Cloned (Comment) | Organism |
---|---|
expression of wild-type and mutant AKR1C17s in Escherichia coli strain BL21(DE3) | Rattus norvegicus |
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 | Comment | Organism | Structure |
---|---|---|---|
Ketamine | inhibition of AKR1C17 | Rattus norvegicus |
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 | 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 Maximum [Da] | Comment | Organism |
---|---|---|---|
36000 | - |
recombinant AKR1C17, gel filtration | Rattus norvegicus |
37000 | - |
1 * 37000, recombinant AKR1C17, SDS-PAGE | Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
female Wistar rats | - |
Purification (Comment) | Organism |
---|---|
recombinant wild-type and mutant AKR1C17s from Escherichia coli strain BL21(DE3) | Rattus norvegicus |
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 | 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 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 | 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 | Comment | Organism |
---|---|---|
monomer | 1 * 37000, recombinant AKR1C17, SDS-PAGE | Rattus norvegicus |
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 Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Rattus norvegicus |
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 Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | 9.5 | recombinant enzyme | Rattus norvegicus |
pH Minimum | pH Maximum | Comment | Organism |
---|---|---|---|
5.5 | 11 | - |
Rattus norvegicus |
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 maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics, overview | Rattus norvegicus |