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(R)-1,2,3,4-tetrahydro-1-naphthol + NAD+
3,4-dihydronaphthalen-1(2H)-one + NADH + H+
i.e. (R)-tetralol
-
-
?
(S)-1,2,3,4-tetrahydro-1-naphthol + NAD+
3,4-dihydronaphthalen-1(2H)-one + NADH + H+
(S)-1,2,3,4-tetrahydro-1-naphthol + NADP+
3,4-dihydronaphthalen-1(2H)-one + NADPH + H+
i.e. (S)-tetralol
-
-
?
(S)-1-indanol + NAD+
2,3-dihydro-1H-inden-1-one + NADH + H+
(S)-alpha-tetralol + NADP+
alpha-tetralone + NADPH + H+
-
-
-
?
(S)-camphorquinone + NADH + H+
? + NAD+
(S)-camphorquinone + NADPH + H+
? + NADP+
-
-
-
?
(S)-tetralol + NADP+
? + NADPH
-
-
-
?
1-acenaphthenol + NAD+
acenaphthylen-1(2H)-one + NADH + H+
-
-
-
?
1-phenyl-1,2-propanedione + NADH + H+
? + NAD+
-
-
-
?
11alpha-hydroxytestosterone + NAD+
11alpha-hydroxyandrost-4-ene-3,17-dione + NADH
-
156% velocity compared to testosterone
-
r
11beta-hydroxytestosterone + NAD+
11beta-hydroxyandrost-4-ene-3,17-dione + NADH
15alpha-hydroxytestosterone + NAD+
15alpha-hydroxyandrost-4-ene-3,17-dione + NADH
-
131% velocity compared to testosterone
-
r
16-oxoestrone + NADH + H+
? + NAD+
-
-
-
?
17beta-estradiol + NAD+
? + NADH + H+
-
-
-
r
17beta-estradiol + NAD+
estrone + NADH + H+
17beta-hydroxy-1alpha-methyl-5alpha-androstan-3-one + NAD+
1alpha-methyl-5alpha-androstane-3,17-dione + NADH
-
192% velocity compared to testosterone
-
r
17beta-hydroxy-5beta-androstan-3-one + NAD+
5beta-androstane-3,17-dione + NADH
-
86% velocity compared to testosterone
-
r
2,3-butanedione + NADH + H+
? + NAD+
-
-
-
?
2-cyclohexen-1-ol + NAD+
2-cyclohexen-1-one + NADH + H+
2-[(2-bromoethyl)(2-[[(2-hydroxyethyl)amino]methyl]-4,6-dinitrophenyl)amino]ethyl methanesulfonate + 2 NADH + 2 H+
2-[(2-bromoethyl)[4-(hydroxyamino)-2-[[(2-hydroxyethyl)amino]methyl]-6-nitrophenyl]amino]ethyl methanesulfonate + 2 NAD+ + H2O
-
i.e. PR-104A, phosphate ester prodrug designed to exploit tumor hypoxia
i.e. PR-104H, enzyme acts as nitroreductase for activation of PR-104A
-
?
20alpha-hydroxyprogesterone + NADH + H+
? + NAD+
-
-
-
?
3alpha-hydroxyprogesterone + NADH + H+
? + NAD+
-
-
-
?
3beta-hydroxy-5alpha-androstane-17-one + NAD+
5alpha-androstane-3,17-dione + NADH
-
75% velocity compared to testosterone
-
r
3beta-hydroxyprogesterone + NADH + H+
? + NAD+
-
-
-
?
4-androstenedione + NADPH + H+
testosterone + NADP+
-
-
-
-
?
4-oxo-2-nonenal + NADPH + H+
4-hydroxy-2-nonenal + NADP+
-
-
-
?
4-pregnen-3alpha-ol-2-one + NAD+
4-pregnen-3,20-dione + NADH + H+
-
-
-
r
4-pregnen-3alpha-ol-20-one + NAD+
4-pregnen-3,20-dione + NADH + H+
-
-
-
?
5alpha-androstan-17beta-ol-3-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
?
5alpha-androstan-3alpha,17beta-diol + NAD+
5alpha-androstan-3alpha-ol-17-one + NADH
-
-
-
?
5alpha-androstan-3alpha-ol-17-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
5alpha-androstan-3beta-ol-17-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
?
5alpha-androstane-17beta-ol-3-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
r
5alpha-androstane-3,17-dione + NADH + H+
? + NAD+
-
-
-
?
5alpha-androstane-3alpha,17beta-diol + NAD+
5alpha-androstane-3alpha-ol-17-one + NADH
5alpha-androstane-3alpha,17beta-diol + NAD+
?
-
-
-
?
5alpha-androstane-3alpha,17beta-diol + NAD+
? + NADH + H+
5alpha-androstane-3beta,17beta-diol + NAD+
5alpha-androstane-3beta-ol-17-one + NADH
5alpha-androstane-3beta,17beta-diol + NAD+
?
-
-
-
?
5alpha-dihydrotestosterone + NAD+
5alpha-androstane-3,17-dione + NADH + H+
5alpha-dihydrotestosterone + NAD+
androstandione + NADH + H+
-
-
-
r
5alpha-dihydrotestosterone + NAD+
androstanedione + NADH + H+
5alpha-pregnan-20alpha-ol-3-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
-
-
-
?
5alpha-pregnan-3,21alpha-diol-20-one + NAD+
5alpha-pregnan-21-ol-3,20-dione + NADH
-
-
-
?
5alpha-pregnan-3alpha-ol-20-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
5alpha-pregnan-3beta-ol-20-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
-
-
-
?
5beta-androstan-17beta-ol-3-one + NAD+
5beta-androstan-3,17-dione + NADH
-
-
-
?
5beta-androstan-17beta-ol-3-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
5beta-androstan-3alpha,17beta-diol + NAD+
5beta-androstan-3alpha-ol-17-one + NADH
-
-
-
?
5beta-androstan-3alpha-ol-17-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
5beta-androstane-17beta-ol-3-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
-
-
-
r
5beta-androstane-3,17-dione + NADH + H+
? + NAD+
-
-
-
?
5beta-androstane-3alpha,17beta-diol + NAD+
5beta-androstane-3alpha-ol-17-one + NADH
-
57% velocity compared to testosterone
-
r
5beta-androstane-3alpha,17beta-diol + NAD+
?
-
-
-
?
5beta-androstane-3alpha,17beta-diol + NAD+
? + NADH + H+
5beta-androstane-3beta,17beta-diol + NAD+
?
-
-
-
?
5beta-dihydrotestosterone + NAD+
androstanedione + NADH + H+
5beta-pregnan-20alpha-ol-3-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
-
-
-
?
5beta-pregnan-3alpha,21-diol-20-one + NAD+
5beta-pregnan-21-ol-3,20-dione + NADH
-
-
-
?
5beta-pregnan-3alpha-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH
-
-
-
?
5beta-pregnan-3alpha-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
5beta-pregnan-3beta,21-diol-20-one + NAD+
?
-
-
-
?
5beta-pregnan-3beta-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
-
-
-
?
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one + NADH + H+
? + NAD+
-
-
-
?
6beta-hydroxytestosterone + NAD+
6beta-hydroxyandrost-4-ene-3,17-dione + NADH
-
84% velocity compared to testosterone
-
r
9,10-phenanthrenequinone + NADH + H+
? + NAD+
-
-
-
?
alpha-3-hydroxyhexobarbital + NAD+
?
-
-
-
?
alpha-tetralone + NADH + H+
? + NAD+
-
-
-
?
androst-4-ene-3beta,17beta-diol + NAD+
androst-4-ene-3beta-ol-17-one + NADH
-
75% velocity compared to testosterone
-
r
androst-4-ene-3beta,17beta-diol + NAD+
androst-4-ene-3beta-ol-17-one + NADH + H+
-
-
-
-
?
androst-5-ene-3beta,17beta-diol + NAD+
androst-5-ene-3beta-ol-17-one + NADH
-
33% velocity compared to testosterone
-
r
androstandiol + NAD+
androsterone + NADH
-
-
-
r
androstanediol + NAD+
androsterone + NADH
-
-
-
r
benzene dihydrodiol + NAD+
?
-
-
-
?
benzene dihydrodiol + NAD+
? + NADH + H+
-
-
-
?
beta-3-hydroxyhexobarbital + NAD+
?
-
-
-
?
beta-ionol + NAD+
(3E)-4-(2,6,6-trimethylcyclohex-1-en-1-yl)but-3-en-2-one + NADH + H+
cis-benzene dihydrodiol + NAD+
?
-
-
-
?
daunorubicin + NADPH + H+
daunorubicinol + NADP+
dehydroepiandrosterone + NAD+
? + NADH + H+
-
-
-
?
estradiol + NAD+
estrone + NADH
estrone + NADPH + H+
17beta-estradiol + NADP+
-
-
-
-
?
farnesol + NAD+
?
-
-
-
?
farnesol + NAD+
? + NADH + H+
-
-
-
?
farnesol + NAD+
farnesal + NADH + H+
-
-
-
?
geraniol + NAD+
?
-
-
-
?
geraniol + NAD+
? + NADH + H+
-
-
-
?
geraniol + NAD+
geranial + NADH + H+
-
-
-
?
geranylgeraniol + NAD+
?
-
-
-
?
geranylgeraniol + NAD+
? + NADH + H+
-
-
-
?
geranylgeraniol + NAD+
geranylgeranial + NADH + H+
-
-
-
?
glycochenodeoxycholic acid + NAD+
7alpha-hydroxy-3-oxo-5-beta-cholanoyl glycine + NADH
-
-
-
?
glycolithocholic acid + NAD+
3-oxo-5beta-cholanoyl glycine + NADH
-
-
-
?
isatin + NADH + H+
? + NAD+
-
-
-
?
lithocholic acid
5beta-cholan-3-one-24-oic acid + NADH + H+
-
-
-
?
lithocholic acid + NAD+
5-beta-cholan-3-one-24-oic acid + NADH + H+
-
-
-
?
lithocholic acid + NAD+
5beta-cholan-3-one-24-oic acid + NADH
-
-
-
?
lithocholic acid + NAD+
5beta-cholan-3-one-24-oic acid + NADH + H+
-
-
-
?
morphine + NAD+
morphinone + NADH + H+
reaction of EC 1.1.1.218
-
-
?
naphthalene dihydrodiol + NAD+
? + NADH + H+
-
-
-
?
nerol + NAD+
neral + NADH + H+
-
-
-
?
progesterone + NADPH + H+
20alpha-hydroxyprogesterone + NADP+
-
-
-
-
?
prostaglandin D2 + NADPH + H+
9alpha,11beta-prostaglandin F2 + NADP+
-
-
-
-
?
pyridine-3-aldehyde + NADH + H+
? + NAD+
-
-
-
?
testosterone + NAD+
4-androstenedione + NADH + H+
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
testosterone + NAD+
androstenedione + NADH + H+
testosterone + NADP+
androst-4-ene-3,17-dione + NADPH + H+
-
NADP is 3fold less efficient as cofactor
-
r
testosterone + NADP+
androstenedione + NADPH + H+
-
-
-
r
trans-benzene dihydrodiol + NAD+
?
-
-
-
?
additional information
?
-
(S)-1,2,3,4-tetrahydro-1-naphthol + NAD+
3,4-dihydronaphthalen-1(2H)-one + NADH + H+
i.e. (S)-tetralol
-
-
r
(S)-1,2,3,4-tetrahydro-1-naphthol + NAD+
3,4-dihydronaphthalen-1(2H)-one + NADH + H+
i.e. (S)-tetralol
-
-
?
(S)-1,2,3,4-tetrahydro-1-naphthol + NAD+
3,4-dihydronaphthalen-1(2H)-one + NADH + H+
i.e. (S)-tetralol
-
-
?
(S)-1-indanol + NAD+
2,3-dihydro-1H-inden-1-one + NADH + H+
-
-
-
?
(S)-1-indanol + NAD+
2,3-dihydro-1H-inden-1-one + NADH + H+
-
-
-
?
(S)-camphorquinone + NADH + H+
? + NAD+
-
-
-
?
(S)-camphorquinone + NADH + H+
? + NAD+
-
-
-
?
11beta-hydroxytestosterone + NAD+
11beta-hydroxyandrost-4-ene-3,17-dione + NADH
-
136% velocity compared to testosterone
-
r
11beta-hydroxytestosterone + NAD+
11beta-hydroxyandrost-4-ene-3,17-dione + NADH
-
-
-
r
11beta-hydroxytestosterone + NAD+
11beta-hydroxyandrost-4-ene-3,17-dione + NADH
-
76% of testosterone oxidation rate
-
r
17beta-estradiol + NAD+
estrone + NADH + H+
-
-
-
?
17beta-estradiol + NAD+
estrone + NADH + H+
-
-
-
?
2-cyclohexen-1-ol + NAD+
2-cyclohexen-1-one + NADH + H+
-
-
-
?
2-cyclohexen-1-ol + NAD+
2-cyclohexen-1-one + NADH + H+
-
-
-
?
5alpha-androstan-3alpha-ol-17-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
?
5alpha-androstan-3alpha-ol-17-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
?
5alpha-androstan-3alpha-ol-17-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
r
5alpha-androstane-3alpha,17beta-diol + NAD+
5alpha-androstane-3alpha-ol-17-one + NADH
-
72% velocity compared to testosterone
-
r
5alpha-androstane-3alpha,17beta-diol + NAD+
5alpha-androstane-3alpha-ol-17-one + NADH
-
204% velocity compared to testosterone
-
r
5alpha-androstane-3alpha,17beta-diol + NAD+
? + NADH + H+
-
-
-
?
5alpha-androstane-3alpha,17beta-diol + NAD+
? + NADH + H+
-
-
-
r
5alpha-androstane-3beta,17beta-diol + NAD+
5alpha-androstane-3beta-ol-17-one + NADH
-
72% velocity compared to testosterone
-
r
5alpha-androstane-3beta,17beta-diol + NAD+
5alpha-androstane-3beta-ol-17-one + NADH
-
17% velocity compared to testosterone
-
r
5alpha-dihydrotestosterone + NAD+
5alpha-androstane-3,17-dione + NADH + H+
-
133% velocity compared to testosterone
-
r
5alpha-dihydrotestosterone + NAD+
5alpha-androstane-3,17-dione + NADH + H+
-
-
-
?
5alpha-dihydrotestosterone + NAD+
androstanedione + NADH + H+
-
-
-
r
5alpha-dihydrotestosterone + NAD+
androstanedione + NADH + H+
-
119% initial velocity compared to testosterone
-
r
5alpha-pregnan-3alpha-ol-20-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
-
-
-
?
5alpha-pregnan-3alpha-ol-20-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
-
-
-
?
5alpha-pregnan-3alpha-ol-20-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
-
-
-
r
5beta-androstan-17beta-ol-3-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
-
-
-
?
5beta-androstan-17beta-ol-3-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
-
-
-
?
5beta-androstan-3alpha-ol-17-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
-
-
-
?
5beta-androstan-3alpha-ol-17-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
-
-
-
?
5beta-androstan-3alpha-ol-17-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
-
-
-
r
5beta-androstane-3alpha,17beta-diol + NAD+
? + NADH + H+
-
-
-
?
5beta-androstane-3alpha,17beta-diol + NAD+
? + NADH + H+
-
-
-
r
5beta-dihydrotestosterone + NAD+
androstanedione + NADH + H+
-
-
-
?
5beta-dihydrotestosterone + NAD+
androstanedione + NADH + H+
-
50% initial velocity compared to testosterone
-
r
5beta-pregnan-3alpha-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
-
-
-
?
5beta-pregnan-3alpha-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
-
-
-
?
5beta-pregnan-3alpha-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
-
-
-
r
beta-ionol + NAD+
(3E)-4-(2,6,6-trimethylcyclohex-1-en-1-yl)but-3-en-2-one + NADH + H+
-
-
-
?
beta-ionol + NAD+
(3E)-4-(2,6,6-trimethylcyclohex-1-en-1-yl)but-3-en-2-one + NADH + H+
-
-
-
?
daunorubicin + NADPH + H+
daunorubicinol + NADP+
inactivation of the anticancer drug
-
-
r
daunorubicin + NADPH + H+
daunorubicinol + NADP+
the enzyme reduces daunorubicin to its corresponding alcohol daunorubicinol using NADPH as the coenzyme
-
-
r
estradiol + NAD+
estrone + NADH
-
72% velocity compared to testosterone oxidation
-
r
estradiol + NAD+
estrone + NADH
-
-
-
r
estradiol + NAD+
estrone + NADH
-
46% of testosterone oxidation rate
-
r
estradiol + NAD+
estrone + NADH
-
15% velocity compared to testosterone oxidation
-
r
testosterone + NAD+
4-androstenedione + NADH + H+
-
-
-
?
testosterone + NAD+
4-androstenedione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
r
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androstenedione + NADH + H+
-
-
-
r
testosterone + NAD+
androstenedione + NADH + H+
the enzyme shows LNCaP-AKR1C3 mediates formation of testosterone, conversion of 4-androstene-3,17-dione to testosterone
-
-
r
testosterone + NAD+
androstenedione + NADH + H+
-
-
-
r
additional information
?
-
the enzyme AKR1C34 shows 3alpha/17beta/20alpha-hydroxysteroid dehydrogenase activities, substrate specificity, detailed overview. Ala54 plays a critical role in non-/recognition of the steroidal substrates. Reaction products identification by thin-layer chromatography (TLC) and liquid chromatography/mass spectrometry (LC/MS). AKR1C34 also has morphine dehydrogenase activity, EC 1.1.1.218. No activity with cyclohexanol
-
-
?
additional information
?
-
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. AKR1C28 exhibits low dehydrogenase activity for 20alpha-hydroxysteroids, but does not oxidize 3beta-hydroxysteroids (5alpha/beta-androstan-3beta-ol-17-ones and 5alpha/beta-pregnan-3beta-ol-20-ones), 17alpha-hydroxysteroids (4-androsten-17alpha-ol-3-one and 17alpha-estradiol) and 20beta-hydroxysteroids (4-pregnene-17alpha/20beta-diol-3-one and 5alpha-pregnan-20beta-ol-3-one). In the NADH-linked reverse reaction, AKR1C28 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. AKR1C28 shows higher kcat/Km values for 17beta-hydroxy-C19-steroids than those for 3alpha-hydroxysteroids, and most efficiently oxidized 17beta-estradiol. Substrate specificity, overview
-
-
?
additional information
?
-
J7M9D0
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. AKR1C28 exhibits low dehydrogenase activity for 20alpha-hydroxysteroids, but does not oxidize 3beta-hydroxysteroids (5alpha/beta-androstan-3beta-ol-17-ones and 5alpha/beta-pregnan-3beta-ol-20-ones), 17alpha-hydroxysteroids (4-androsten-17alpha-ol-3-one and 17alpha-estradiol) and 20beta-hydroxysteroids (4-pregnene-17alpha/20beta-diol-3-one and 5alpha-pregnan-20beta-ol-3-one). In the NADH-linked reverse reaction, AKR1C28 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. AKR1C28 shows higher kcat/Km values for 17beta-hydroxy-C19-steroids than those for 3alpha-hydroxysteroids, and most efficiently oxidized 17beta-estradiol. Substrate specificity, overview
-
-
?
additional information
?
-
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. AKR1C28 exhibits low dehydrogenase activity for 20alpha-hydroxysteroids, but does not oxidize 3beta-hydroxysteroids (5alpha/beta-androstan-3beta-ol-17-ones and 5alpha/beta-pregnan-3beta-ol-20-ones), 17alpha-hydroxysteroids (4-androsten-17alpha-ol-3-one and 17alpha-estradiol) and 20beta-hydroxysteroids (4-pregnene-17alpha/20beta-diol-3-one and 5alpha-pregnan-20beta-ol-3-one). In the NADH-linked reverse reaction, AKR1C28 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. AKR1C28 shows higher kcat/Km values for 17beta-hydroxy-C19-steroids than those for 3alpha-hydroxysteroids, and most efficiently oxidized 17beta-estradiol. Substrate specificity, overview
-
-
?
additional information
?
-
-
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. AKR1C28 exhibits low dehydrogenase activity for 20alpha-hydroxysteroids, but does not oxidize 3beta-hydroxysteroids (5alpha/beta-androstan-3beta-ol-17-ones and 5alpha/beta-pregnan-3beta-ol-20-ones), 17alpha-hydroxysteroids (4-androsten-17alpha-ol-3-one and 17alpha-estradiol) and 20beta-hydroxysteroids (4-pregnene-17alpha/20beta-diol-3-one and 5alpha-pregnan-20beta-ol-3-one). In the NADH-linked reverse reaction, AKR1C28 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. AKR1C28 shows higher kcat/Km values for 17beta-hydroxy-C19-steroids than those for 3alpha-hydroxysteroids, and most efficiently oxidized 17beta-estradiol. Substrate specificity, overview
-
-
?
additional information
?
-
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. In the NADH-linked reverse reaction, AKR1C27 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. Substrate specificity, detailed overview
-
-
?
additional information
?
-
J7M9D0
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. In the NADH-linked reverse reaction, AKR1C27 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. Substrate specificity, detailed overview
-
-
?
additional information
?
-
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. In the NADH-linked reverse reaction, AKR1C27 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. Substrate specificity, detailed overview
-
-
?
additional information
?
-
-
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. In the NADH-linked reverse reaction, AKR1C27 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. Substrate specificity, detailed overview
-
-
?
additional information
?
-
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, and 5alpha-pregnan-20alpha-ol-3-one
-
-
?
additional information
?
-
J7M9D0
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, and 5alpha-pregnan-20alpha-ol-3-one
-
-
?
additional information
?
-
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, and 5alpha-pregnan-20alpha-ol-3-one
-
-
?
additional information
?
-
-
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, and 5alpha-pregnan-20alpha-ol-3-one
-
-
?
additional information
?
-
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, beta-ionol, geraniogeraniol, farnesol, 5alpha-androstane-3alpha,17beta-diol, 5alpha-pregnan-20alpha-ol-3-one, and 4-pregnen-20alpha-3-one
-
-
?
additional information
?
-
J7M9D0
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, beta-ionol, geraniogeraniol, farnesol, 5alpha-androstane-3alpha,17beta-diol, 5alpha-pregnan-20alpha-ol-3-one, and 4-pregnen-20alpha-3-one
-
-
?
additional information
?
-
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, beta-ionol, geraniogeraniol, farnesol, 5alpha-androstane-3alpha,17beta-diol, 5alpha-pregnan-20alpha-ol-3-one, and 4-pregnen-20alpha-3-one
-
-
?
additional information
?
-
-
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, beta-ionol, geraniogeraniol, farnesol, 5alpha-androstane-3alpha,17beta-diol, 5alpha-pregnan-20alpha-ol-3-one, and 4-pregnen-20alpha-3-one
-
-
?
additional information
?
-
the enzyme shows NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids
-
-
?
additional information
?
-
J7M9D0
the enzyme shows NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids
-
-
?
additional information
?
-
the enzyme shows NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids
-
-
?
additional information
?
-
-
the enzyme shows NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids
-
-
?
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(2E)-3-(3,3-dimethyl-3,4-dihydro-2H-1-benzopyran-6-yl)prop-2-enoate
-
(2E)-3-(4-bromophenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
93.3% inhibition at 0.1 mM
(2E)-3-(4-ethylphenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
89.1% inhibition at 0.1 mM
(2E)-3-(4-methylphenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
92.7% inhibition at 0.1 mM
(2E)-3-prop-2-enoic acid
-
(2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoate
-
(2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoic acid
i.e. baccharin, a component of Brazilian propolis, exhibits a high inhibitory potency and selectivity for AKR1C3 over other AKR1C isoforms. When the cinnamic acid group of baccharin is esterified, there is a dramatic decrease in potency and selectivity for AKR1C3 in comparison to baccharin. Low or submicromolar inhibition is observed when the 3-prenyl group of baccharin is removed, and the selectivity over AKR1C2 is low. Inhibition of NAD+ dependent oxidation of S-tetralol
(2E)-3-[4-(acetyloxy)-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoate
-
(2E)-3-[4-(acetyloxy)-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoic acid
-
(2E)-3-[4-(benzoyloxy)phenyl]prop-2-enoic acid
-
(2E)-3-[4-(methylsulfanyl)phenyl]-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
93.5% inhibition at 0.1 mM
(2E)-3-[4-(pyridine-4-carbonyloxy)phenyl]prop-2-enoic acid
-
(2E)-3-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoate
37% inhibition at 0.010 mM
(4-chlorophenyl)(5-methoxy-2-methyl-1H-indol-1-yl)methanone
-
(E)-3-(3-((3-phenylpropanoyl)oxy)phenyl)acrylic acid
-
(Z/E)-3-(4-((3-phenylpropanoyl)oxy)phenyl)acrylic acid
-
(Z/E)-tert-butyl 3-(4-(3-phenylpropanoyloxy)phenyl)acrylate
-
1-(4-[[(2R)-2-methylpiperidin-1-yl]sulfonyl]phenyl)-1,3-dihydro-2H-pyrrol-2-one
IC50 value in HCT-116 cells engineered to over-express AKR1C3 is 11 nM
1-(4-[[(2R,6S)-2,6-dimethylpiperidin-1-yl]sulfonyl]phenyl)pyrrolidin-2-one
IC50 value in HCT-116 cells engineered to over-express AKR1C3 is 22 nM
1-[4-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)phenyl]pyrrolidin-2-one
IC50 value in HCT-116 cells engineered to over-express AKR1C3 is 24 nM
17alpha-methyltestosterone
-
competitive inhibition
17beta-estradiol
-
0.175 mM, 25-40% inhibition of testosterone oxidation
2'-des-methyl-indomethacin
the cofactor binding cavity of AKR1C3 is not perturbed upon binding of the inhibitor
-
2-(2,4-dioxo-1,3-thiazolidin-5-yl)-N-(2-hydroxyphenyl)acetamide
inhibitor is about 1000times more selective for isoform AKR1C3 over AKR1C2, and selectivity is even higher when compared with AKR1C1 and AKR1C4
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(2-methylbenzene-1-sulfonyl)acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-cyanobenzene-1-sulfonyl)acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-fluorobenzene-1-sulfonyl)acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methoxybenzene-1-sulfonyl)acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methylbenzene-1-sulfonyl)acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-phenoxybenzene-1-sulfonyl)acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(5-chlorothiophene-2-sulfonyl)acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(methanesulfonyl)acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(naphthalene-2-sulfonyl)acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[3-(trifluoromethyl)benzene-1-sulfonyl]acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]acetamide
-
2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide
-
2-[[(3-hydroxyphenyl)carbonyl]amino]-4,5-dimethoxybenzoic acid
-
2-[[(3-hydroxyphenyl)carbonyl]amino]-5-nitrobenzoic acid
-
21-hydroxypregn-4-ene-3,20-dione
-
0.010 mM, 73% inhibition
3-((4-nitronaphthalen-1-yl)amino)benzoic acid
inhibitor nanomolar potency and selective inhibition of isoform AKR1C3 but also acts as an androgen receptor antagonist. It inhibits 5alpha-dihydrotestosterone stimulated androgen receptor reporter gene activity with an IC50 value of 4.7 microM and produces a concentration dependent reduction in androgen receptor levels in prostate cancer cells
3-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)benzoate
-
3-(5-methoxy-2-methyl-1H-indol-3-yl)propanoic acid
-
3-(phenylamino)benzoic acid
-
3-phenoxybenzoic acid
inhibitor carboxylic acid binds to the oxyanion site, in which the carboxylate group very closely overlays the acetate molecule found in other AKR1C3 structures and forms hydrogen bonds to the enzyme catalytic residues His117 and Tyr55, as well as to a conserved water network located in and near the SP3 subpocket. The 3-phenoxy ring extends into the SP1 subpocket and makes van der Waals contacts with the aromatic residues Phe306, Phe311 and Tyr319 that line the pocket
3-[(4-nitrophenyl)amino]benzoic acid
94fold selectivity for the inhibition of isoform AKR1C3 over AKR1C2
3-[1-(4-chlorobenzoyl)-2-ethyl-5-methoxy-1H-indol-3-yl]propanoic acid
-
3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid
-
3-[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]propanoic acid
-
3-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]propanoic acid
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2-methylpropanoic acid
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(2-methylbenzene-1-sulfonyl)propanamide
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(4-methylbenzene-1-sulfonyl)propanamide
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(5-chlorothiophene-2-sulfonyl)propanamide
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)-2-methylpropanamide
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)propanamide
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(naphthalene-2-sulfonyl)propanamide
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(trifluoromethanesulfonyl)propanamide
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]propanamide
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethoxy)benzene-1-sulfonyl]propanamide
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]propanamide
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanoic acid
-
3-[[4-(methoxymethyl)phenyl]amino]benzoic acid
360fold selectivity for the inhibition of isoform AKR1C3 over AKR1C2
3-[[4-(trifluoromethyl)phenyl]amino]benzoic acid
3a-phenyl-2,3,3a,4-tetrahydro-1H-pyrrolo[1,2-a]benzimidazol-1-one
inhibitor shows 17fold and 30fold selectivity against isoforms AKR1C2 and AKR1C1, respectively, and much higher selectivity against AKR1C4
3beta-cyclohexylethyl-androsterone
-
potent inhibitor
3beta-n-hexyl-androsterone
-
potent inhibitor
3beta-phenylethyl-androsterone
-
potent inhibitor
4-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]butanoic acid
-
5-bromo-2-[[(3-hydroxyphenyl)carbonyl]amino]benzoic acid
-
5-chloro-2-[[(3-hydroxyphenyl)carbonyl]amino]benzoic acid
-
5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylic acid
-
5alpha-Androstan-3beta-ol-17-one
-
0.005 mM, 55% inhibition
5alpha-pregnan-3beta-ol-20-one
-
0.005 mM, 52% inhibition
5beta-androstan-3,17-dione
-
product inhibition, forward reaction
5beta-androstan-3beta-ol-17-one
-
0.005 mM, 87% inhibition
5beta-dihydrotestosterone
-
product inhibition, reverse reaction
5beta-Pregnan-3beta-ol-20-one
-
0.005 mM, 81% inhibition
6-methoxy-9-[3-(trifluoromethyl)benzoyl]-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid
-
7-hydroxyflavone
-
0.007 mM, 50% inhibition, oxidation of androstandiol
9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-2-carboxylic acid
-
9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid
-
9-(4-chlorobenzoyl)-N-(methanesulfonyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxamide
-
abietic acid
-
0.010 mM, 50% inhibition, oxidation of androstandiol
Ag+
-
0.1 mM, complete inhibition
biochain A
-
0.014 mM, 50% inhibition, reduction of androst-4-ene-3,17-dione, 0.008 mM, oxidation of androstanediol
chrysin
-
0.010 mM, 50% inhibition, oxidation of androstandiol
coumestrol
-
0.005 mM, 50% inhibition, reduction of androst-4-ene-3,17-dione, 0.011 mM, 50% inhibition, oxidation of androstanediol
CuCl2
-
1 mM, complete inhibition
dexamethasone
-
0.10 mM, 39% inhibition
Dienstrol
-
0.010 mM, 60% inhibition
FeCl3
-
10 mM, 46% inhibition
Hg2+
-
0.1 mM, complete inhibition
ikarisoside A
competitive; competitive
Medroxyprogesterone acetate
-
0.010 mM, 22% inhibition
methyl 5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylate
-
methyl [1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetate
-
methyl [1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetate
-
methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate
-
methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate
-
N-(4-acetylbenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
-
N-(4-acetylbenzene-1-sulfonyl)-3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanamide
-
N-(4-bromobenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
-
N-(4-chlorobenzoyl)-melatonin
-
N-benzoylanthranilic acid
-
N-[2,5-bis(trifluoromethyl)benzene-1-sulfonyl]-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
-
NaCN
-
1 mM, 50% inhibition
naringenin
-
0.010 mM, 50% inhibition, oxidation of androstandiol
p-chloromercuribenzoate
-
0.1 mM, complete inhibition
Sodium amytal
-
10 mM, 25% inhibition
stilboestrol
-
0.010 mM, 61% inhibition
tert-butyl(2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoate
-
Triton X-100
-
immediate loss of 60-70% activity, remaining activity is stable for 4 days, competitive vs. testosterone, non-competitive vs. NAD+
ZnCl2
-
10 mM, 10% inhibition
[1-(4-chlorobenzoyl)-5-fluoro-1H-indol-3-yl]acetic acid
-
[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]acetic acid
-
[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid
-
[1-(4-chlorobenzoyl)-5-methoxy-2-propyl-1H-indol-3-yl]acetic acid
-
[1-(4-fluorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid
-
[1-(4-fluorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid
-
[1-[4-(chloromethyl)benzoyl]-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid
-
[5-fluoro-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
-
[5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetic acid
-
[5-methoxy-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
-
[5-methoxy-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
-
[5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetic acid
-
[5-methoxy-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
-
[5-methoxy-2-methyl-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
-
3-[[4-(trifluoromethyl)phenyl]amino]benzoic acid
250fold selectivity for the inhibition of isoform AKR1C3 over AKR1C2
3-[[4-(trifluoromethyl)phenyl]amino]benzoic acid
in complex with AKR1C3. Compound adopts a similar binding orientation as flufenamic acid, however, its phenylamino ring projects deeper into a subpocket and confers selectivity over the other AKR1C isoforms
Hexestrol
-
Hexestrol
competitive; competitive
Hexoestrol
-
0.010 mM, 62% inhibition
hinokitiol
-
hinokitiol
competitive; competitive
indomethacin
-
indomethacin
-
0.10 mM, 67% inhibition
kaempferol
-
0.008 mM, 50% inhibition, oxidation of androstandiol
Phenolphthalein
-
quercetin
-
0.009 mM, 50% inhibition, reduction of androst-4-ene-3,17-dione, 0.005 mM, oxidation of androstanediol
zearalenone
-
0.004 mM, 50% inhibition, reduction of androst-4-ene-3,17-dione, 0.002 mM, oxidation of androstanediol
zearalenone
competitive; competitive
additional information
development of potent and selective indomethacin analogues for the inhibition of AKR1C3 in castrate-resistant prostate cancer, overview. Increasing the length of the aliphatic side chain of indomethacin from -ethyl to -propyl leads to a 2fold reduction in AKR1C3 potency, but the compound retained 257fold selectivity for AKR1C3 over AKR1C2
-
additional information
screening of baccharin analogues as selective inhibitors against type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3), selectivity versus AKR1C2
-
additional information
no or poor inhibition by 7-hydroxyflavone, chrysin, quercetin, genistein, galangin, lithocholic acid, and zearalenone
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.095
(R)-1,2,3,4-tetrahydro-1-naphthol
pH 7.4, 25°C, recombinant enzyme
0.004 - 0.25
(S)-1,2,3,4-tetrahydro-1-naphthol
0.014 - 0.181
(S)-1-indanol
0.0019 - 0.0067
(S)-camphorquinone
0.148
1-Acenaphthenol
pH 7.4, 25°C, recombinant enzyme
0.0008 - 0.005
1-phenyl-1,2-propanedione
0.0021 - 0.01
16-oxoestrone
0.0021 - 0.1
17beta-estradiol
0.19 - 0.371
2,3-Butanedione
0.035 - 0.67
2-Cyclohexen-1-ol
0.0031
4-oxo-2-nonenal
pH 7.4, 25°C
0.0057 - 0.081
4-pregnen-3alpha-ol-20-one
0.00067 - 0.13
5alpha-androstan-17beta-ol-3-one
0.0031
5alpha-androstan-3alpha,17beta-diol
-
-
0.0022 - 0.0092
5alpha-Androstan-3alpha-ol-17-one
0.0005 - 0.0078
5alpha-androstane-3alpha,17beta-diol
0.00067 - 0.0035
5alpha-pregnan-3alpha-ol-20-one
0.00067 - 0.03
5beta-androstan-17beta-ol-3-one
0.0066
5beta-androstan-3,17-dione
-
-
0.0048
5beta-Androstan-3alpha,17beta-diol
-
-
0.0015 - 0.0023
5beta-Androstan-3alpha-ol-17-one
0.0022 - 0.02
5beta-androstane-3alpha,17beta-diol
0.0038
5beta-pregnan-3,20-dione
-
-
0.0062
5beta-pregnan-3alpha,17beta-diol-20-one
-
-
0.0036 - 0.17
5beta-Pregnan-3alpha-ol-20-one
0.0021 - 0.101
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one
0.0001 - 0.0002
9,10-phenanthrenequinone
0.03
alpha-3-hydroxyhexobarbital
pH 7.4, 25°C, recombinant enzyme
0.0038 - 0.15
alpha-tetralone
0.0016
androst-4-ene-3,17-dione
-
-
0.024
androstendione
-
reduction of androstendione, pH 7.0
0.027 - 1.11
benzene dihydrodiol
0.013
beta-3-hydroxyhexobarbital
pH 7.4, 25°C, recombinant enzyme
0.0006 - 0.0097
beta-ionol
0.63
cis-benzene dihydrodiol
pH 7.4, 25°C, recombinant enzyme
0.009
estrone
-
pH 7.0, 37°C
0.0007 - 0.0012
geranylgeraniol
0.0075
glycochenodeoxycholic acid
-
-
0.003
glycolithocholic acid
-
-
0.0005 - 0.14
lithocholic acid
0.52
morphine
pH 7.4, 25°C
1.38
NADP+
pH 7.4, 25°C, with substrate S-camphorquinone
0.027
Naphthalene dihydrodiol
pH 7.4, 25°C
0.162
nerol
pH 7.4, 25°C, recombinant enzyme
0.29 - 1.1
Pyridine-3-aldehyde
0.0016 - 0.25
testosterone
1
trans-benzene dihydrodiol
pH 7.4, 25°C, recombinant enzyme
additional information
additional information
-
0.004
(S)-1,2,3,4-tetrahydro-1-naphthol
pH 7.4, 25°C
0.022
(S)-1,2,3,4-tetrahydro-1-naphthol
pH 7.4, 25°C
0.061
(S)-1,2,3,4-tetrahydro-1-naphthol
pH 7.4, 25°C, recombinant enzyme
0.25
(S)-1,2,3,4-tetrahydro-1-naphthol
pH 7.4, 25°C
0.014
(S)-1-indanol
pH 7.4, 25°C
0.042
(S)-1-indanol
pH 7.4, 25°C
0.11
(S)-1-indanol
pH 7.4, 25°C
0.181
(S)-1-indanol
pH 7.4, 25°C, recombinant enzyme
0.0019
(S)-camphorquinone
pH 7.4, 25°C
0.0029
(S)-camphorquinone
pH 7.4, 25°C
0.0067
(S)-camphorquinone
pH 7.4, 25°C
0.0008
1-phenyl-1,2-propanedione
pH 7.4, 25°C
0.003
1-phenyl-1,2-propanedione
pH 7.4, 25°C
0.005
1-phenyl-1,2-propanedione
pH 7.4, 25°C
0.0021
16-oxoestrone
pH 7.4, 25°C
0.003
16-oxoestrone
pH 7.4, 25°C
0.01
16-oxoestrone
pH 7.4, 25°C
0.0021
17beta-estradiol
pH 7.4, 25°C
0.0064
17beta-estradiol
-
-
0.0139
17beta-estradiol
-
cofactor S-NAD+
0.021
17beta-estradiol
-
-
0.1
17beta-estradiol
pH 7.4, 25°C
0.19
2,3-Butanedione
pH 7.4, 25°C
0.21
2,3-Butanedione
pH 7.4, 25°C
0.371
2,3-Butanedione
pH 7.4, 25°C
0.035
2-Cyclohexen-1-ol
pH 7.4, 25°C
0.066
2-Cyclohexen-1-ol
pH 7.4, 25°C
0.569
2-Cyclohexen-1-ol
pH 7.4, 25°C, recombinant enzyme
0.67
2-Cyclohexen-1-ol
pH 7.4, 25°C
0.0057
4-pregnen-3alpha-ol-20-one
pH 7.4, 25°C
0.0073
4-pregnen-3alpha-ol-20-one
pH 7.4, 25°C
0.081
4-pregnen-3alpha-ol-20-one
pH 7.4, 25°C
0.00067
5alpha-androstan-17beta-ol-3-one
pH 7.4, 25°C
0.0078
5alpha-androstan-17beta-ol-3-one
pH 7.4, 25°C
0.13
5alpha-androstan-17beta-ol-3-one
pH 7.4, 25°C
0.0022
5alpha-Androstan-3alpha-ol-17-one
pH 7.4, 25°C
0.0092
5alpha-Androstan-3alpha-ol-17-one
pH 7.4, 25°C
0.0005
5alpha-androstane-3alpha,17beta-diol
pH 7.4, 25°C
0.0078
5alpha-androstane-3alpha,17beta-diol
pH 7.4, 25°C
0.00067
5alpha-pregnan-3alpha-ol-20-one
pH 7.4, 25°C
0.0035
5alpha-pregnan-3alpha-ol-20-one
pH 7.4, 25°C
0.00067
5beta-androstan-17beta-ol-3-one
pH 7.4, 25°C
0.0049
5beta-androstan-17beta-ol-3-one
-
-
0.0076
5beta-androstan-17beta-ol-3-one
pH 7.4, 25°C
0.03
5beta-androstan-17beta-ol-3-one
pH 7.4, 25°C
0.0015
5beta-Androstan-3alpha-ol-17-one
pH 7.4, 25°C
0.0023
5beta-Androstan-3alpha-ol-17-one
pH 7.4, 25°C
0.0022
5beta-androstane-3alpha,17beta-diol
pH 7.4, 25°C
0.02
5beta-androstane-3alpha,17beta-diol
pH 7.4, 25°C
0.0036
5beta-Pregnan-3alpha-ol-20-one
pH 7.4, 25°C
0.0037
5beta-Pregnan-3alpha-ol-20-one
pH 7.4, 25°C
0.0046
5beta-Pregnan-3alpha-ol-20-one
-
-
0.17
5beta-Pregnan-3alpha-ol-20-one
pH 7.4, 25°C
0.0021
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one
pH 7.4, 25°C
0.0042
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one
pH 7.4, 25°C
0.101
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one
pH 7.4, 25°C
0.0001
9,10-phenanthrenequinone
pH 7.4, 25°C
0.0002
9,10-phenanthrenequinone
pH 7.4, 25°C
0.0038
alpha-tetralone
pH 7.4, 25°C
0.06
alpha-tetralone
pH 7.4, 25°C
0.15
alpha-tetralone
pH 7.4, 25°C
0.027
benzene dihydrodiol
pH 7.4, 25°C
0.12
benzene dihydrodiol
pH 7.4, 25°C
1.11
benzene dihydrodiol
pH 7.4, 25°C
0.0006
beta-ionol
pH 7.4, 25°C
0.009
beta-ionol
pH 7.4, 25°C
0.0097
beta-ionol
pH 7.4, 25°C, recombinant enzyme
0.00074
farnesol
pH 7.4, 25°C
0.0025
farnesol
pH 7.4, 25°C
0.011
farnesol
pH 7.4, 25°C, recombinant enzyme
0.0042
geraniol
pH 7.4, 25°C
0.012
geraniol
pH 7.4, 25°C
0.076
geraniol
pH 7.4, 25°C, recombinant enzyme
0.57
geraniol
pH 7.4, 25°C
0.0007
geranylgeraniol
pH 7.4, 25°C
0.00083
geranylgeraniol
pH 7.4, 25°C
0.0012
geranylgeraniol
pH 7.4, 25°C, recombinant enzyme
0.0005
isatin
pH 7.4, 25°C
0.0008
isatin
pH 7.4, 25°C
0.0011
isatin
pH 7.4, 25°C
0.0005
lithocholic acid
-
-
0.012
lithocholic acid
pH 7.4, 25°C
0.14
lithocholic acid
pH 7.4, 25°C
0.0068
NAD+
-
reduction of androstendione, pH 7.0
0.013
NAD+
pH 7.4, 25°C, with substrate S-tetralol
0.0181
NAD+
-
enzyme activity in hepatic microsomes
0.0185
NAD+
-
enzyme avtivity in hepatic microsomes, one individual animal
0.1
NAD+
-
solubilized enzyme
0.1
NAD+
-
solubilized with Triton X-100
0.164
NAD+
-
membrane bound
0.198
NAD+
-
oxidation of testosterone, pH 10.0
0.215
NAD+
-
oxidation of testosterone, pH 7.4
0.0026
NADH
pH 7.4, 25°C
0.013
NADH
pH 7.4, 25°C, with substrate S-camphorquinone
0.29
Pyridine-3-aldehyde
pH 7.4, 25°C
0.3
Pyridine-3-aldehyde
pH 7.4, 25°C
1.1
Pyridine-3-aldehyde
pH 7.4, 25°C
0.0016
testosterone
-
solubilized enzyme
0.00167
testosterone
pH 7.4, 25°C
0.0022
testosterone
-
membrane bound
0.0073
testosterone
-
solubilized with Triton X-100
0.009
testosterone
-
cofactor S-NAD+
0.0095
testosterone
-
oxidation of testosterone, pH 10.0
0.014
testosterone
-
oxidation of testosterone, pH 7.4
0.0174
testosterone
-
enzyme avtivity in hepatic microsomes, one individual animal
0.033
testosterone
-
approximate value, data fitted by eye
0.037
testosterone
pH 7.4, 25°C
0.25
testosterone
pH 7.4, 25°C
additional information
additional information
Michaelis-Menten kinetics
-
additional information
additional information
Michaelis-Menten kinetics
-
additional information
additional information
J7M9D0
Michaelis-Menten kinetics
-
additional information
additional information
Michaelis-Menten kinetics
-
additional information
additional information
-
Michaelis-Menten kinetics
-
additional information
additional information
Michaelis-Menten kinetics of wild-type and mutant enzymes, overview
-
additional information
additional information
J7M9D0
Michaelis-Menten kinetics of wild-type and mutant enzymes, overview
-
additional information
additional information
Michaelis-Menten kinetics of wild-type and mutant enzymes, overview
-
additional information
additional information
-
Michaelis-Menten kinetics of wild-type and mutant enzymes, overview
-
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0.021
(2E)-3-(3,3-dimethyl-3,4-dihydro-2H-1-benzopyran-6-yl)prop-2-enoate
Homo sapiens
pH 7.0, 37°C
0.0136
(2E)-3-(4-bromophenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0136
(2E)-3-(4-ethylphenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0134
(2E)-3-(4-methylphenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0047
(2E)-3-prop-2-enoic acid
Homo sapiens
pH 7.0, 37°C
0.0001
(2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoic acid
Homo sapiens
pH 7.0, 37°C
0.0086
(2E)-3-[4-(acetyloxy)-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoate
Homo sapiens
pH 7.0, 37°C
0.00044
(2E)-3-[4-(acetyloxy)-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoic acid
Homo sapiens
pH 7.0, 37°C
0.0063
(2E)-3-[4-(benzoyloxy)phenyl]prop-2-enoic acid
Homo sapiens
pH 7.0, 37°C
0.0058
(2E)-3-[4-(methylsulfanyl)phenyl]-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.068
(2E)-3-[4-(pyridine-4-carbonyloxy)phenyl]prop-2-enoic acid
Homo sapiens
pH 7.0, 37°C
0.0097
(2E)-3-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoate
Homo sapiens
pH 7.0, 37°C
0.00356
(4-chlorophenyl)(5-methoxy-2-methyl-1H-indol-1-yl)methanone
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00096
(E)-3-(3-((3-phenylpropanoyl)oxy)phenyl)acrylic acid
Homo sapiens
pH 7.0, 37°C
0.0023
(Z/E)-3-(4-((3-phenylpropanoyl)oxy)phenyl)acrylic acid
Homo sapiens
pH 7.0, 37°C
0.632
(Z/E)-tert-butyl 3-(4-(3-phenylpropanoyloxy)phenyl)acrylate
Homo sapiens
pH 7.0, 37°C
0.000094
1-(4-[[(2R)-2-methylpiperidin-1-yl]sulfonyl]phenyl)-1,3-dihydro-2H-pyrrol-2-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000056
1-(4-[[(2R,6S)-2,6-dimethylpiperidin-1-yl]sulfonyl]phenyl)pyrrolidin-2-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000052
1-[4-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)phenyl]pyrrolidin-2-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000213
2-(2,4-dioxo-1,3-thiazolidin-5-yl)-N-(2-hydroxyphenyl)acetamide
Homo sapiens
pH 7.0, temperature not specified in the publication
0.00882
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(2-methylbenzene-1-sulfonyl)acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00111
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-cyanobenzene-1-sulfonyl)acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00786
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-fluorobenzene-1-sulfonyl)acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0058
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methoxybenzene-1-sulfonyl)acetamide
Homo sapiens
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0124
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methylbenzene-1-sulfonyl)acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00252
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-phenoxybenzene-1-sulfonyl)acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00373
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(5-chlorothiophene-2-sulfonyl)acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.012
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(methanesulfonyl)acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00119
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(naphthalene-2-sulfonyl)acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00021
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00265
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[3-(trifluoromethyl)benzene-1-sulfonyl]acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00634
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]acetamide
Homo sapiens
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00207
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00074
2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0052
2-[[(3-hydroxyphenyl)carbonyl]amino]-4,5-dimethoxybenzoic acid
Homo sapiens
pH 7.0, temperature not specified in the publication
0.00084
2-[[(3-hydroxyphenyl)carbonyl]amino]-5-nitrobenzoic acid
Homo sapiens
pH 7.0, temperature not specified in the publication
0.08
3-((4-nitronaphthalen-1-yl)amino)benzoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.1
3-(5-methoxy-2-methyl-1H-indol-3-yl)propanoic acid
Homo sapiens
above, 100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.000036
3-[(4-nitrophenyl)amino]benzoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00015
3-[1-(4-chlorobenzoyl)-2-ethyl-5-methoxy-1H-indol-3-yl]propanoic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00007 - 0.00009
3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid
0.00029
3-[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]propanoic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00022
3-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]propanoic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00012
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00029
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2-methylpropanoic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00325
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(2-methylbenzene-1-sulfonyl)propanamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00311
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(4-methylbenzene-1-sulfonyl)propanamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00553
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)-2-methylpropanamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00034
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)propanamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00254
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(naphthalene-2-sulfonyl)propanamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00144
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(trifluoromethanesulfonyl)propanamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00469
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]propanamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0025
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethoxy)benzene-1-sulfonyl]propanamide
Homo sapiens
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00111
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]propanamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00013
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanoic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.000054
3-[[4-(methoxymethyl)phenyl]amino]benzoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000062
3-[[4-(trifluoromethyl)phenyl]amino]benzoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00546
3a-phenyl-2,3,3a,4-tetrahydro-1H-pyrrolo[1,2-a]benzimidazol-1-one
Homo sapiens
pH 7.0, temperature not specified in the publication
0.00015
4-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]butanoic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0019
5-bromo-2-[[(3-hydroxyphenyl)carbonyl]amino]benzoic acid
Homo sapiens
pH 7.0, temperature not specified in the publication
0.0022
5-chloro-2-[[(3-hydroxyphenyl)carbonyl]amino]benzoic acid
Homo sapiens
pH 7.0, temperature not specified in the publication
0.0024
5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.000279
6-methoxy-9-[3-(trifluoromethyl)benzoyl]-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00034
9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-2-carboxylic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00016
9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00507
9-(4-chlorobenzoyl)-N-(methanesulfonyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.021
ferulic acid
Homo sapiens
pH 7.0, 37°C
0.00013 - 0.02
ikarisoside A
0.0001
indomethacin
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.086
m-coumaric acid
Homo sapiens
pH 7.0, 37°C
0.02278
methyl 5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylate
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.01134
methyl [1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetate
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00564
methyl [1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetate
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00224 - 0.00759
methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate
0.00754 - 0.01571
methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate
0.00209
N-(4-acetylbenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00265
N-(4-acetylbenzene-1-sulfonyl)-3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00397
N-(4-bromobenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00194
N-[2,5-bis(trifluoromethyl)benzene-1-sulfonyl]-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0022 - 0.015
noranhydroicaritin
0.199
p-coumaric acid
Homo sapiens
pH 7.0, 37°C
0.00065 - 0.02
Phenolphthalein
607
tert-butyl(2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoate
Homo sapiens
pH 7.0, 37°C
0.0091 - 0.05
zearalenone
0.0005
[1-(4-chlorobenzoyl)-5-fluoro-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00025
[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00096
[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00007
[1-(4-chlorobenzoyl)-5-methoxy-2-propyl-1H-indol-3-yl]acetic acid
Homo sapiens
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00496
[1-(4-fluorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00071
[1-(4-fluorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00012
[1-[4-(chloromethyl)benzoyl]-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00223
[5-fluoro-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00014
[5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00521
[5-methoxy-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
Homo sapiens
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00108
[5-methoxy-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
Homo sapiens
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00016
[5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00244
[5-methoxy-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00027
[5-methoxy-2-methyl-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00007
3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid
Homo sapiens
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00009
3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.009
Hexestrol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.013
Hexestrol
Mesocricetus auratus
pH 7.4, 25°C, recombinant enzyme
0.05
Hexestrol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.05
Hexestrol
Oryctolagus cuniculus
above, pH 7.4, 25°C, recombinant wild-type and mutant enzymes
0.073
Hexestrol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.002
hinokitiol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.0026
hinokitiol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant mutant Y118F/F310I enzyme
0.0032
hinokitiol
Mesocricetus auratus
pH 7.4, 25°C, recombinant enzyme
0.01
hinokitiol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant mutant Y118F enzyme
0.013
hinokitiol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant mutant F310I enzyme
0.037
hinokitiol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.042
hinokitiol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.017
icarisid II
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.021
icarisid II
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.05
icarisid II
Oryctolagus cuniculus
above, pH 7.4, 25°C, recombinant enzyme
0.00013
ikarisoside A
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.0004
ikarisoside A
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant mutant Y118F/F310I enzyme
0.00049
ikarisoside A
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant mutant Y118F enzyme
0.009
ikarisoside A
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.009
ikarisoside A
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant wild-type enzyme
0.013
ikarisoside A
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.02
ikarisoside A
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant mutant F310I enzyme
0.015
kaempferol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.02
kaempferol
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.02
kaempferol
Oryctolagus cuniculus
above, pH 7.4, 25°C, recombinant enzyme
0.00224
methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00759
methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate
Homo sapiens
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00754
methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate
Homo sapiens
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.01571
methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate
Homo sapiens
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0022
noranhydroicaritin
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.0064
noranhydroicaritin
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.015
noranhydroicaritin
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.00065
Phenolphthalein
Mesocricetus auratus
pH 7.4, 25°C, recombinant enzyme
0.007
Phenolphthalein
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.017
Phenolphthalein
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.02
Phenolphthalein
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.012
quercetin
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.018
quercetin
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.026
quercetin
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.0024
quercitrin
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.0025
quercitrin
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.04
quercitrin
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.0091
zearalenone
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.05
zearalenone
Oryctolagus cuniculus
pH 7.4, 25°C, recombinant enzyme
0.05
zearalenone
Oryctolagus cuniculus
above, pH 7.4, 25°C, recombinant enzyme
0.05
zearalenone
Oryctolagus cuniculus
above, pH 7.4, 25°C, recombinant wild-type and mutant enzymesenzyme
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Ohmura, M.; Hara, A.; Nakagawa, M.; Sawada, H.
Demonstration of 3alpha(17beta)-hydroxysteroid dehydrogenase distinct from 3alpha-hydroxysteroid dehydrogenase in hamster liver
Biochem. J.
266
583-589
1990
Mesocricetus auratus
brenda
Sawada, H.; Hara, A.; Ohmura, M.; Nakayama, T.; Deyashi, Y.
Kinetic and stereochemical characterization of hamster liver 3alpha-hydroxysteroid dehydrogenase and 3alpha(17beta)-hydroxysteroid dehydrogenase
J. Biochem.
109
770-775
1991
Mesocricetus auratus
brenda
Krazeisen, A.; Breitling, R.; Mller, G.; Adamski, J.
Phytoestrogens inhibit human 17beta-hydroxysteroid dehydrogenase type 5
Mol. Cell. Endocrinol.
171
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2001
Homo sapiens
brenda
Stupans, I.; Kong, S.; Kirlich, S.; McKinnon, R.A.; Murray, M.
Testosterone dehydrogenase activity in koala liver: characterization of cofactor and steroid substrate differences
Comp. Biochem. Physiol. B
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2000
Homo sapiens, Notamacropus eugenii, Phascolarctos cinereus, Rattus norvegicus
brenda
Carre, J.L.; Quemener, E.; Amet, Y.; Simon, B.; Berthou, F.; Mangin, P.; Floch, H.H.; Abalain, J.H.
Characterization and solubization of testosterone 17beta-hydroxysteroid dehydrogenase in human hyperplastic prostate
J. Steroid Biochem. Mol. Biol.
46
265-267
1993
Homo sapiens
brenda
Dumont, M.; Luu-The, V.; de Lanoit, Y.; Labrie, F.
Expression of human 17beta-hydroxysteroid dehydrogenase in mammalian cells
J. Steroid Biochem. Mol. Biol.
41
605-608
1992
Homo sapiens
brenda
Itagaki, E.; Iwaya, T.
Purification and characterization of 17beta-hydroxysteroid dehydrogenase from Cylindrocarpon radicicola
J. Biochem.
103
1039-1044
1988
Ilyonectria destructans
brenda
Payne, D.W.; Talalay, P.
Isolation of novel microbiol 3alpha-, 3beta, and 17beta-hydroxysteroid dehydrogenases
J. Biol. Chem.
260
13648-13655
1985
Alcaligenes sp.
brenda
Blomquist, C.H.; Kotts, C.E.; Hakanson, E.Y.
Microsomal 17beta-hydroxysteroid dehydrogenase of guinea pig liver: detergent solubilization and a comparison of kinetic and stability properties of bound and solubilized forms
J. Steroid Biochem.
8
193-198
1977
Cavia porcellus
brenda
Markert, C.; Trger, L.
Enzyminduktion bei Streptomyces hydrogenans, V. Charakterisierung der Testosteron-17beta-Dehydrogenase und ihre Induktion durch Steroide
Hoppe-Seyler's Z. Physiol. Chem.
356
1843-1852
1975
Streptomyces exfoliatus
-
brenda
Ghraf, R.; Raible, M.; Schriefers, H.
11beta- und 17beta-Hydroxysteroid-dehydrogenase-Aktivitten der Rattenleber
Hoppe-Seyler's Z. Physiol. Chem.
354
299-305
1973
Rattus norvegicus
brenda
Endahl, G.L.; Kochakian, C.D.; Hamm, D.
Separation of a triphosphopyridine nucleotide-specific from a diphosphopyridine nucleotide-specific 17beta-hydroxy-(testosterone)dehydrogenase of guinea pig liver
J. Biol. Chem.
235
2793-2796
1960
Cavia porcellus
-
brenda
Villee, C.A.; Spencer, J.M.
Some properties of the pyridine nucleotide-specific 17beta-hydroxy steroid dehydrogenases of guinea pig liver
J. Biol. Chem.
235
3615-3619
1960
Cavia porcellus
brenda
Sweat, M.L.; Samuels, L.T.; Lumry, R.
Preparation and characterization of the enzyme which converts testosterone to androstendione
J. Biol. Chem.
185
75-84
1950
Bos taurus
brenda
Ngatcha, B.T.; Laplante, Y.; Labrie, F.; Luu-The, V.; Poirier, D.
3beta-Alkyl-androsterones as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase: inhibitory potency in intact cells, selectivity towards isoforms 1, 2, 5 and 7, binding affinity for steroid receptors, and proliferative/antiproliferative activities on AR+ and ER+ cell lines
Mol. Cell. Endocrinol.
248
225-232
2006
Homo sapiens
brenda
Fung, K.M.; Samara, E.N.; Wong, C.; Metwalli, A.; Krlin, R.; Bane, B.; Liu, C.Z.; Yang, J.T.; Pitha, J.V.; Culkin, D.J.; Kropp, B.P.; Penning, T.M.; Lin, H.K.
Increased expression of type 2 3alpha-hydroxysteroid dehydrogenase/type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3) and its relationship with androgen receptor in prostate carcinoma
Endocr. Relat. Cancer
13
169-180
2006
Homo sapiens
brenda
Azzarello, J.; Fung, K.M.; Lin, H.K.
Tissue distribution of human AKR1C3 and rat homolog in adult genitourinary system
J. Histochem. Cytochem.
56
853-861
2008
Homo sapiens, Rattus norvegicus
brenda
Guise, C.P.; Abbattista, M.R.; Singleton, R.S.; Holford, S.D.; Connolly, J.; Dachs, G.U.; Fox, S.B.; Pollock, R.; Harvey, J.; Guilford, P.; Donate, F.; Wilson, W.R.; Patterson, A.V.
The bioreductive prodrug PR-104A is activated under aerobic conditions by human aldo-keto reductase 1C3
Cancer Res.
70
1573-1584
2010
Homo sapiens
brenda
Nakamura, Y.; Hornsby, P.; Casson, P.; Morimoto, R.; Satoh, F.; Xing, Y.; Kennedy, M.; Sasano, H.; Rainey, W.
Type 5 17-hydroxysteroid dehydrogenase (AKR1C3) contributes to testosterone production in the adrenal reticularis
J. Clin. Endocrinol. Metab.
94
2192-2198
2009
Homo sapiens
brenda
Byrns, M.C.; Duan, L.; Lee, S.H.; Blair, I.A.; Penning, T.M.
Aldo-keto reductase 1C3 expression in MCF-7 cells reveals roles in steroid hormone and prostaglandin metabolism that may explain its over-expression in breast cancer
J. Steroid Biochem. Mol. Biol.
118
177-187
2010
Homo sapiens
brenda
Ashley, R.A.; Yu, Z.; Fung, K.M.; Frimberger, D.; Kropp, B.P.; Penning, T.M.; Lin, H.K.
Developmental evaluation of aldo-keto reductase 1C3 expression in the cryptorchid testis
Urology
76
67-72
2010
Homo sapiens
brenda
Jackson, V.J.; Yosaatmadja, Y.; Flanagan, J.U.; Squire, C.J.
Structure of AKR1C3 with 3-phenoxybenzoic acid bound
Acta Crystallogr. Sect. F
68
409-413
2012
Homo sapiens (P42330), Homo sapiens
brenda
Adeniji, A.O.; Twenter, B.M.; Byrns, M.C.; Jin, Y.; Winkler, J.D.; Penning, T.M.
Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3)
Bioorg. Med. Chem. Lett.
21
1464-1468
2011
Homo sapiens (P42330)
brenda
Chen, M.; Adeniji, A.O.; Twenter, B.M.; Winkler, J.D.; Christianson, D.W.; Penning, T.M.
Crystal structures of AKR1C3 containing an N-(aryl)amino-benzoate inhibitor and a bifunctional AKR1C3 inhibitor and androgen receptor antagonist. Therapeutic leads for castrate resistant prostate cancer
Bioorg. Med. Chem. Lett.
22
3492-3497
2012
Homo sapiens (P42330)
brenda
Sinreih, M.; Sosic, I.; Beranic, N.; Turk, S.; Adeniji, A.O.; Penning, T.M.; Rizner, T.L.; Gobec, S.
N-Benzoyl anthranilic acid derivatives as selective inhibitors of aldo-keto reductase AKR1C3
Bioorg. Med. Chem. Lett.
22
5948-5951
2012
Homo sapiens (P42330)
brenda
Matsunaga, T.; Hojo, A.; Yamane, Y.; Endo, S.; El-Kabbani, O.; Hara, A.
Pathophysiological roles of aldo-keto reductases (AKR1C1 and AKR1C3) in development of cisplatin resistance in human colon cancers
Chem. Biol. Interact.
202
234-242
2013
Homo sapiens (P42330)
brenda
Heinrich, D.M.; Flanagan, J.U.; Jamieson, S.M.; Silva, S.; Rigoreau, L.J.; Trivier, E.; Raynham, T.; Turnbull, A.P.; Denny, W.A.
Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3
Eur. J. Med. Chem.
62
738-744
2013
Homo sapiens (P42330)
brenda
Gazvoda, M.; Beranic, N.; Turk, S.; Burja, B.; Kocevar, M.; Rizner, T.L.; Gobec, S.; Polanc, S.
2,3-diarylpropenoic acids as selective non-steroidal inhibitors of type-5 17?-hydroxysteroid dehydrogenase (AKR1C3)
Eur. J. Med. Chem.
62
89-97
2013
Homo sapiens (P42330)
brenda
Zakharov, V.; Lin, H.K.; Azzarello, J.; McMeekin, S.; Moore, K.N.; Penning, T.M.; Fung, K.M.
Suppressed expression of type 2 3alpha/type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3) in endometrial hyperplasia and carcinoma
Int. J. Clin. Exp. Pathol.
3
608-617
2010
Homo sapiens (P42330)
brenda
Miller, V.L.; Lin, H.K.; Murugan, P.; Fan, M.; Penning, T.M.; Brame, L.S.; Yang, Q.; Fung, K.M.
Aldo-keto reductase family 1 member C3 (AKR1C3) is expressed in adenocarcinoma and squamous cell carcinoma but not small cell carcinoma
Int. J. Clin. Exp. Pathol.
5
278-289
2012
Homo sapiens
brenda
Brozic, P.; Turk, S.; Adeniji, A.O.; Konc, J.; Janezic, D.; Penning, T.M.; Lanisnik Rizner, T.; Gobec, S.
Selective inhibitors of aldo-keto reductases AKR1C1 and AKR1C3 discovered by virtual screening of a fragment library
J. Med. Chem.
55
7417-7424
2012
Homo sapiens (P42330)
brenda
Liedtke, A.J.; Adeniji, A.O.; Chen, M.; Byrns, M.C.; Jin, Y.; Christianson, D.W.; Marnett, L.J.; Penning, T.M.
Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer
J. Med. Chem.
56
2429-2446
2013
Homo sapiens (P42330)
brenda
Byrns, M.C.; Mindnich, R.; Duan, L.; Penning, T.M.
Overexpression of aldo-keto reductase 1C3 (AKR1C3) in LNCaP cells diverts androgen metabolism towards testosterone resulting in resistance to the 5alpha-reductase inhibitor finasteride
J. Steroid Biochem. Mol. Biol.
130
7-15
2012
Homo sapiens (P42330)
brenda
Matsunaga, T.; Yamaguchi, A.; Morikawa, Y.; Kezuka, C.; Takazawa, H.; Endo, S.; El-Kabbani, O.; Tajima, K.; Ikari, A.; Hara, A.
Induction of aldo-keto reductases (AKR1C1 and AKR1C3) abolishes the efficacy of daunorubicin chemotherapy for leukemic U937 cells
Anticancer Drugs
25
868-877
2014
Homo sapiens (P42330)
brenda
Endo, S.; Matsunaga, T.; Fujimoto, A.; Kumada, S.; Arai, Y.; Miura, Y.; Mikamo, H.; El-Kabbani, O.; Yamano, S.; Iinuma, M.; Hara, A.
Characterization of rabbit morphine 6-dehydrogenase and two NAD+-dependent 3alpha(17beta)-hydroxysteroid dehydrogenases
Arch. Biochem. Biophys.
529
131-139
2013
Oryctolagus cuniculus (G1T465), Oryctolagus cuniculus (J7M9D0), Oryctolagus cuniculus (J7MBS9), Oryctolagus cuniculus
brenda
Zang, T.; Verma, K.; Chen, M.; Jin, Y.; Trippier, P.C.; Penning, T.M.
Screening baccharin analogs as selective inhibitors against type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3)
Chem. Biol. Interact.
234
339-348
2015
Homo sapiens (P42330)
brenda
Endo, S.; Noda, M.; Ikari, A.; Tatematsu, K.; El-Kabbani, O.; Hara, A.; Kitade, Y.; Matsunaga, T.
Characterization of hamster NAD+-dependent 3(17)beta-hydroxysteroid dehydrogenase belonging to the aldo-keto reductase 1C subfamily
J. Biochem.
158
425-434
2015
Mesocricetus auratus (A0A097ZMY7)
brenda
Ji, Y.; Yang, J.; Gao, L.; Xiong, G.; Yu, Y.; Zhang, Y.
Characterization of a LuxR repressor for 3,17beta-HSD in Comamonas testosteroni ATCC11996
Chem. Biol. Interact.
336
109271
2021
Comamonas testosteroni, Comamonas testosteroni ATCC 11996
brenda