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Literature summary for 1.1.1.50 extracted from

  • Steckelbroeck, S.; Jin, Y.; Gopishetty, S.; Oyesanmi, B.; Penning, T.M.
    Human cytosolic 3alpha-hydroxysteroid dehydrogenases of the aldo-keto reductase superfamily display significant 3beta-hydroxysteroid dehydrogenase activity: implications for steroid hormone metabolism and action (2004), J. Biol. Chem., 279, 10784-10795.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
overexpression of isozymes AKR1C1-AKR1C4 in Escherichia coli Homo sapiens

Inhibitors

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

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Natural Substrates/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens Q04828 4 isozymes AKR1C1-AKR1C4
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzymes from Escherichia coli by DE52 and Blue Sepharose chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell hepatoma cell, expresses isozymes AKR1C1-AKR1C3 Homo sapiens
-

Specific Activity [micromol/min/mg]

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 and Products (Substrate)

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

Synonyms Comment Organism
3alpha-HSD
-
Homo sapiens
3alpha-hydroxysteroid dehydrogenase
-
Homo sapiens
AKR1C
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

Turnover Number [1/s]

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

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NAD+
-
Homo sapiens
NADP+
-
Homo sapiens
NADPH dependent on Homo sapiens