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(S)-alpha-tetralol + NADP+
alpha-tetralone + NADPH + H+
-
-
-
?
(S)-tetralol + NADP+
? + NADPH
-
-
-
?
4-oxo-2-nonenal + NADPH + H+
4-hydroxynonenal + NADP+
-
-
-
?
1-acenaphthenol + NADPH
?
-
-
-
-
?
1-indanone + NADPH
?
-
-
-
?
10-oxonortriptyline + NADPH
?
3-ketosteroids + NADPH
3-hydroxysteroids + NADP+
-
-
-
?
4-hydroxynonenal + NADPH
?
-
-
-
?
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
5alpha-dihydrotestosterone + NADPH + H+
5alpha-androstan-3alpha,17beta-diol + NADP+
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH
9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+
oracin + NADPH
? + NADP+
-
-
-
-
?
tibolone + NADPH + H+
3-hydroxytibolone + NADP+
additional information
?
-
10-oxonortriptyline + NADPH
?
-
-
-
?
10-oxonortriptyline + NADPH
?
a drug acting as substrate
-
-
?
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
androgen-inactivating enzyme
-
-
r
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
the enzyme is important in inactivation of DHT
-
-
?
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
the enzyme plays a crucial role in the regulation of the intracellular concentrations of testosterone and 5alpha-dihydrotestosterone, two steroids directly linked to the etiology and the progression of many prostate diseases and cancer, overview
-
-
r
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
i.e. DHT
-
-
?
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
i.e. DHT, substrate and cofactor binding site structure
-
-
r
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
i.e. DHT, the enzyme prefers the reductive reaction
-
-
r
5alpha-dihydrotestosterone + NADPH + H+
5alpha-androstan-3alpha,17beta-diol + NADP+
-
inactivation of the potent androgen in human prostate
-
-
r
5alpha-dihydrotestosterone + NADPH + H+
5alpha-androstan-3alpha,17beta-diol + NADP+
-
inactivation of the potent androgen in human prostate, fluorometric activity measurement in intact cells, overview
-
-
?
5alpha-dihydrotestosterone + NADPH + H+
5alpha-androstan-3alpha,17beta-diol + NADP+
-
i.e. DHT
-
-
?
5alpha-dihydrotestosterone + NADPH + H+
5alpha-androstan-3alpha,17beta-diol + NADP+
-
i.e. DHT
-
-
r
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH
9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+
-
competitive substrate, fluorometric activity measurement in intact cells, overview
-
-
?
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH
9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+
-
competitive substrate
-
-
?
acetohexamide + NADPH
?
-
-
-
?
acetohexamide + NADPH
?
a drug acting as substrate
-
-
?
befunolol + NADPH
?
-
-
-
?
befunolol + NADPH
?
a drug acting as substrate
-
-
?
daunorubicin + NADPH
?
-
-
-
?
daunorubicin + NADPH
?
a drug acting as substrate
-
-
?
dolasetron + NADPH
?
-
-
-
?
dolasetron + NADPH
?
a drug acting as substrate
-
-
?
haloperidol + NADPH
?
-
-
-
?
haloperidol + NADPH
?
a drug acting as substrate
-
-
?
ketoprofen + NADPH
?
-
-
-
?
ketoprofen + NADPH
?
a drug acting as substrate
-
-
?
ketotifen + NADPH
?
-
-
-
?
ketotifen + NADPH
?
a drug acting as substrate
-
-
?
loxoprofen + NADPH
?
-
-
-
?
loxoprofen + NADPH
?
a drug acting as substrate
-
-
?
Naloxone + NADPH
?
-
-
-
?
Naloxone + NADPH
?
a drug acting as substrate
-
-
?
Naltrexone + NADPH
?
-
-
-
?
Naltrexone + NADPH
?
a drug acting as substrate
-
-
?
oracin + NADPH
?
-
-
-
?
oracin + NADPH
?
a drug acting as substrate
-
-
?
oxycodone + NADPH
?
-
-
-
?
oxycodone + NADPH
?
a drug acting as substrate
-
-
?
tibolone + NADPH + H+
3-hydroxytibolone + NADP+
-
tibolone is used to treat climacteric symptoms and prevent osteoporosis, it exerts tissue-selective effects via site-specific metabolism into 3alpha- and 3beta-hydroxymetabolites and a DELTA4-isomer
-
-
?
tibolone + NADPH + H+
3-hydroxytibolone + NADP+
-
i.e. [7alpha,17alpha]-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one, stereoselctive reaction to the 3alpha-hydroxytibolone product
-
-
?
additional information
?
-
the enzyme is important in the synthesis of neuroactive 5alpha/beta-pregnan-3alpha-ol-20-ones from their precursors, the enzyme plays a role in development and progression of prostate cancer
-
-
?
additional information
?
-
-
the enzyme is important in the synthesis of neuroactive 5alpha/beta-pregnan-3alpha-ol-20-ones from their precursors, the enzyme plays a role in development and progression of prostate cancer
-
-
?
additional information
?
-
the RODH like 3alpha/17beta-HSD, EC 1.1.1.239, regulates the transactivation of AKR1C2, overview
-
-
?
additional information
?
-
-
the RODH like 3alpha/17beta-HSD, EC 1.1.1.239, regulates the transactivation of AKR1C2, overview
-
-
?
additional information
?
-
besides 3alpha-hydroxysteroid dehydrogenase activity, the enzyme shows also 17beta-hydroxysteroid dehydrogenase activity towards 5alpha-dihydrotestosterone, EC 1.1.1.239, overview, the enzyme reveals an 'induced-fit' mechanism and a conserved basic motif involved in the binding of androgen, the enzyme also binds many structurally different molecules such as 4-hydroxynonenal, polycyclic aromatic hydrocarbons, and indanone
-
-
?
additional information
?
-
-
besides 3alpha-hydroxysteroid dehydrogenase activity, the enzyme shows also 17beta-hydroxysteroid dehydrogenase activity towards 5alpha-dihydrotestosterone, EC 1.1.1.239, overview, the enzyme reveals an 'induced-fit' mechanism and a conserved basic motif involved in the binding of androgen, the enzyme also binds many structurally different molecules such as 4-hydroxynonenal, polycyclic aromatic hydrocarbons, and indanone
-
-
?
additional information
?
-
-
AKR1C3 catalyzes androgen, estrogen, and prostaglandin metabolism, AKR1C3 is also involved in cancer development or progression
-
-
?
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10-oxonortriptyline + NADPH
?
a drug acting as substrate
-
-
?
3-ketosteroids + NADPH
3-hydroxysteroids + NADP+
-
-
-
?
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
5alpha-dihydrotestosterone + NADPH + H+
5alpha-androstan-3alpha,17beta-diol + NADP+
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH
9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+
-
competitive substrate, fluorometric activity measurement in intact cells, overview
-
-
?
acetohexamide + NADPH
?
a drug acting as substrate
-
-
?
befunolol + NADPH
?
a drug acting as substrate
-
-
?
daunorubicin + NADPH
?
a drug acting as substrate
-
-
?
dolasetron + NADPH
?
a drug acting as substrate
-
-
?
haloperidol + NADPH
?
a drug acting as substrate
-
-
?
ketoprofen + NADPH
?
a drug acting as substrate
-
-
?
ketotifen + NADPH
?
a drug acting as substrate
-
-
?
loxoprofen + NADPH
?
a drug acting as substrate
-
-
?
Naloxone + NADPH
?
a drug acting as substrate
-
-
?
Naltrexone + NADPH
?
a drug acting as substrate
-
-
?
oracin + NADPH
?
a drug acting as substrate
-
-
?
oxycodone + NADPH
?
a drug acting as substrate
-
-
?
tibolone + NADPH + H+
3-hydroxytibolone + NADP+
-
tibolone is used to treat climacteric symptoms and prevent osteoporosis, it exerts tissue-selective effects via site-specific metabolism into 3alpha- and 3beta-hydroxymetabolites and a DELTA4-isomer
-
-
?
additional information
?
-
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
androgen-inactivating enzyme
-
-
r
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
the enzyme is important in inactivation of DHT
-
-
?
5alpha-dihydrotestosterone + NADPH
5alpha-androstane-3alpha,17beta-diol + NADP+
the enzyme plays a crucial role in the regulation of the intracellular concentrations of testosterone and 5alpha-dihydrotestosterone, two steroids directly linked to the etiology and the progression of many prostate diseases and cancer, overview
-
-
r
5alpha-dihydrotestosterone + NADPH + H+
5alpha-androstan-3alpha,17beta-diol + NADP+
-
inactivation of the potent androgen in human prostate
-
-
r
5alpha-dihydrotestosterone + NADPH + H+
5alpha-androstan-3alpha,17beta-diol + NADP+
-
inactivation of the potent androgen in human prostate, fluorometric activity measurement in intact cells, overview
-
-
?
additional information
?
-
the enzyme is important in the synthesis of neuroactive 5alpha/beta-pregnan-3alpha-ol-20-ones from their precursors, the enzyme plays a role in development and progression of prostate cancer
-
-
?
additional information
?
-
-
the enzyme is important in the synthesis of neuroactive 5alpha/beta-pregnan-3alpha-ol-20-ones from their precursors, the enzyme plays a role in development and progression of prostate cancer
-
-
?
additional information
?
-
the RODH like 3alpha/17beta-HSD, EC 1.1.1.239, regulates the transactivation of AKR1C2, overview
-
-
?
additional information
?
-
-
the RODH like 3alpha/17beta-HSD, EC 1.1.1.239, regulates the transactivation of AKR1C2, overview
-
-
?
additional information
?
-
-
AKR1C3 catalyzes androgen, estrogen, and prostaglandin metabolism, AKR1C3 is also involved in cancer development or progression
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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(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-[4-(methylsulfanyl)phenyl]-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
93.5% inhibition at 0.1 mM
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
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-[[(3-hydroxyphenyl)carbonyl]amino]-4,5-dimethoxybenzoic acid
-
2-[[(3-hydroxyphenyl)carbonyl]amino]-5-nitrobenzoic acid
-
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-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-[[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
5-bromo-2-[[(3-hydroxyphenyl)carbonyl]amino]benzoic acid
-
5-chloro-2-[[(3-hydroxyphenyl)carbonyl]amino]benzoic acid
-
2'-hydroxyflavanone
-
most potent inhibitor, 0.02 mM inhibits by 98.9% and in an uncompetitive manner
7-hydroxyflavone
-
very potent inhibitor, 0.02 mM inhibits by 82.5%
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one
-
competitive
apigenin
-
0.02 mM inhibits by ca. 50%
celecoxib
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.050 mM in fluorometric assay, in vitro IC50: 0.050 mM in fluorometric assay
epigallocatechin gallate
-
-
Ibuprofen
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.017 mM in fluorometric assay, in vitro IC50: 0.009 mM in fluorometric assay
luteolin
-
0.02 mM inhibits by ca. 50%
naproxen
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0094 mM in fluorometric assay, 0.016 mM in radiometric assay, in vitro IC50: 0.0027 mM in fluorometric assay
naringenin
-
very potent inhibitor, 0.02 mM inhibits by 71.9%
Phenolphthalein
-
AKR1C4-selective inhibitor, in vitro and in vivo inhibition, IC50: 0.0004 mM
quercetin
-
0.02 mM inhibits by ca. 50%
silibinin
-
0.02 mM inhibits by ca. 50%
ursodeoxycholate
-
natural inhibitor, in vivo IC50: 0.00024 mM in fluorometric assay, 0.00014 mM in radiometric assay, in vitro IC50: 0.000049 mM in fluorometric assay
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
Flufenamic acid
-
a nonsteroidalanti-inflammatory drug, IC50: 1.084 mM
Flufenamic acid
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0040 mM in fluorometric assay, in vitro IC50: 0.00031 mM in fluorometric assay
additional information
-
dutasteride alters the expression level of the enzyme in breast cancer cells, the inhibitor affects the 5alpha-progesterone reductase and the progesterone metabolism, overview
-
additional information
-
no inhibition by the bile acid 5beta-cholanic acid-3alpha,7alpha-diol
-
additional information
-
is not inhibited by 0.02 mM caffeic acid, rutin, 4-hydroxybenzoic acid, cyanin chloride and taxifolin
-
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Adenocarcinoma
Expression of dihydrodiol dehydrogenase and resistance to chemotherapy and radiotherapy in adenocarcinoma cells of lung.
Adenocarcinoma
[Gene expression profiling of human ovarian epithelial tumors by digo nucleotide microarray]
Breast Neoplasms
An indomethacin analogue, N-(4-chlorobenzoyl)-melatonin, is a selective inhibitor of aldo-keto reductase 1C3 (type 2 3alpha-HSD, type 5 17beta-HSD, and prostaglandin F synthase), a potential target for the treatment of hormone dependent and hormone independent malignancies.
Breast Neoplasms
Selective loss of AKR1C1 and AKR1C2 in breast cancer and their potential effect on progesterone signaling.
Carcinoma
Dihydrodiol dehydrogenase in drug resistance and sensitivity of human carcinomas.
Carcinoma
Expression and characterization of recombinant type 2 3 alpha-hydroxysteroid dehydrogenase (HSD) from human prostate: demonstration of bifunctional 3 alpha/17 beta-HSD activity and cellular distribution.
Carcinoma
Expression of dihydrodiol dehydrogenase plays important roles in apoptosis- and drug-resistance of A431 squamous cell carcinoma.
Carcinoma
Increased expression of dihydrodiol dehydrogenase induces resistance to cisplatin in human ovarian carcinoma cells.
Carcinoma
Inverse expression of dihydrodiol dehydrogenase and glutathione-S-transferase in patients with esophageal squamous cell carcinoma.
Carcinoma
Sequence of the cDNA of a human dihydrodiol dehydrogenase isoform (AKR1C2) and tissue distribution of its mRNA.
Carcinoma
Steroid-converting enzymes in human ovarian carcinomas.
Carcinoma
Ubiquitous induction of resistance to platinum drugs in human ovarian, cervical, germ-cell and lung carcinoma tumor cells overexpressing isoforms 1 and 2 of dihydrodiol dehydrogenase.
Carcinoma
[Gene expression profiling of human ovarian epithelial tumors by digo nucleotide microarray]
Carcinoma, Hepatocellular
Characterization of dihydrodiol dehydrogenase in rat H-4IIe hepatoma cells.
Carcinoma, Hepatocellular
Proteome analysis of rat hepatomas: carcinogen-dependent tumor-associated protein variants.
Carcinoma, Hepatocellular
Reduction of dihydrodiol dehydrogenase expression in resected hepatocellular carcinoma.
Carcinoma, Non-Small-Cell Lung
Expression of dihydrodiol dehydrogenase in the resected stage I non-small cell lung cancer.
Carcinoma, Non-Small-Cell Lung
Overexpression of dihydrodiol dehydrogenase as a prognostic marker of non-small cell lung cancer.
Carcinoma, Non-Small-Cell Lung
Proteomics-based identification of secreted protein dihydrodiol dehydrogenase as a novel serum markers of non-small cell lung cancer.
Carcinoma, Ovarian Epithelial
Steroid-converting enzymes in human ovarian carcinomas.
Carcinoma, Squamous Cell
Expression of dihydrodiol dehydrogenase plays important roles in apoptosis- and drug-resistance of A431 squamous cell carcinoma.
Cataract
Inhibition of naphthalene cataract in rats by aldose reductase inhibitors.
Colorectal Neoplasms
The long variant of human ileal bile acid-binding protein associated with colorectal cancer exhibits sub-cellular localization and lipid binding behaviour distinct from those of the common isoform.
Dupuytren Contracture
Common Variants of the ALDH2 and DHDH Genes and the Risk of Dupuytren's Disease.
Epilepsy
Characterization of the 5alpha-reductase-3alpha-hydroxysteroid dehydrogenase complex in the human brain.
Esophageal Squamous Cell Carcinoma
Inverse expression of dihydrodiol dehydrogenase and glutathione-S-transferase in patients with esophageal squamous cell carcinoma.
Glaucoma
Altered expression of 3 alpha-hydroxysteroid dehydrogenases in human glaucomatous optic nerve head astrocytes.
Hepatoblastoma
Hepatocyte nuclear factor (HNF)-4 alpha/gamma, HNF-1 alpha, and vHNF-1 regulate the cell-specific expression of the human dihydrodiol dehydrogenase (DD)4/AKR1C4 gene.
Hirsutism
3{alpha}-Hydroxysteroid Dehydrogenase Type III Deficiency: A Novel Mechanism for Hirsutism.
Hirsutism
Cutaneous androgen metabolism: basic research and clinical perspectives.
Hypercholesterolemia
Identification of a novel hypocholesterolemic protein, major royal jelly protein 1, derived from royal jelly.
Hyperglycemia
Pathogenesis of diabetic neuropathy--do hyperglycemia and aldose reductase inhibitors affect neuroactive steroid formation in the rat sciatic nerves?
Infections
Infection of human papillomavirus and overexpression of dihydrodiol dehydrogenase in uterine cervical cancer.
Liver Diseases
Serum bile acid concentrations in patients with liver disease.
Lung Neoplasms
A possible role for dihydrodiol dehydrogenase in the formation of benzo[a]pyrene-DNA adducts in lung cancer cells and tumor tissues.
Lung Neoplasms
Diagnostic value of serum dihydrodiol dehydrogenase 2 levels in patients with non-small-cell lung cancer.
Lung Neoplasms
Expression of dihydrodiol dehydrogenase in the resected stage I non-small cell lung cancer.
Lung Neoplasms
Overexpression of dihydrodiol dehydrogenase as a prognostic marker of non-small cell lung cancer.
Lung Neoplasms
Proteomics-based identification of secreted protein dihydrodiol dehydrogenase as a novel serum markers of non-small cell lung cancer.
Melanoma
Sebocytes are the key regulators of androgen homeostasis in human skin.
Neoplasm Metastasis
Extracts of Koelreuteria henryi Dummer induce apoptosis and autophagy by inhibiting dihydrodiol dehydrogenase, thus enhancing anticancer effects.
Neoplasm Metastasis
Hepatocyte growth factor and HER2/neu downregulate expression of apoptosis-inducing factor in non-small cell lung cancer.
Neoplasms
A possible role for dihydrodiol dehydrogenase in the formation of benzo[a]pyrene-DNA adducts in lung cancer cells and tumor tissues.
Neoplasms
An indomethacin analogue, N-(4-chlorobenzoyl)-melatonin, is a selective inhibitor of aldo-keto reductase 1C3 (type 2 3alpha-HSD, type 5 17beta-HSD, and prostaglandin F synthase), a potential target for the treatment of hormone dependent and hormone independent malignancies.
Neoplasms
Dihydrodiol dehydrogenases regulate the generation of reactive oxygen species and the development of cisplatin resistance in human ovarian carcinoma cells.
Neoplasms
Evaluation of the prognostic role of a panel of biomarkers in stage IB-IIIA non-small cell lung cancer patients.
Neoplasms
Extracts of Koelreuteria henryi Dummer induce apoptosis and autophagy by inhibiting dihydrodiol dehydrogenase, thus enhancing anticancer effects.
Neoplasms
Glutathione-related enzymes contribute to resistance of tumor cells and low toxicity in normal organs to artesunate.
Neoplasms
Hepatocyte growth factor and HER2/neu downregulate expression of apoptosis-inducing factor in non-small cell lung cancer.
Neoplasms
Inhibition of 3alpha-hydroxysteroid dehydrogenase (3alpha-HSD) activity of human lung microsomes by genistein, daidzein, coumestrol and C(18)-, C(19)- and C(21)-hydroxysteroids and ketosteroids.
Neoplasms
Temporal and spatial patterns of ovarian gene transcription following an ovulatory dose of gonadotropin in the rat.
Neoplasms
Ubiquitous induction of resistance to platinum drugs in human ovarian, cervical, germ-cell and lung carcinoma tumor cells overexpressing isoforms 1 and 2 of dihydrodiol dehydrogenase.
Neoplasms
[Gene expression profiling of human ovarian epithelial tumors by digo nucleotide microarray]
Neoplasms, Germ Cell and Embryonal
Dihydrodiol dehydrogenases regulate the generation of reactive oxygen species and the development of cisplatin resistance in human ovarian carcinoma cells.
Optic Nerve Injuries
Altered expression of 3 alpha-hydroxysteroid dehydrogenases in human glaucomatous optic nerve head astrocytes.
Ovarian Neoplasms
Overexpression of dihydrodiol dehydrogenase is associated with cisplatin-based chemotherapy resistance in ovarian cancer patients.
Pneumonia
Increased annexin A1 and A2 levels in bronchoalveolar lavage fluid are associated with resistance to respiratory disease in beef calves.
Prostatic Hyperplasia
Expression and characterization of recombinant type 2 3 alpha-hydroxysteroid dehydrogenase (HSD) from human prostate: demonstration of bifunctional 3 alpha/17 beta-HSD activity and cellular distribution.
Prostatic Hyperplasia
Function of human brain short chain L-3-hydroxyacyl coenzyme A dehydrogenase in androgen metabolism.
Prostatic Neoplasms
5alpha-androstane-3alpha,17beta-diol selectively activates the canonical PI3K/AKT pathway: a bioinformatics-based evidence for androgen-activated cytoplasmic signaling.
Prostatic Neoplasms
5alpha-androstane-3alpha,17beta-diol supports human prostate cancer cell survival and proliferation through androgen receptor-independent signaling pathways: implication of androgen-independent prostate cancer progression.
Stomach Neoplasms
Identification of genes differentially expressed between gastric cancers and normal gastric mucosa with cDNA microarrays.
Stomach Neoplasms
Overexpression of dihydrodiol dehydrogenase as a prognostic marker in resected gastric cancer patients.
Uterine Cervical Neoplasms
Infection of human papillomavirus and overexpression of dihydrodiol dehydrogenase in uterine cervical cancer.
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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
0.0058
(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
0.000094
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
0.0052
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
0.000036
3-[(4-nitrophenyl)amino]benzoic acid
Homo sapiens
pH not specified in the publication, temperature 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
0.0019
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
0.0003
2'-hydroxyflavanone
Homo sapiens
-
-
0.0049
7-hydroxyflavone
Homo sapiens
-
-
0.0218
apigenin
Homo sapiens
-
-
0.05
celecoxib
Homo sapiens
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.050 mM in fluorometric assay, in vitro IC50: 0.050 mM in fluorometric assay
0.00031 - 1.084
Flufenamic acid
0.009
Ibuprofen
Homo sapiens
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.017 mM in fluorometric assay, in vitro IC50: 0.009 mM in fluorometric assay
0.0374
luteolin
Homo sapiens
-
-
0.0027
naproxen
Homo sapiens
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0094 mM in fluorometric assay, 0.016 mM in radiometric assay, in vitro IC50: 0.0027 mM in fluorometric assay
0.0024
naringenin
Homo sapiens
-
-
0.0004
Phenolphthalein
Homo sapiens
-
AKR1C4-selective inhibitor, in vitro and in vivo inhibition, IC50: 0.0004 mM
0.0188
quercetin
Homo sapiens
-
-
0.0062
silibinin
Homo sapiens
-
-
0.000049
ursodeoxycholate
Homo sapiens
-
natural inhibitor, in vivo IC50: 0.00024 mM in fluorometric assay, 0.00014 mM in radiometric assay, in vitro IC50: 0.000049 mM in fluorometric assay
0.00031
Flufenamic acid
Homo sapiens
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0040 mM in fluorometric assay, in vitro IC50: 0.00031 mM in fluorometric assay
1.084
Flufenamic acid
Homo sapiens
-
a nonsteroidalanti-inflammatory drug, IC50: 1.084 mM
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-
brenda
uniform, diffuse, and strong expression of isoform AKR1C3 in normal endometrial epithelium but not in endometrial stromal cells. The expression of AKR1C3 is reduced in both hyperplastic and carcinomatous endometrial epithelium
brenda
uniform, diffuse, and strong expression of isoform AKR1C3 in normal endometrial epithelium but not in endometrial stromal cells. The expression of AKR1C3 is reduced in both hyperplastic and carcinomatous endometrial epithelium
brenda
-
brenda
-
brenda
-
brenda
the enzyme expression is positively correlated to adiposity in woman
brenda
high expression and activity in astrocytes of glaucomatous optic nerve head
brenda
-
the urothelial epithelium lining the renal pelvis is strongly immunoreactive, but stromal cells in the underlying supporting connective tissue are negative
brenda
-
-
brenda
-
only a small number of epithelial cells are immunoreactive with both nuclear and cytoplasmic reactivity
brenda
-
-
brenda
-
positive AKR1C3 immunoreactivity is extensively present in both adenocarcinoma and squamous cell carcinoma arising from the lung and the gastroesophageal junction
brenda
-
positive AKR1C3 immunoreactivity is extensively present in both adenocarcinoma and squamous cell carcinoma arising from the lung and the gastroesophageal junction
brenda
-
strong isoform AKR1C3 immunoreactivity in columnar epithelium but only weak immunoreactivity in squamous epithelium of the gastrointestinal junction
brenda
-
primary, high expression and activity in healthy hepatocytes
brenda
-
in renal cortex, endothelial cells of the glomeruli lack immunoreactivity for AKR1C3, but the Bowmans capsule and mesangial cells are strongly reactive, as well as larger epithelial cells of the medulla, overview
brenda
-
high expression and activity in female and male liver
brenda
-
strong isoform AKR1C3 immunoreactivity in bronchial epithelium but not in bronchial glands or alveolar pneumocytes
brenda
-
positive AKR1C3 immunoreactivity is extensively present in both adenocarcinoma and squamous cell carcinoma arising from the lung and the gastroesophageal junction
brenda
-
positive AKR1C3 immunoreactivity is extensively present in both adenocarcinoma and squamous cell carcinoma arising from the lung and the gastroesophageal junction
brenda
-
-
brenda
-
positive AKR1C3 immunoreactivity is extensively present in both adenocarcinoma and squamous cell carcinoma arising from the lung and the gastroesophageal junction
brenda
-
in Leydig cells, but no or poor activity in germ cells and Sertoli cells
brenda
-
-
brenda
-
brenda
in primary prostate stromal cells, co-localization with RODH like 3alpha/17beta-HSD, EC 1.1.1.239
brenda
additional information
wide tissue distribution
brenda
additional information
-
wide tissue distribution
brenda
additional information
-
no activity in the hepatoma cell line Hep-G2
brenda
additional information
-
tissue distribution of AKR1C3, immunohistochemic analysis, overview
brenda
additional information
-
no isoform AKR1C3 immunoreactivity in bronchial glands or alveolar pneumocytes and small cell carcinoma of the lung, only weak immunoreactivity in squamous epithelium of the gastrointestinal junction
brenda
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Matsunaga, T.; Shintani, S.; Hara, A.
Multiplicity of mammalian reductases for xenobiotic carbonyl compounds
Drug Metab. Pharmacokinet.
21
1-18
2006
Homo sapiens (P52895), Homo sapiens
brenda
Jin, Y.; Penning, T.M.
Multiple steps determine the overall rate of the reduction of 5alpha-dihydrotestosterone catalyzed by human type 3 3alpha-hydroxysteroid dehydrogenase: implications for the elimination of androgens
Biochemistry
45
13054-13063
2006
Homo sapiens
brenda
Steckelbroeck, S.; Oyesanmi, B.; Jin, Y.; Lee, S.H.; Kloosterboer, H.J.; Penning, T.M.
Tibolone metabolism in human liver is catalyzed by 3alpha/3beta-hydroxysteroid dehydrogenase activities of the four isoforms of the aldo-keto reductase (AKR)1C subfamily
J. Pharmacol. Exp. Ther.
316
1300-1309
2006
Homo sapiens
brenda
Wiebe, J.P.; Souter, L.; Zhang, G.
Dutasteride affects progesterone metabolizing enzyme activity/expression in human breast cell lines resulting in suppression of cell proliferation and detachment
J. Steroid Biochem. Mol. Biol.
100
129-140
2006
Homo sapiens
brenda
Bauman, D.R.; Steckelbroeck, S.; Williams, M.V.; Peehl, D.M.; Penning, T.M.
Identification of the major oxidative 3alpha-hydroxysteroid dehydrogenase in human prostate that converts 5alpha-androstane-3alpha,17beta-diol to 5alpha-dihydrotestosterone: a potential therapeutic target for androgen-dependent disease
Mol. Endocrinol.
20
444-458
2006
Homo sapiens (P52895), Homo sapiens
brenda
Yee, D.J.; Balsanek, V.; Bauman, D.R.; Penning, T.M.; Sames, D.
Fluorogenic metabolic probes for direct activity readout of redox enzymes: Selective measurement of human AKR1C2 in living cells
Proc. Natl. Acad. Sci. USA
103
13304-13309
2006
Homo sapiens
brenda
Couture, J.F.; de Jesus-Tran, K.P.; Roy, A.M.; Cantin, L.; Cote, P.L.; Legrand, P.; Luu-The, V.; Labrie, F.; Breton, R.
Comparison of crystal structures of human type 3 3alpha-hydroxysteroid dehydrogenase reveals an 'induced-fit' mechanism and a conserved basic motif involved in the binding of androgen
Protein Sci.
14
1485-1497
2005
Homo sapiens (P52895), 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
Skarydova, L.; Zivna, L.; Xiong, G.; Maser, E.; Wsol, V.
AKR1C3 as a potential target for the inhibitory effect of dietary flavonoids
Chem. Biol. Interact.
178
138-144
2009
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)
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
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
Milivojevic, V.; Feinn, R.; Kranzler, H.R.; Covault, J.
Variation in AKR1C3, which encodes the neuroactive steroid synthetic enzyme 3alpha-HSD type 2 (17beta-HSD type 5), moderates the subjective effects of alcohol
Psychopharmacology
231
3597-3608
2014
Homo sapiens (P42330)
brenda