Inhibitors | Comment | Organism | Structure |
---|---|---|---|
bromazepam | competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 | Homo sapiens | |
cloxazolam | potent and specific, competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 | Homo sapiens | |
diazepam | competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 | Homo sapiens | |
estazolam | competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 | Homo sapiens | |
flunitrazepam | competitive inhibition of isozymes AKR1C1 and AKR1C2 | Homo sapiens | |
medazepam | competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 | Homo sapiens | |
additional information | no inhibition by oxazolam and oxazepam, benzodiazepams inhibit competitive versus the steroid substrates | Homo sapiens | |
nitrazepam | competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0006 | - |
5alpha-dihydroprogesterone | pH 7.0, 25°C, isozyme AKR1C2 | Homo sapiens | |
0.0007 | - |
5beta-dihydroprogesterone | pH 7.0, 25°C, isozyme AKR1C2 | Homo sapiens | |
0.0011 | - |
5alpha-dihydroprogesterone | pH 7.0, 25°C, isozyme AKR1C1 | Homo sapiens | |
0.0012 | - |
5beta-dihydroprogesterone | pH 7.0, 25°C, isozyme AKR1C1 | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | isozyme AKR1C2 is involved in neurosteroid biosynthesis, while isozyme AKE1C1 eliminates the neurosteroid precursor from the pathway and decreases the neurosteroid concentration in the brain, pathway overview | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isozymes AKR1C1, AKR1C2, and AKR1C4 | - |
Reaction | Comment | Organism | Reaction ID |
---|---|---|---|
a 3alpha-hydroxysteroid + NAD(P)+ = a 3-oxosteroid + NAD(P)H + H+ | isozymes AKR1C1 and AKR1C2 are bifunctional enzymes also showing minor 20alpha-hydroxysteroid dehydrogenase activity, EC 1.1.1.149 | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
5alpha-dihydroprogesterone + NADPH + H+ | isozyme AKR1C2 | Homo sapiens | 5alpha-hydroxy-pregnan-20-one + NADP+ | - |
? | |
5beta-dihydroprogesterone + NADPH | isozyme AKR1C1 and AKR1C2 | Homo sapiens | ? | - |
? | |
additional information | isozyme AKR1C2 is involved in neurosteroid biosynthesis, while isozyme AKE1C1 eliminates the neurosteroid precursor from the pathway and decreases the neurosteroid concentration in the brain, pathway overview | Homo sapiens | ? | - |
? | |
additional information | isozymes AKR1C1, AKR1C4, and AKR1C2 show broad enzyme specificities, overview | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
3alpha-HSD | - |
Homo sapiens |
AKR1C | - |
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 |
---|---|---|---|---|---|
0.008 | - |
5alpha-dihydroprogesterone | pH 7.0, 25°C, isozyme AKR1C2 | Homo sapiens | |
0.018 | - |
5beta-dihydroprogesterone | pH 7.0, 25°C, isozyme AKR1C2 | Homo sapiens | |
0.04 | - |
5alpha-dihydroprogesterone | pH 7.0, 25°C, isozyme AKR1C1 | Homo sapiens | |
0.05 | - |
5beta-dihydroprogesterone | pH 7.0, 25°C, isozyme AKR1C1 | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition specificity of benzodiazepams for the 3 isozymes AKR1C1, AKR1C2, and AKR1C4 | Homo sapiens | |
0.0003 | - |
diazepam | pH 7.0, 25°C, isozyme AKR1C2 | Homo sapiens | |
0.0008 | - |
estazolam | pH 7.0, 25°C, isozyme AKR1C1 | Homo sapiens | |
0.001 | - |
estazolam | pH 7.0, 25°C, isozyme AKR1C2 | Homo sapiens | |
0.0011 | - |
medazepam | pH 7.0, 25°C, isozyme AKR1C1 | Homo sapiens | |
0.0014 | - |
diazepam | pH 7.0, 25°C, isozyme AKR1C4 | Homo sapiens | |
0.0029 | - |
diazepam | pH 7.0, 25°C, isozyme AKR1C1 | Homo sapiens | |
0.0086 | - |
medazepam | pH 7.0, 25°C, isozyme AKR1C2 | Homo sapiens | |
0.011 | - |
nitrazepam | pH 7.0, 25°C, isozyme AKR1C1 | Homo sapiens | |
0.027 | - |
nitrazepam | pH 7.0, 25°C, isozyme AKR1C2 | Homo sapiens |