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Literature summary extracted from

  • Penning, T.M.; Jin, Y.; Steckelbroeck, S.; Lanisnik Rizner, T.; Lewis, M.
    Structure-function of human 3alpha-hydroxysteroid dehydrogenases: genes and proteins (2004), Mol. Cell. Endocrinol., 215, 63-72.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.50 isozymes AKR1C1-AKR1C4, genetic organization, transient expression in COS-1 cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.50 NADPH strongly inhibits the oxidation of 3-hydroxymetabolites in vivo and in vitro, determining the role of enzymes as 3-ketosteroid reductases in vivo, overview Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.50 0.0035
-
 androsterone pH 7.4, 25°C, recombinant isozyme AKR1C2 and isozyme AKR1C4 Homo sapiens
1.1.1.50 0.017
-
 benzenedihydrodiol pH 7.4, 25°C, recombinant isozyme AKR1C4 Homo sapiens
1.1.1.50 0.022
-
 1-Acenaphthenol pH 7.4, 25°C, recombinant isozyme AKR1C1 and isozyme AKR1C2 Homo sapiens
1.1.1.50 0.048
-
 1-Indanol pH 7.4, 25°C, recombinant isozyme AKR1C1 Homo sapiens
1.1.1.50 0.07
-
 1-Acenaphthenol pH 7.4, 25°C, recombinant isozyme AKR1C3 Homo sapiens
1.1.1.50 0.14
-
 1-Acenaphthenol pH 7.4, 25°C, recombinant isozyme AKR1C4 Homo sapiens
1.1.1.50 0.15
-
 benzenedihydrodiol pH 7.4, 25°C, recombinant isozyme AKR1C1 Homo sapiens
1.1.1.50 0.17
-
 1-Indanol pH 7.4, 25°C, recombinant isozyme AKR1C4 Homo sapiens
1.1.1.50 0.32
-
 benzenedihydrodiol pH 7.4, 25°C, recombinant isozyme AKR1C3 Homo sapiens
1.1.1.50 0.94
-
 1-Indanol pH 7.4, 25°C, recombinant isozyme AKR1C2 Homo sapiens
1.1.1.50 1.4
-
 1-Indanol pH 7.4, 25°C, recombinant isozyme AKR1C3 Homo sapiens
1.1.1.50 1.8
-
 benzenedihydrodiol pH 7.4, 25°C, recombinant isozyme AKR1C2 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.50 5alpha-dihydroprogesterone + 2 NADPH + 2 H+ Homo sapiens in the prostate: forward reaction by type 2 isozyme AKR1C3, reverse reaction by type 3 isozyme AKR1C2 pregnan-3alpha,20beta-diol + 2 NADP+
-
 ir
1.1.1.50 5alpha-dihydroprogesterone + NADPH + H+ Homo sapiens in the CNS: both reaction directions by type 3 isozyme AKR1C2 3alpha,5alpha-3-hydroxypregnan-20-one + NADP+
-
 r
1.1.1.50 additional information Homo sapiens role of the isozymes in bile acid biosynthesis and steroid metabolism, product profiling, pre-receptor regulation of steroid hormone action, overview ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.50 Homo sapiens
-
 4 isozymes AKR1C1-AKR1C4
-

Reaction

EC Number Reaction Comment Organism Reaction ID
1.1.1.50 a 3alpha-hydroxysteroid + NAD(P)+ = a 3-oxosteroid + NAD(P)H + H+ steroid substrate recognition mechanism by isozymes AKR1C1-AKR1C4, Tyr55 is involved in catalysis, ordered bi bi mechanism Homo sapiens
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.50 Hep-G2 cell hepatoma cell Homo sapiens
-
1.1.1.50 liver specific isozyme AKR1C4 Homo sapiens
-
1.1.1.50 mammary gland isozyme AKR1C3 Homo sapiens
-
1.1.1.50 additional information tissue specificity and substrate specificity of human isozymes, overview Homo sapiens
-
1.1.1.50 prostate isozyme AKR1C2 Homo sapiens
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.1.1.50 additional information
-
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.50 1-acenaphthenol + NADP+ isozymes AKR1C1-AKR1C4 Homo sapiens ?
-
 r
1.1.1.50 1-indanol + NADP+ isozymes AKR1C1-AKR1C4 Homo sapiens ?
-
 r
1.1.1.50 17beta-estradiol + NADP+
-
 Homo sapiens estrone + NADPH
-
 r
1.1.1.50 5alpha-dihydroprogesterone + 2 NADPH + 2 H+
-
 Homo sapiens pregnan-3alpha,20beta-diol + 2 NADP+
-
 ir
1.1.1.50 5alpha-dihydroprogesterone + 2 NADPH + 2 H+ in the prostate: forward reaction by type 2 isozyme AKR1C3, reverse reaction by type 3 isozyme AKR1C2 Homo sapiens pregnan-3alpha,20beta-diol + 2 NADP+
-
 ir
1.1.1.50 5alpha-dihydroprogesterone + NADPH + H+
-
 Homo sapiens 3alpha,5alpha-3-hydroxypregnan-20-one + NADP+
-
 r
1.1.1.50 5alpha-dihydroprogesterone + NADPH + H+ in the CNS: both reaction directions by type 3 isozyme AKR1C2 Homo sapiens 3alpha,5alpha-3-hydroxypregnan-20-one + NADP+
-
 r
1.1.1.50 5alpha-dihydroprogesterone + NADPH + H+ isozymes AKR1C1-AKR1C4 Homo sapiens (3alpha,5alpha)-3-hydroxypregnan-20-one + NADP+
-
 r
1.1.1.50 androsterone + NADP+ isozymes AKR1C2, and AKR1C4 Homo sapiens androstane-3,17-dione + NADPH
-
 r
1.1.1.50 benzenedihydrodiol + NADP+ isozymes AKR1C1-AKR1C4 Homo sapiens ?
-
 r
1.1.1.50 additional information role of the isozymes in bile acid biosynthesis and steroid metabolism, product profiling, pre-receptor regulation of steroid hormone action, overview Homo sapiens ?
-
 ?
1.1.1.50 additional information structure-function study, the isozymes provide 3alpha-, 17beta-, and 20alpha-hydroxysteroid oxidase activity as well as 3-, 17-, and 20-ketosteroid reductase activity in vitro Homo sapiens ?
-
 ?
1.1.1.50 testosterone + NADP+ isozymes AKR1C1-AKR1C4 Homo sapiens 4-androstene-3,17-dione + NADPH + H+
-
 r

Synonyms

EC Number Synonyms Comment Organism
1.1.1.50 3alpha-hydroxysteroid dehydrogenase
-
 Homo sapiens
1.1.1.50 AKR1C
-
 Homo sapiens
1.1.1.50 bile-acid binding protein i.e. type 3 isozyme AKR1C2 Homo sapiens
1.1.1.50 chlordecone reductase i.e. type 1 isozyme AKR1C4 Homo sapiens
1.1.1.50 DD2 i.e. type 3 isozyme AKR1C2 Homo sapiens
1.1.1.50 DD21 i.e. isozyme AKR1C1 Homo sapiens
1.1.1.50 dihydrodiol dehydrogenase i.e. type 1 isozyme AKR1C4 Homo sapiens
1.1.1.50 HSD
-
 Homo sapiens
1.1.1.50 More the isozymes belong to the AKR1C subfamily of the aldo-keto-reductase AKR superfamily Homo sapiens
1.1.1.50 prostaglandin F2alpha-synthase i.e. type 2 isozyme AKR1C3 Homo sapiens
1.1.1.50 type 5 17beta-hydroxysteroid dehydrogenase i.e. type 2 isozyme AKR1C3 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.50 25
-
 assay at Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.1.1.50 0.0018
-
 androsterone pH 7.4, 25°C, recombinant isozyme AKR1C4 Homo sapiens
1.1.1.50 0.007
-
 androsterone pH 7.4, 25°C, recombinant isozyme AKR1C2 Homo sapiens
1.1.1.50 0.015
-
 benzenedihydrodiol pH 7.4, 25°C, recombinant isozyme AKR1C3 Homo sapiens
1.1.1.50 0.02
-
 benzenedihydrodiol pH 7.4, 25°C, recombinant isozyme AKR1C2 Homo sapiens
1.1.1.50 0.03
-
 benzenedihydrodiol pH 7.4, 25°C, recombinant isozyme AKR1C4 Homo sapiens
1.1.1.50 0.05
-
 benzenedihydrodiol pH 7.4, 25°C, recombinant isozyme AKR1C1 Homo sapiens
1.1.1.50 0.09
-
 1-Indanol pH 7.4, 25°C, recombinant isozyme AKR1C3 Homo sapiens
1.1.1.50 0.13
-
 1-Acenaphthenol pH 7.4, 25°C, recombinant isozyme AKR1C4 Homo sapiens
1.1.1.50 0.158
-
 1-Indanol pH 7.4, 25°C, recombinant isozyme AKR1C4 Homo sapiens
1.1.1.50 0.163
-
 1-Indanol pH 7.4, 25°C, recombinant isozyme AKR1C2 Homo sapiens
1.1.1.50 0.21
-
 1-Indanol pH 7.4, 25°C, recombinant isozyme AKR1C1 Homo sapiens
1.1.1.50 0.42
-
 1-Acenaphthenol pH 7.4, 25°C, recombinant isozyme AKR1C3 Homo sapiens
1.1.1.50 0.49
-
 1-Acenaphthenol pH 7.4, 25°C, recombinant isozyme AKR1C1 Homo sapiens
1.1.1.50 0.59
-
 1-Acenaphthenol pH 7.4, 25°C, recombinant isozyme AKR1C2 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.50 7.4
-
 assay at Homo sapiens