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Literature summary for 1.1.1.50 extracted from

  • Sanai, M.; Endo, S.; Matsunaga, T.; Ishikura, S.; Tajima, K.; El-Kabbani, O.; Hara, A.
    Rat NAD+-dependent 3alpha-hydroxysteroid dehydrogenase (AKR1C17): a member of the aldo-keto reductase family highly expressed in kidney cytosol (2007), Arch. Biochem. Biophys., 464, 122-129.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant AKR1C17s in Escherichia coli strain BL21(DE3) Rattus norvegicus

Protein Variants

Protein Variants Comment Organism
E276R site-directed mutagenesis, the mutation alters the cofactor specificity of AKR1C17 from NAD+ to NADP+, the switch is analogy th the residues of AKR1C9 and its cofactor specificity, overview Rattus norvegicus
Q270K site-directed mutagenesis, the mutation alters the cofactor specificity of AKR1C17 from NAD+ to NADP+, the switch is analogy th the residues of AKR1C9 and its cofactor specificity, overview Rattus norvegicus
Q270K/E276R site-directed mutagenesis, the mutation alters the cofactor specificity of AKR1C17 from NAD+ to NADP+, the switch is analogy th the residues of AKR1C9 and its cofactor specificity, overview Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
Ketamine inhibition of AKR1C17 Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information cofactor kinetics of wild-type and mutant enzymes, overview Rattus norvegicus
0.0021
-
5beta-androstane-3,17-dione pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.0024
-
5beta-pregnane-3,20-dione pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.0027
-
(5beta,20R)-20-hydroxypregnan-3-one pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.004
-
Dehydrolithocholic acid pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.022
-
isatin pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.023
-
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.038
-
9,10-phenanthrenequinone pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.42
-
diacetyl pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol AKR1C17 and AKR1C9 Rattus norvegicus 5829
-
additional information subcellular localization of isozymes, overview Rattus norvegicus
-
-

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
36000
-
recombinant AKR1C17, gel filtration Rattus norvegicus
37000
-
1 * 37000, recombinant AKR1C17, SDS-PAGE Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
female Wistar rats
-

Purification (Commentary)

Purification (Comment) Organism
recombinant wild-type and mutant AKR1C17s from Escherichia coli strain BL21(DE3) Rattus norvegicus

Reaction

Reaction Comment Organism Reaction ID
a 3alpha-hydroxysteroid + NAD(P)+ = a 3-oxosteroid + NAD(P)H + H+ the enzyme shows a sequential ordered reaction mechanism, where NAD+ binds to the enzyme first and NADH leaves last Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
kidney specific expression of AKR1C17, two enzymes are expressed more highly in renal cortex than in the medulla Rattus norvegicus
-
additional information tissue distribution of isozymes, overview Rattus norvegicus
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.07
-
recombinant AKR1C17 in cell extract, substrate 4-androsten-3alpha-ol-17-one Rattus norvegicus
0.23
-
purified recombinant AKR1C17, substrate 4-androsten-3alpha-ol-17-one Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(5beta,20R)-20-hydroxypregnan-3-one + NADH + H+
-
Rattus norvegicus ?
-
?
4-androsten-3alpha-ol-17-one + NADH + H+ AKR1C17 Rattus norvegicus 4-androsten-3alpha,17beta-diol + NAD+
-
r
4-androstene-3,17-dione + NADH + H+ low activity Rattus norvegicus 4-androsten-3alpha-ol-17-one + NAD+
-
r
5alpha-androstan-3alpha-ol-17-one + NADH + H+
-
Rattus norvegicus 5beta-androstan-3alpha,17beta-diol + NAD+
-
r
5alpha-androstane-3,17-dione + NADH low activity Rattus norvegicus 5alpha-androstan-3alpha-ol-17-one + NAD+ AKR1C9 r
5alpha-dihydrotestosterone + NADH low activity Rattus norvegicus ?
-
?
5alpha-pregnane-20alpha-ol-3-one + NADH
-
Rattus norvegicus 5alpha-pregnane-3,20alpha-diol + NAD+
-
?
5alpha-pregnane-3,20-dione + NADH low activity Rattus norvegicus 5alpha-pregnan-3alpha-ol-20-one + NAD+
-
r
5beta-androstan-3alpha-ol-17-one + NADH
-
Rattus norvegicus 5beta-androstane-3alpha,17beta-diol + NAD+
-
r
5beta-androstane-3,17-dione + NADH
-
Rattus norvegicus 5beta-androstan-3alpha-ol-17-one + NAD+
-
r
5beta-pregnane-20alpha-ol-3-one + NADH + H+
-
Rattus norvegicus 5beta-pregnane-3,20alpha-diol + NAD+
-
?
5beta-pregnane-3,20-dione + NADH + H+
-
Rattus norvegicus 5beta-pregnan-3alpha-ol-20-one + NAD+
-
r
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one + NADH the enzyme produces both R- and S-form products in a ratio of 2.3 : 1 Rattus norvegicus ?
-
?
9,10-phenanthrenequinone + NADH
-
Rattus norvegicus ?
-
?
beta-muricholic acid + NADH low activity Rattus norvegicus ?
-
?
chenodeoxycholic acid + NADH
-
Rattus norvegicus ?
-
?
cholic acid + NADH low activity Rattus norvegicus ?
-
?
dehydrolithocholic acid + NADH + H+
-
Rattus norvegicus ?
-
?
deoxycholic acid + NADH low activity Rattus norvegicus ?
-
?
diacetyl + NADH
-
Rattus norvegicus ?
-
?
glycochenodeoxycholic acid + NADH
-
Rattus norvegicus ?
-
?
glycolithocholic acid + NADH
-
Rattus norvegicus ?
-
?
glycoursodeoxycholic acid + NADH
-
Rattus norvegicus ?
-
?
hyodeoxycholic acid + NADH low activity Rattus norvegicus ?
-
?
isatin + NADH
-
Rattus norvegicus ?
-
?
lithocholic acid + NADH
-
Rattus norvegicus ?
-
?
additional information substrate specificty, overview, recombinant AKR1C17 efficiently oxidizes 3alpha-hydroxysteroids and diverse bile acids using NAD+ as the preferred coenzyme, no activity with progesterone, cortisone, and aldosterone. The enzyme also reduces non-steroidal alpha-dicarbonyl compounds such as 9,10-phenanethrenequinone, isatin, 6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one and diacetyl, but does not show significant activities towards 4-nitrobenzaldehyde and 4-nitroacetophenone Rattus norvegicus ?
-
?
murocholic acid + NADH low activity Rattus norvegicus ?
-
?
taurolithocholic acid + NADH
-
Rattus norvegicus ?
-
?
tauroursodeoxycholic acid + NADH
-
Rattus norvegicus ?
-
?
testosterone + NADH low activity Rattus norvegicus ?
-
?
ursodeoxycholic acid + NADH
-
Rattus norvegicus ?
-
?

Subunits

Subunits Comment Organism
monomer 1 * 37000, recombinant AKR1C17, SDS-PAGE Rattus norvegicus

Synonyms

Synonyms Comment Organism
AKR1C17
-
Rattus norvegicus
AKR1C9
-
Rattus norvegicus
More cf. EC 1.1.1.213, the enzyme belongs to the short-chain dehydrogenase/reductase family Rattus norvegicus
NAD+-dependent 3alpha-HSD
-
Rattus norvegicus
NADP(H)-dependent 3alpha-HSD
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Rattus norvegicus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
additional information
-
additional information cofactor kinetics of wild-type and mutant enzymes, overview Rattus norvegicus
0.022
-
Dehydrolithocholic acid pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.047
-
5beta-androstane-3,17-dione pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.1
-
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.105
-
5beta-pregnane-3,20-dione pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.115
-
(5beta,20R)-20-hydroxypregnan-3-one pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.167
-
diacetyl pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.183
-
9,10-phenanthrenequinone pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus
0.283
-
isatin pH 7.4, 25°C, recombinant wild-type AKR1C17 Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4 9.5 recombinant enzyme Rattus norvegicus

pH Range

pH Minimum pH Maximum Comment Organism
5.5 11
-
Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NAD+ preferred by AKR1C17, dependent on, residues Gln270 and Glu276 are important for cofactor specificity, overview Rattus norvegicus
NADH
-
Rattus norvegicus
NADP+ preferred by AKR1C9, dependent on, residues Gln270 and Glu276 are important for cofactor specificity, overview Rattus norvegicus
NADPH
-
Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics, overview Rattus norvegicus