213 benzenedihydrodiol + NAD(P)+ pH 9.0 Rattus norvegicus ?
-
 ?
1.1.1.213 benzenedihydrodiol + NAD(P)+ pH 9.0 Rattus norvegicus Sprangue-Dawley ?
-
 ?
1.1.1.213 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 ?
-
 ?
1.1.1.213 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

EC Number Subunits Comment Organism
1.1.1.213 monomer 1 * 34000 SDS-PAGE Rattus norvegicus
1.1.1.213 monomer 1 * 33000 gel filtration Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.213 25
-
 assay at Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.213 additional information for a number of substrates the reactions are more efficient in the presence of NADPH and NADP+ Rattus norvegicus
1.1.1.213 NAD+
-
 Rattus norvegicus
1.1.1.213 NADH
-
 Rattus norvegicus
1.1.1.213 NADP+
-
 Rattus norvegicus
1.1.1.213 NADPH
-
 Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.213 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
1.1.1.213 0.0002
-
 indomethacin competitive, for 9,10-phenanthrenequinone and 5alpha-androstane-3,17-dione reduction at pH 6.0 Rattus norvegicus
1.1.1.213 0.0008
-
 Prostaglandin B1 androsterone oxidation Rattus norvegicus
1.1.1.213 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
1.1.1.213 0.0031
-
 prostaglandin A1 androsterone oxidation Rattus norvegicus
1.1.1.213 0.0045
-
 Betamethasone androsterone oxidation Rattus norvegicus
1.1.1.213 0.006
-
 arachidonic acid androsterone oxidation Rattus norvegicus
1.1.1.213 0.0075
-
 prostaglandin E1 androsterone oxidation Rattus norvegicus
1.1.1.213 0.0075
-
 6alpha-Methylprednisolone androsterone oxidation Rattus norvegicus
1.1.1.213 0.01
-
 dexamethasone androsterone oxidation Rattus norvegicus
1.1.1.213 0.012
-
 prostaglandin F1alpha androsterone oxidation Rattus norvegicus
1.1.1.213 0.0175
-
 Prednisolone androsterone oxidation Rattus norvegicus
1.1.1.213 0.0175
-
 Prednisone androsterone oxidation Rattus norvegicus
1.1.1.213 0.115 0.75 salicylate
-
 Rattus norvegicus
1.1.1.213 0.19
-
 cortisol androsterone oxidation Rattus norvegicus
1.1.1.213 0.285
-
 cortisone androsterone oxidation Rattus norvegicus
1.1.1.213 0.65
-
 aspirin for androsterone oxidation Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.213 0.000735
-
 competitive, IC50 for reduction of 9,10-phenanthrenequinone by NADPH at pH6.0 is 0.000735 mM Rattus norvegicus indomethacin
1.1.1.213 0.00333
-
 competitive, IC50 for oxidation of androsterone by NAD+ at pH 7.0 0.00333 mM Rattus norvegicus indomethacin