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Literature summary extracted from

  • Usami, N.; Yamamoto, T.; Shintani, S.; Ishikura, S.; Higaki, Y.; Katagiri, Y.; Hara, A.
    Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines (2002), Biol. Pharm. Bull., 25, 441-445.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.50 bromazepam competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 Homo sapiens
1.1.1.50 cloxazolam potent and specific, competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 Homo sapiens
1.1.1.50 diazepam competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 Homo sapiens
1.1.1.50 estazolam competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 Homo sapiens
1.1.1.50 flunitrazepam competitive inhibition of isozymes AKR1C1 and AKR1C2 Homo sapiens
1.1.1.50 medazepam competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 Homo sapiens
1.1.1.50 additional information no inhibition by oxazolam and oxazepam, benzodiazepams inhibit competitive versus the steroid substrates Homo sapiens
1.1.1.50 nitrazepam competitive inhibition of isozymes AKR1C1, AKR1C4, and AKR1C2 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.50 0.0006
-
 5alpha-dihydroprogesterone pH 7.0, 25°C, isozyme AKR1C2 Homo sapiens
1.1.1.50 0.0007
-
 5beta-dihydroprogesterone pH 7.0, 25°C, isozyme AKR1C2 Homo sapiens
1.1.1.50 0.0011
-
 5alpha-dihydroprogesterone pH 7.0, 25°C, isozyme AKR1C1 Homo sapiens
1.1.1.50 0.0012
-
 5beta-dihydroprogesterone pH 7.0, 25°C, isozyme AKR1C1 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 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

EC Number Organism UniProt Comment Textmining
1.1.1.50 Homo sapiens
-
 isozymes AKR1C1, AKR1C2, and 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+ isozymes AKR1C1 and AKR1C2 are bifunctional enzymes also showing minor 20alpha-hydroxysteroid dehydrogenase activity, EC 1.1.1.149 Homo sapiens
a

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.50 5alpha-dihydroprogesterone + NADPH + H+ isozyme AKR1C2 Homo sapiens 5alpha-hydroxy-pregnan-20-one + NADP+
-
 ?
1.1.1.50 5beta-dihydroprogesterone + NADPH isozyme AKR1C1 and AKR1C2 Homo sapiens ?
-
 ?
1.1.1.50 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 ?
-
 ?
1.1.1.50 additional information isozymes AKR1C1, AKR1C4, and AKR1C2 show broad enzyme specificities, overview Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.50 3alpha-HSD
-
 Homo sapiens
1.1.1.50 AKR1C
-
 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 0.008
-
 5alpha-dihydroprogesterone pH 7.0, 25°C, isozyme AKR1C2 Homo sapiens
1.1.1.50 0.018
-
 5beta-dihydroprogesterone pH 7.0, 25°C, isozyme AKR1C2 Homo sapiens
1.1.1.50 0.04
-
 5alpha-dihydroprogesterone pH 7.0, 25°C, isozyme AKR1C1 Homo sapiens
1.1.1.50 0.05
-
 5beta-dihydroprogesterone pH 7.0, 25°C, isozyme AKR1C1 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.50 7
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.50 NADPH
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.50 additional information
-
 additional information inhibition specificity of benzodiazepams for the 3 isozymes AKR1C1, AKR1C2, and AKR1C4 Homo sapiens
1.1.1.50 0.0003
-
 diazepam pH 7.0, 25°C, isozyme AKR1C2 Homo sapiens
1.1.1.50 0.0008
-
 estazolam pH 7.0, 25°C, isozyme AKR1C1 Homo sapiens
1.1.1.50 0.001
-
 estazolam pH 7.0, 25°C, isozyme AKR1C2 Homo sapiens
1.1.1.50 0.0011
-
 medazepam pH 7.0, 25°C, isozyme AKR1C1 Homo sapiens
1.1.1.50 0.0014
-
 diazepam pH 7.0, 25°C, isozyme AKR1C4 Homo sapiens
1.1.1.50 0.0029
-
 diazepam pH 7.0, 25°C, isozyme AKR1C1 Homo sapiens
1.1.1.50 0.0086
-
 medazepam pH 7.0, 25°C, isozyme AKR1C2 Homo sapiens
1.1.1.50 0.011
-
 nitrazepam pH 7.0, 25°C, isozyme AKR1C1 Homo sapiens
1.1.1.50 0.027
-
 nitrazepam pH 7.0, 25°C, isozyme AKR1C2 Homo sapiens