Cloned (Comment) | Organism |
---|---|
isozymes AKR1C1-AKR1C4, genetic organization, transient expression in COS-1 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
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] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0035 | - |
androsterone | pH 7.4, 25°C, recombinant isozyme AKR1C2 and isozyme AKR1C4 | Homo sapiens | |
0.017 | - |
benzenedihydrodiol | pH 7.4, 25°C, recombinant isozyme AKR1C4 | Homo sapiens | |
0.022 | - |
1-Acenaphthenol | pH 7.4, 25°C, recombinant isozyme AKR1C1 and isozyme AKR1C2 | Homo sapiens | |
0.048 | - |
1-Indanol | pH 7.4, 25°C, recombinant isozyme AKR1C1 | Homo sapiens | |
0.07 | - |
1-Acenaphthenol | pH 7.4, 25°C, recombinant isozyme AKR1C3 | Homo sapiens | |
0.14 | - |
1-Acenaphthenol | pH 7.4, 25°C, recombinant isozyme AKR1C4 | Homo sapiens | |
0.15 | - |
benzenedihydrodiol | pH 7.4, 25°C, recombinant isozyme AKR1C1 | Homo sapiens | |
0.17 | - |
1-Indanol | pH 7.4, 25°C, recombinant isozyme AKR1C4 | Homo sapiens | |
0.32 | - |
benzenedihydrodiol | pH 7.4, 25°C, recombinant isozyme AKR1C3 | Homo sapiens | |
0.94 | - |
1-Indanol | pH 7.4, 25°C, recombinant isozyme AKR1C2 | Homo sapiens | |
1.4 | - |
1-Indanol | pH 7.4, 25°C, recombinant isozyme AKR1C3 | Homo sapiens | |
1.8 | - |
benzenedihydrodiol | pH 7.4, 25°C, recombinant isozyme AKR1C2 | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
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 | |
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 | |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
4 isozymes AKR1C1-AKR1C4 | - |
Reaction | Comment | Organism | Reaction ID |
---|---|---|---|
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 |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
Hep-G2 cell | hepatoma cell | Homo sapiens | - |
liver | specific isozyme AKR1C4 | Homo sapiens | - |
mammary gland | isozyme AKR1C3 | Homo sapiens | - |
additional information | tissue specificity and substrate specificity of human isozymes, overview | Homo sapiens | - |
prostate | isozyme AKR1C2 | Homo sapiens | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
additional information | - |
- |
Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
1-acenaphthenol + NADP+ | isozymes AKR1C1-AKR1C4 | Homo sapiens | ? | - |
r | |
1-indanol + NADP+ | isozymes AKR1C1-AKR1C4 | Homo sapiens | ? | - |
r | |
17beta-estradiol + NADP+ | - |
Homo sapiens | estrone + NADPH | - |
r | |
5alpha-dihydroprogesterone + 2 NADPH + 2 H+ | - |
Homo sapiens | pregnan-3alpha,20beta-diol + 2 NADP+ | - |
ir | |
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 | |
5alpha-dihydroprogesterone + NADPH + H+ | - |
Homo sapiens | 3alpha,5alpha-3-hydroxypregnan-20-one + NADP+ | - |
r | |
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 | |
5alpha-dihydroprogesterone + NADPH + H+ | isozymes AKR1C1-AKR1C4 | Homo sapiens | (3alpha,5alpha)-3-hydroxypregnan-20-one + NADP+ | - |
r | |
androsterone + NADP+ | isozymes AKR1C2, and AKR1C4 | Homo sapiens | androstane-3,17-dione + NADPH | - |
r | |
benzenedihydrodiol + NADP+ | isozymes AKR1C1-AKR1C4 | Homo sapiens | ? | - |
r | |
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 | ? | - |
? | |
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 | ? | - |
? | |
testosterone + NADP+ | isozymes AKR1C1-AKR1C4 | Homo sapiens | 4-androstene-3,17-dione + NADPH + H+ | - |
r |
Synonyms | Comment | Organism |
---|---|---|
3alpha-hydroxysteroid dehydrogenase | - |
Homo sapiens |
AKR1C | - |
Homo sapiens |
bile-acid binding protein | i.e. type 3 isozyme AKR1C2 | Homo sapiens |
chlordecone reductase | i.e. type 1 isozyme AKR1C4 | Homo sapiens |
DD2 | i.e. type 3 isozyme AKR1C2 | Homo sapiens |
DD21 | i.e. isozyme AKR1C1 | Homo sapiens |
dihydrodiol dehydrogenase | i.e. type 1 isozyme AKR1C4 | Homo sapiens |
HSD | - |
Homo sapiens |
More | the isozymes belong to the AKR1C subfamily of the aldo-keto-reductase AKR superfamily | Homo sapiens |
prostaglandin F2alpha-synthase | i.e. type 2 isozyme AKR1C3 | Homo sapiens |
type 5 17beta-hydroxysteroid dehydrogenase | i.e. type 2 isozyme AKR1C3 | Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0018 | - |
androsterone | pH 7.4, 25°C, recombinant isozyme AKR1C4 | Homo sapiens | |
0.007 | - |
androsterone | pH 7.4, 25°C, recombinant isozyme AKR1C2 | Homo sapiens | |
0.015 | - |
benzenedihydrodiol | pH 7.4, 25°C, recombinant isozyme AKR1C3 | Homo sapiens | |
0.02 | - |
benzenedihydrodiol | pH 7.4, 25°C, recombinant isozyme AKR1C2 | Homo sapiens | |
0.03 | - |
benzenedihydrodiol | pH 7.4, 25°C, recombinant isozyme AKR1C4 | Homo sapiens | |
0.05 | - |
benzenedihydrodiol | pH 7.4, 25°C, recombinant isozyme AKR1C1 | Homo sapiens | |
0.09 | - |
1-Indanol | pH 7.4, 25°C, recombinant isozyme AKR1C3 | Homo sapiens | |
0.13 | - |
1-Acenaphthenol | pH 7.4, 25°C, recombinant isozyme AKR1C4 | Homo sapiens | |
0.158 | - |
1-Indanol | pH 7.4, 25°C, recombinant isozyme AKR1C4 | Homo sapiens | |
0.163 | - |
1-Indanol | pH 7.4, 25°C, recombinant isozyme AKR1C2 | Homo sapiens | |
0.21 | - |
1-Indanol | pH 7.4, 25°C, recombinant isozyme AKR1C1 | Homo sapiens | |
0.42 | - |
1-Acenaphthenol | pH 7.4, 25°C, recombinant isozyme AKR1C3 | Homo sapiens | |
0.49 | - |
1-Acenaphthenol | pH 7.4, 25°C, recombinant isozyme AKR1C1 | Homo sapiens | |
0.59 | - |
1-Acenaphthenol | pH 7.4, 25°C, recombinant isozyme AKR1C2 | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |