Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
androstenedione + NADPH + H+
testosterone + NADP+
corticosterone + NADPH + H+
corticosterol + NADP+
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
-
-
-
?
1,2-dehydrocortisone + NADPH
1,2-dehydrocortisol + NADP+
-
-
-
-
r
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
11-dehydrocorticosterone + NADPH + H+
?
-
-
-
-
?
11-dehydrocorticosterone + NADPH + H+
corticosterone + NADP+
-
-
-
-
?
11-oxo-progesterone + NADPH + H+
11beta-hydroxyprogesterone + NADP+
-
-
-
-
r
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+
21-hydroxy-pregn-4-en-3,11,20-trione + NADPH
16alpha-methyl-1,2-dehydrocortisone + NADPH
16alpha-methyl-1,2-dehydrocortisol + NADP+
-
-
-
-
r
16alpha-methylcortisone + NADPH
16alpha-methylcortisol + NADP+
-
-
-
-
r
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADPH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NADP+
7beta-hydroxycholesterol + NADP+
7-oxocholesterol + NADPH
9alpha-fluorocortisone + NADPH
9alpha-fluorocortisol + NADP+
-
-
-
-
r
corticosterone + NAD+
11-dehydrocorticosterone + NADH + H+
A0A1B0GWP2
-
-
-
?
corticosterone + NADP+
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
11-dehydrocorticosterone + NADPH + H+
corticosterone + NADP+
?
-
-
-
-
?
corticosterone + NADPH + H+
?
-
-
-
-
?
corticosterone + NADPH + H+
corticosterol + NADP+
-
-
-
-
r
cortisol + NAD+
cortisone + NADH + H+
A0A1B0GWP2
-
-
-
?
cortisol + NADP+
cortisone + NADPH
-
-
-
-
?
cortisol + NADP+
cortisone + NADPH + H+
-
-
-
-
?
cortisone + NAD(P)H
cortisol + NAD(P)+
-
-
-
-
r
cortisone + NADH + H+
cortisol + NAD+
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
additional information
?
-
androstenedione + NADPH + H+
testosterone + NADP+
-
i.e. 4-androsten-17-ol-3-one
-
?
androstenedione + NADPH + H+
testosterone + NADP+
the two reactions 11beta-HSD1-dehydrogenase, EC 1.1.1146, and 17beta-HSD3, EC 1.1.1.64, which utilize NADPH are competing for NADPH from the same cofactor pool. 11beta-HSD1-dehydrogenase serves as a NADPH-regenerating system that is tightly coupled in regulating 17beta-HSD3 reaction synthesizing testosterone. A cycle can exist whereby the NADPH produced by 11beta-HSD1 dehydrogenase can drive the reductase activity of 17beta-HSD3 and the NADP+ produced by 17beta-HSD3 and other enzymes involved in testosterone biosynthesis can drive the dehydrogenase activity of 11beta-HSD1
i.e. 4-androsten-17beta-ol-3-one
-
?
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
-
-
-
-
?
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
-
-
-
-
r
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
-
predominantly a reductase in vivo
-
-
r
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
-
primarly a reductase in vivo
-
-
r
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
-
isozyme 11beta-HSD1
-
-
?
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
-
isozyme 11beta-HSD1, biological activation of the glucocorticoid
-
-
?
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+
21-hydroxy-pregn-4-en-3,11,20-trione + NADPH
-
in aldosterone-insensitive Pars Recta
-
-
r
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+
21-hydroxy-pregn-4-en-3,11,20-trione + NADPH
-
i.e. corticosterone, 5.5times higher affinity for 11-dehydrocorticosterone than for cortisone, 24times higher affinity of corticosterone to 11-dehydrogenase than of cortisol, predominant reductive activity
-
-
r
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADPH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NADP+
-
i.e. cortisone, 5.5 times lower affinity than for 11-dehydrocorticosterone
i.e. cortisol
-
r
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADPH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NADP+
-
i.e. cortisone, stable dehydrogenase activity, unstable oxidoreductase activity
i.e. cortisol
-
?
7beta-hydroxycholesterol + NADP+
7-oxocholesterol + NADPH
-
-
-
-
r
7beta-hydroxycholesterol + NADP+
7-oxocholesterol + NADPH
-
in lysates of HEK-293 cells expressing 11beta-HSD1, no oxidation in intact HEK293 cells expressing 11beta-HSD1
-
-
r
corticosterone + NADP+
11-dehydrocorticosterone + NADPH
-
-
-
-
?
corticosterone + NADP+
11-dehydrocorticosterone + NADPH
-
-
-
-
r
corticosterone + NADP+
11-dehydrocorticosterone + NADPH + H+
-
-
-
-
r
corticosterone + NADP+
11-dehydrocorticosterone + NADPH + H+
-
bidirectional in vitro, believed to predominantly function as an oxidoreductase in vivo
-
-
r
cortisone + NADPH + H+
cortisol + NADP+
-
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
-
isozyme 11beta-HSD1
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
-
isozyme 11beta-HSD1
-
-
r
cortisone + NADPH + H+
cortisol + NADP+
-
isozyme 11beta-HSD1 might play an important role in the metabolic syndrome
-
-
r
cortisone + NADPH + H+
cortisol + NADP+
-
isozyme 11beta-HSD1 prefers the reduction of cortisone
-
-
r
cortisone + NADPH + H+
cortisol + NADP+
-
isozyme 11beta-HSD1, biological activation of the glucocorticoid
-
-
?
additional information
?
-
-
effects of hypertension on cardiac steroid metabolism, overview
-
-
?
additional information
?
-
-
estradiol has a regulatory function on the isozymes in the liver, isozyme 11beta-HSD1 expression is about 30% reduced in castrated male rats, while expression of isozyme 11beta-HSD2 is increased, overview
-
-
?
additional information
?
-
-
isozyme 11beta-HSD1 and hexose-6-phosphate dehydrogenase are co-localized in the hepatic endoplasmic reticulum and act in close cooperation in generation of cofactors for each other, functional coupling, overview
-
-
?
additional information
?
-
-
isozyme 11beta-HSD1 is regulated by the pentose phosphate pathway flux, overview
-
-
?
additional information
?
-
-
the enzyme activates pro-glucocorticoid hormones in a tissue-specific manner
-
-
?
additional information
?
-
-
substrate specificity overview, DELTA4-3-ketones and 5alpha-hydrogen steroids are readily metabolized by the enzyme, 5beta-hydrogen steroids and DELTA4-3-ketones with certain large a-substituents are metabolized to a limited extent or not at all, halogen substitution in the 9alpha-position enhances the rate of reduction of 11-ketones but blocks the oxidation of the related 11beta-ols
-
-
?
additional information
?
-
-
in liver cells, isoform 11beta-HSD1 behaves as a primary reductase, while in Leydig cells it acts as a primary oxidase
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
androstenedione + NADPH + H+
testosterone + NADP+
the two reactions 11beta-HSD1-dehydrogenase, EC 1.1.1146, and 17beta-HSD3, EC 1.1.1.64, which utilize NADPH are competing for NADPH from the same cofactor pool. 11beta-HSD1-dehydrogenase serves as a NADPH-regenerating system that is tightly coupled in regulating 17beta-HSD3 reaction synthesizing testosterone. A cycle can exist whereby the NADPH produced by 11beta-HSD1 dehydrogenase can drive the reductase activity of 17beta-HSD3 and the NADP+ produced by 17beta-HSD3 and other enzymes involved in testosterone biosynthesis can drive the dehydrogenase activity of 11beta-HSD1
i.e. 4-androsten-17beta-ol-3-one
-
?
corticosterone + NADPH + H+
corticosterol + NADP+
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
-
-
-
?
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+
21-hydroxy-pregn-4-en-3,11,20-trione + NADPH
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADPH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NADP+
7beta-hydroxycholesterol + NADP+
7-oxocholesterol + NADPH
-
-
-
-
r
corticosterone + NAD+
11-dehydrocorticosterone + NADH + H+
A0A1B0GWP2
-
-
-
?
corticosterone + NADP+
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
11-dehydrocorticosterone + NADPH + H+
-
bidirectional in vitro, believed to predominantly function as an oxidoreductase in vivo
-
-
r
cortisol + NAD+
cortisone + NADH + H+
A0A1B0GWP2
-
-
-
?
cortisol + NADP+
cortisone + NADPH + H+
-
-
-
-
?
cortisone + NAD(P)H
cortisol + NAD(P)+
-
-
-
-
r
cortisone + NADH + H+
cortisol + NAD+
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
additional information
?
-
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
-
-
-
-
r
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
-
predominantly a reductase in vivo
-
-
r
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
-
primarly a reductase in vivo
-
-
r
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
-
isozyme 11beta-HSD1, biological activation of the glucocorticoid
-
-
?
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+
21-hydroxy-pregn-4-en-3,11,20-trione + NADPH
-
in aldosterone-insensitive Pars Recta
-
-
r
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+
21-hydroxy-pregn-4-en-3,11,20-trione + NADPH
-
i.e. corticosterone, 5.5times higher affinity for 11-dehydrocorticosterone than for cortisone, 24times higher affinity of corticosterone to 11-dehydrogenase than of cortisol, predominant reductive activity
-
-
r
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADPH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NADP+
-
i.e. cortisone, 5.5 times lower affinity than for 11-dehydrocorticosterone
i.e. cortisol
-
r
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADPH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NADP+
-
i.e. cortisone, stable dehydrogenase activity, unstable oxidoreductase activity
i.e. cortisol
-
?
corticosterone + NADP+
11-dehydrocorticosterone + NADPH
-
-
-
-
?
corticosterone + NADP+
11-dehydrocorticosterone + NADPH
-
-
-
-
r
cortisone + NADPH + H+
cortisol + NADP+
-
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
-
isozyme 11beta-HSD1 might play an important role in the metabolic syndrome
-
-
r
cortisone + NADPH + H+
cortisol + NADP+
-
isozyme 11beta-HSD1 prefers the reduction of cortisone
-
-
r
cortisone + NADPH + H+
cortisol + NADP+
-
isozyme 11beta-HSD1, biological activation of the glucocorticoid
-
-
?
additional information
?
-
-
effects of hypertension on cardiac steroid metabolism, overview
-
-
?
additional information
?
-
-
estradiol has a regulatory function on the isozymes in the liver, isozyme 11beta-HSD1 expression is about 30% reduced in castrated male rats, while expression of isozyme 11beta-HSD2 is increased, overview
-
-
?
additional information
?
-
-
isozyme 11beta-HSD1 and hexose-6-phosphate dehydrogenase are co-localized in the hepatic endoplasmic reticulum and act in close cooperation in generation of cofactors for each other, functional coupling, overview
-
-
?
additional information
?
-
-
isozyme 11beta-HSD1 is regulated by the pentose phosphate pathway flux, overview
-
-
?
additional information
?
-
-
the enzyme activates pro-glucocorticoid hormones in a tissue-specific manner
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(1E,4E)-1,5-bis(thiophen-2-yl) penta-1,4-dien-3-one
derivative of curcumin, IC50 value in intact cells 184 nM. Not inhibitory to isoform 11beta-HSD2 in kidney at 100 microM
(2S)-2-[[(E)-[(1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-3-(4-hydroxyphenyl)propanoic acid
-
(E)-5-((benzo[d]thiazol-2-ylimino)(methylthio)methylamino)-2-hydroxybenzoic acid
-
2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane
competitive. Also inhibitory to isoform 11beta-HSD2
2-hydroxy-5-[[(E)-[(5-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
2-hydroxy-5-[[(E)-[(5-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
2-hydroxy-5-[[(E)-[(6-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
2-hydroxy-5-[[(E)-[(6-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
2-hydroxy-5-[[(E)-[(7-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
2-hydroxy-5-[[(E)-[(7-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
5-[[(E)-[(5-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(5-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(5-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(6-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(6-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(6-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(7-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(7-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(7-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
curcumin
inhibitory against isoform 11beta-HSD1 in intact cells with IC50 value of 5.79 microM, competitive. Treatment with curcumin reduces serum glucose, cholesterol, triglyceride, low density lipoprotein levels in high-fat-diet-induced obese rats
(3beta)-3-hydroxyandrost-5-en-17-one
-
treatment of rats induces a shift from isoform 11beta-HSD1 to 11beta-HSD2 expression, increasing conversion from active to inactive glucocorticoids. Dehydroepiandrosterone likely modulates the transcription of 11beta-HSD2 in a phosphatidylinositol-3 kinase/Akt-dependent manner by increasing CCAAT/enhancer-binding protein beta mRNA and protein expression
(4R,7S)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methanoindazol-3-one
-
-
(4S,7R)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-2-(2'-methyl[1,1'-biphenyl]-3-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-2-(4-methylphenyl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-2-(pyridin-2-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-2-[2-(trifluoromethyl)phenyl]-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-2-[[2-(trifluoromethyl)phenyl]methyl]-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1-benzyl-2-(2,4-difluorophenyl)-7,8,8-trimethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1-benzyl-2-(2-fluorophenyl)-7,8,8-trimethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1-benzyl-7,8,8-trimethyl-2-phenyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1-ethyl-7,8,8-trimethyl-2-phenyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
11-oxoandrosterone
-
0.0021 mM, 50% inhibition of oxido-reductase reaction
11-oxoprogesterone
-
0.0095 mM, 50% inhibition of oxido-reductase reaction
11-oxotestosterone
-
0.018 mM, 50% inhibition of oxido-reductase reaction
11beta-hydroxyandrosterone
-
0.07 mM, 50% inhibition of dehydrogenase reaction
11beta-hydroxydehydroepiandrosterone
-
0.003 mM, 50% inhibition of dehydrogenase reaction
11beta-hydroxyprogesterone
-
0.0004 mM, 50% inhibition of dehydrogenase reaction
11beta-hydroxytestosterone
-
0.0017 mM, 50% inhibition of dehydrogenase reaction
2'-hydroxyflavanone
-
0.2 mM, more than 90% inhibition of 7-oxocholesterol reduction in liver homogenates
2-(2,4-difluorophenyl)-7,8,8-trimethyl-1-(2-phenylethyl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2,5-dichlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2,6-dichlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2-chlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2-fluorophenyl)-7,8,8-trimethyl-1-(prop-2-en-1-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2-fluorophenyl)-7,8,8-trimethyl-1-(propan-2-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2-fluorophenyl)-7,8,8-trimethyl-1-propyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(3-iodophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(3-methoxyphenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-benzyl-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-bis-(4-hydroxyphenyl)-1,1,1-trichloroethane
A0A1B0GWP2
-
3-methoxy-7,8,8-trimethyl-2-(4-methylphenyl)-4,5,6,7-tetrahydro-2H-4,7-methanoindazole
-
-
3-monoglucuronyl-glycyrrhetinic acid
A0A1B0GWP2
-
3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid
-
i.e. glycyrrhetinic acid; more effective for 11-dehydrogenase than for 11-oxoreductase activity
4-chloromercuribenzoate
-
complete inhibition of cortisol oxidation at 0.01 mM
9alpha-Fluorocortisol
-
a competitive inhibitor of the oxidation of cortisol
arylsulfoamidothiazole
-
-
arylsulfoamidothiazoles
-
weak or not binding binding inhibitors, inhibition mode and profiles
-
BDE-3
-
inhibitor of isoform HSD11B2
BDE-47
-
inhibitor of isoform HSD11B2
bisphenol A
A0A1B0GWP2
weak inhibition of isoform 11beta-HSD2, 41.61% inhibition at 0.1 mM
butylated hydroxyanisole
A0A1B0GWP2
highly selective inhibitor of isoform 11beta-HSD2
dexamethasone
-
dexmethasone inhibits 11beta-HSD1 activity and expression in a time- and concentration-dependent manner, the effect of dexamethasone is mimicked by both cortisol and corticosterone but blocked by the glucocorticoid receptor antagonist RU486
estradiol
-
50% inhibition, DTT protects at 10 mM, estradiol has a regulatory function on the isozymes in the liver
follicular fluid
-
follicular fluid from small antral follicles inhibits the enzyme in kidney homogenates by 50%, follicular fluid from large antral follicles inhibits by 23%, cyst fluid inhibits by 59%. Net cortisol oxidation in granulosa cells decreases by 35-48% when treated with follicular fluid from large antral follicles, and by 45-75% when treated with cyst fluid
-
glycyrrhizin
A0A1B0GWP2
-
NADP+
-
50% inhibition at 220 nmol
perfluorohexane sulfonate
A0A1B0GWP2
-
perfluorooctane sulfonate
A0A1B0GWP2
-
Perfluorooctanoic acid
A0A1B0GWP2
-
resveratrol
-
non-competitive inhibitor
zearalenone
A0A1B0GWP2
selective inhibitor of isoform 11beta-HSD2
carbenoxolone
-
0.01 mM, more than 90% inhibition of 7-oxocholesterol reduction in liver homogenates
carbenoxolone
-
unspecific inhibitor
testosterone
-
0.003 mM, 50% inhibition of oxido-reductase reaction
testosterone
-
0.02 mM, 50% inhibition of dehydrogenase reaction
additional information
-
isozyme 11beta-HSD1 expression is about 30% reduced in castrated male rats, while expression of isozyme 11beta-HSD2 is increased, overview
-
additional information
-
no inhibition of cortisol oxidation by 0,1 mM o-iodosobenzoate and 2alpha-methylcortisol
-
additional information
-
structure-activity analysis for inhibitor design
-
additional information
-
aldosterone, no effect
-
additional information
-
isoform HSD11B1 is not inhibited by 4-bromobiphenyl, BDE-3, BDE-47, BDE-100, and BDE-153
-
additional information
A0A1B0GWP2
not inhibited by perfluorobutane sulfonic acid
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Alfaidy, N.; Blot-Chabaud, M.; Robic, D.; Kenouch, S.; Bourbouze, R.; Bonvalet, J.P.; Farman, N.
Characteristics and regulation of 11beta-hydroxysteroid dehydrogenase of proximal and distal nephron
Biochim. Biophys. Acta
1243
461-468
1995
Rattus norvegicus
brenda
Monder, C.
The forms and functions of 11beta-hydroxysteroid dehydrogenase
J. Steroid Biochem. Mol. Biol.
45
161-165
1993
Rattus norvegicus
brenda
Hundertmark, S.; Ragosch, V.; Schein, B.; Buhler, H.; Fromm, M.; Lorenz, U.; Weitzel, H.K.
11-beta-Hydroxysteroid dehydrogenase of rat lung: Enzyme kinetic, oxidase-reductase ration, electrolyte and trace element dependence
Enzyme Protein
47
83-91
1993
Rattus norvegicus, Rattus sp.
brenda
Bush, I.E.; Hunter, S.A.; Meigs, R.A.
Metabolism of 11-oxogenated steroids. Metabolism in vitro by preparations of liver
Biochem. J.
107
239-258
1968
Bos taurus, Cavia porcellus, Oryctolagus cuniculus, Rattus norvegicus, Rattus sp.
brenda
Gomez-Sanchez, E.P.; Ganjam, V.; Chen, Y.J.; Liu, Y.; Zhou, M.Y.; Toroslu, C.; Romero, D.G.; Hughson, M.D.; de Rodriguez, A.; Gomez-Sanchez, C.E.
Regulation of 11beta-hydroxysteroid dehydrogenase enzymes in the rat kidney by estradiol
Am. J. Physiol.
285
E272-279
2003
Rattus norvegicus
brenda
Wang, G.M.; Ge, R.S.; Latif, S.A.; Morris, D.J.; Hardy, M.P.
Expression of 11beta-hydroxylase in rat Leydig cells
Endocrinology
143
621-626
2002
Rattus norvegicus
brenda
Waddell, B.J.; Hisheh, S.; Krozowski, Z.S.; Burton, P.J.
Localization of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in the male reproductive tract
Endocrinology
144
3101-3106
2003
Rattus norvegicus
brenda
Schweizer, R.A.; Zurcher, M.; Balazs, Z.; Dick, B.; Odermatt, A.
Rapid hepatic metabolism of 7-ketocholesterol by 11beta-hydroxysteroid dehydrogenase type 1: species-specific differences between the rat, human, and hamster enzyme
J. Biol. Chem.
279
18415-18424
2004
Homo sapiens, Rattus norvegicus, Mesocricetus auratus (Q6R0J2)
brenda
Nobel, C.S.I.; Dunas, F.; Abrahmsen, L.B.
Purification of full-length recombinant human and rat type 1 11beta-hydroxysteroid dehydrogenases with retained oxidoreductase activities
Protein Expr. Purif.
26
349-356
2002
Homo sapiens, Rattus norvegicus
brenda
Gomez-Sanchez, E.P.; Venkataseshu, G.; Chen, Y.J.; Liu, Y.; Zhou, M.Y.; Toroslu, C.; Romero, D.G.; Hughson, M.D.; de Rodriguez, A.; Gomez-Sanchez, C.E.
Regulation of 11beta-hydroxysteroid dehydrogenase enzymes in the rat kidney by estradiol
Am. J. Physiol. Endocrinol. Metab.
285
E272-E279
2003
Rattus norvegicus
brenda
Cherkasova, O.P.
Activity of 11beta-hydroxysteroid dehydrogenase in tissues of hypertensive NISAG rats
Bull. Exp. Biol. Med.
141
30-32
2006
Rattus norvegicus
brenda
McCormick, K.L.; Wang, X.; Mick, G.J.
Evidence that the 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD1) is regulated by pentose pathway flux. Studies in rat adipocytes and microsomes
J. Biol. Chem.
281
341-347
2006
Rattus norvegicus
brenda
Mazancova, K.; Kopecky, M.; Miksik, I.; Pacha, J.
11beta-Hydroxysteroid dehydrogenase in the heart of normotensive and hypertensive rats
J. Steroid Biochem. Mol. Biol.
94
273-277
2005
Rattus norvegicus
brenda
Czegle, I.; Piccirella, S.; Senesi, S.; Csala, M.; Mandl, J.; Banhegyi, G.; Fulceri, R.; Benedetti, A.
Cooperativity between 11beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase is based on a common pyridine nucleotide pool in the lumen of the endoplasmic reticulum
Mol. Cell. Endocrinol.
248
24-25
2006
Rattus norvegicus
brenda
Hult, M.; Shafqat, N.; Elleby, B.; Mitschke, D.; Svensson, S.; Forsgren, M.; Barf, T.; Vallgarda, J.; Abrahmsen, L.; Oppermann, U.
Active site variability of type 1 11beta-hydroxysteroid dehydrogenase revealed by selective inhibitors and cross-species comparisons
Mol. Cell. Endocrinol.
248
26-33
2006
Cavia porcellus, Mus musculus, Rattus norvegicus, Homo sapiens (P28845), Homo sapiens
brenda
Gomez-Sanchez, E.P.; Romero, D.G.; de Rodriguez, A.F.; Warden, M.P.; Krozowski, Z.; Gomez-Sanchez, C.E.
Hexose-6-phosphate dehydrogenase and 11beta-hydroxysteroid dehydrogenase-1 tissue distribution in the rat
Endocrinology
149
525-533
2008
Rattus norvegicus
brenda
Balazs, Z.; Schweizer, R.A.; Frey, F.J.; Rohner-Jeanrenaud, F.; Odermatt, A.
DHEA induces 11 -HSD2 by acting on CCAAT/enhancer-binding proteins
J. Am. Soc. Nephrol.
19
92-101
2008
Rattus norvegicus
brenda
Perrone, C.E.; Mattocks, D.A.; Hristopoulos, G.; Plummer, J.D.; Krajcik, R.A.; Orentreich, N.
Methionine restriction effects on 11 -HSD1 activity and lipogenic/lipolytic balance in F344 rat adipose tissue
J. Lipid Res.
49
12-23
2008
Rattus norvegicus
brenda
Marcolongo, P.; Piccirella, S.; Senesi, S.; Wunderlich, L.; Gerin, I.; Mandl, J.; Fulceri, R.; Banhegyi, G.; Benedetti, A.
The glucose-6-phosphate transporter-hexose-6-phosphate dehydrogenase-11beta-hydroxysteroid dehydrogenase type 1 system of the adipose tissue
Endocrinology
148
2487-2495
2007
Rattus norvegicus
brenda
London, E.; Lala, G.; Berger, R.; Panzenbeck, A.; Kohli, A.A.; Renner, M.; Jackson, A.; Raynor, T.; Loya, K.; Castonguay, T.W.
Sucrose access differentially modifies 11beta-hydroxysteroid dehydrogenase-1 and hexose-6-phosphate dehydrogenase message in liver and adipose tissue in rats
J. Nutr.
137
2616-2621
2007
Rattus norvegicus
brenda
Sunak, N.; Green, D.F.; Abeydeera, L.R.; Thurston, L.M.; Michael, A.E.
Implication of cortisol and 11beta -hydroxysteroid dehydrogenase enzymes in the development of porcine (Sus scrofa domestica) ovarian follicles and cysts
Reproduction
133
1149-1158
2007
Rattus norvegicus, Sus scrofa
brenda
Czegle, I.; Margittai, E.; Senesi, S.; Benedetti, A.; Banhegyi, G.
Different expression and distribution of 11beta-hydroxysteroid dehydrogenase type 1 in obese and lean animal models of type 2 diabetes
Acta Physiol. Hung.
95
419-424
2008
Rattus norvegicus
brenda
Balachandran, A.; Guan, H.; Sellan, M.; van Uum, S.; Yang, K.
Insulin and dexamethasone dynamically regulate adipocyte 11beta-hydroxysteroid dehydrogenase type 1
Endocrinology
149
4069-4079
2008
Mus musculus, Rattus norvegicus
brenda
Chen, B.B.; Lin, H.; Hu, G.X.; Su, Y.; Zhou, H.Y.; Lian, Q.Q.; Cai, H.; Hardy, D.O.; Gu, D.Y.; Ge, R.S.
The (+)- and (-)-gossypols potently inhibit human and rat 11beta-hydroxysteroid dehydrogenase type 2
J. Steroid Biochem. Mol. Biol.
113
177-181
2009
Homo sapiens, Rattus norvegicus
brenda
Gong, R.; Morris, D.J.; Brem, A.S.
Variable expression of 11beta Hydroxysteroid dehydrogenase (11beta-HSD) isoforms in vascular endothelial cells
Steroids
73
1187-1196
2008
Homo sapiens, Homo sapiens (P80365), Rattus norvegicus
brenda
Tagawa, N.; Yuda, R.; Kubota, S.; Wakabayashi, M.; Yamaguchi, Y.; Kiyonaga, D.; Mori, N.; Minamitani, E.; Masuzaki, H.; Kobayashi, Y.
17Beta-estradiol inhibits 11beta-hydroxysteroid dehydrogenase type 1 activity in rodent adipocytes
J. Endocrinol.
202
131-139
2009
Mus musculus, Rattus norvegicus
brenda
Hu, G.; Lin, H.; Lian, Q.; Zhou, S.; Guo, J.; Zhou, H.; Chu, Y.; Ge, R.
Curcumin as a potent and selective inhibitor of 11beta-hydroxysteroid dehydrogenase 1: improving lipid profiles in high-fat-diet-treated rats
PLoS ONE
8
e49976
2013
Rattus norvegicus (P16232), Homo sapiens (P28845)
brenda
Latif, S.A.; Shen, M.; Ge, R.S.; Sottas, C.M.; Hardy, M.P.; Morris, D.J.
Role of 11beta-OH-C(19) and C(21) steroids in the coupling of 11beta-HSD1 and 17beta-HSD3 in regulation of testosterone biosynthesis in rat Leydig cells
Steroids
76
682-689
2011
Rattus norvegicus (P16232)
brenda
Guo, J.; Deng, H.; Li, H.; Zhu, Q.; Zhao, B.; Chen, B.; Chu, Y.; Ge, R.S.
Effects of methoxychlor and its metabolite 2,2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane on 11beta-hydroxysteroid dehydrogenase activities in vitro
Toxicol. Lett.
218
18-23
2013
Homo sapiens (P28845), Rattus norvegicus (P16232)
brenda
Gillespie, P.; Pietranico-Cole, S.; Myers, M.; Bilotta, J.A.; Conde-Knape, K.; Fotouhi, N.; Goodnow, R.A.; Guertin, K.R.; Hamilton, M.M.; Haynes, N.E.; Liu, B.; Qi, L.; Ren, Y.; Scott, N.R.; So, S.S.; Spence, C.; Taub, R.; Thakkar, K.; Tilley, J.W.; Zwingelstein, C.
Discovery of camphor-derived pyrazolones as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
Bioorg. Med. Chem. Lett.
24
2707-2711
2014
Rattus norvegicus
brenda
Cherkasova, O.P.; Selyatitskaya, V.G.; Palchikova, N.A.; Kuznetsova, N.V.
Activity of 11beta-hydroxysteroid dehydrogenase in the adrenal glands, liver, and kidneys of rats with experimental diabetes
Bull. Exp. Biol. Med.
158
185-187
2014
Rattus norvegicus
brenda
Tagawa, N.; Kubota, S.; Kato, I.; Kobayashi, Y.
Resveratrol inhibits 11beta-hydroxysteroid dehydrogenase type 1 activity in rat adipose microsomes
J. Endocrinol.
218
311-320
2013
Rattus norvegicus
brenda
Chen, X.; Dong, Y.; Cao, S.; Li, X.; Wang, Z.; Chen, R.; Ge, R.S.
Effects of polybrominated diphenyl ethers on rat and human 11beta-hydroxysteroid dehydrogenase 1 and 2 activities
Pharmacology
98
115-123
2016
Homo sapiens, Rattus norvegicus
brenda
Ergang, P.; Kuzelova, A.; Sotak, M.; Klusonova, P.; Makal, J.; Pacha, J.
Distinct effect of stress on 11beta-hydroxysteroid dehydrogenase type 1 and corticosteroid receptors in dorsal and ventral hippocampus
Physiol. Res.
63
255-261
2014
Rattus norvegicus
brenda
Li, X.; Hu, G.; Li, X.; Wang, Y.Y.; Hu, Y.Y.; Zhou, H.; Latif, S.A.; Morris, D.J.; Chu, Y.; Zheng, Z.; Ge, R.S.
Metabolic coupling determines the activity: comparison of 11beta-hydroxysteroid dehydrogenase 1 and its coupling between liver parenchymal cells and testicular Leydig cells
PLoS ONE
10
e0141767
2015
Rattus norvegicus, Homo sapiens (P28845), Homo sapiens
brenda
Zhou, C.; Ye, F.; Wu, H.; Ye, H.; Chen, Q.
Recent advances in the study of 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) inhibitors
Environ. Toxicol. Pharmacol.
52
47-53
2017
Rattus norvegicus (A0A1B0GWP2), Homo sapiens (P80365)
brenda
Cabrera Perez, L.C.; Padilla-Martinez, I.I.; Cruz, A.; Correa Basurto, J.; Miliar Garcia, A.; Hernandez Zavala, A.A.; Gomez Lopez, M.; Rosales Hernandez, M.C.
Design, synthesis, molecular docking and in vitro evaluation of benzothiazole derivatives as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
Mol. Divers.
24
971-984
2020
Rattus norvegicus (P16232)
brenda
Inderbinen, S.G.; Zogg, M.; Kley, M.; Smiesko, M.; Odermatt, A.
Species-specific differences in the inhibition of 11beta-hydroxysteroid dehydrogenase 2 by itraconazole and posaconazole
Toxicol. Appl. Pharmacol.
412
115387
2021
Rattus norvegicus (P50233), Mus musculus (P51661), Homo sapiens (P80365), Danio rerio (Q6P0H9)
brenda