Any feedback?
Information on EC 1.1.1.B40 - 11beta-hydroxysteroid dehydrogenase (NAD+) and Organism(s) Homo sapiens
for references in articles please use BRENDA:EC1.1.1.B40preliminary BRENDA-supplied EC number
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
EC Tree
1.1.1.B40 11beta-hydroxysteroid dehydrogenase (NAD+)Specify your search results
Word Map
- 1.1.1.B40
- glucocorticoid
-
mineralocorticoid
- cortisone
- aldosterone
- hypertension
- adrenal
- 11-dehydrocorticosterone
- dexamethasone
- urinary
- fetal
- carbenoxolone
-
glycyrrhetinic
- 11beta-hsds
-
beta-hsd1
- nadp
- acth
- renin
- hypokalemia
- spironolactone
- tetrahydrocortisol
-
cortisol-cortisone
-
liquorice
- thf
-
adrenalectomized
-
cushing
-
11-keto
-
beta-reductase
-
glycyrrhizic
-
hypopituitary
- medicine
-
3hcorticosterone
-
prereceptor
- pharmacology
-
11-beta-hydroxysteroid
-
feto-placental
-
low-renin
- drug development
-
11-dehydro
-
oxo-reductase
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
The enzyme appears in selected viruses and cellular organisms
Synonyms
11 beta-hydroxysteroid dehydrogenase, 11 beta-hydroxysteroid dehydrogenase type 2, 11beta-hsd type 2, 11beta-ohsd, 11beta-hsd 2, 11-beta hydroxysteroid dehydrogenase type 2, type 2 11beta-hydroxysteroid dehydrogenase, 11beta hydroxysteroid dehydrogenase type 2, 11beta-hydroxysteroid dehydrogenase type-2, nad(+)-dependent 11beta-dehydrogenase, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
11beta-HSD2
11beta-hydroxysteroid dehydrogenase 2
-
-
11beta-hydroxysteroid dehydrogenase type 2
11beta-HSD2
-
-
11beta-hydroxysteroid dehydrogenase type 2
-
-
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
an 11beta-hydroxysteroid + NAD+ = an 11-oxosteroid + NADH + H+
the three-dimensional organization of the hydrophobic substrate binding pocket is responsible for species-specific variability of activity with different substrates, overview
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SYSTEMATIC NAME
IUBMB Comments
11beta-hydroxysteroid:NAD+ 11-oxidoreductase
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
11-dehydrocorticosterone + beta-NADPH
corticosterone + beta-NADP+
low activity
-
-
r
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
isozyme 11beta-HSD1
-
-
?
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NAD+
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADH
-
i.e. cortisol
i.e. cortisone
-
r
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+
21-hydroxy-pregn-4-en-3,11,20-trione + NADH
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+
21-hydroxy-pregn-4-en-3,11,20-trione + NADH + H+
-
i.e. corticosterone
-
ir
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NAD+
7-oxocholesterol + NADPH + H+
7beta-hydroxycholesterol + NADP+
isozyme 11beta-HSD1, stereospecific reaction
-
-
?
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+
21-hydroxy-pregn-4-en-3,11,20-trione + NADH
-
i.e. corticosterone
-
-
r
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+
21-hydroxy-pregn-4-en-3,11,20-trione + NADH
-
i.e. corticosterone, clear but not exclusive preference for NAD+, only oxidative activity
-
-
ir
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+
21-hydroxy-pregn-4-en-3,11,20-trione + NADH
-
i.e. corticosterone, significant higher rate of conversion for 11-beta-HSD2 than for 11-beta-HSD1
-
-
ir
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NAD+
-
i.e. cortisone
i.e. cortisol
ir
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NAD+
-
important role in modulating mineralocorticoid and glucocorticoid receptor occupancy by glucocorticoids
i.e. cortisol
ir
cortisol + NAD+
cortisone + NADH
-
oxidase that inactivates glucocorticoids to their 11-oxo derivatives
-
-
?
cortisol + NAD+
cortisone + NADH
-
inactivation of the biologically active glucocorticoid
-
-
r
cortisol + NAD+
cortisone + NADH
-
isozyme 11beta-HSD2 catalyzes the oxidative reaction with cofactor NAD+
-
-
ir
cortisol + NAD+
cortisone + NADH
-
isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+
-
-
ir
cortisol + NAD+
cortisone + NADH
isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+
-
-
ir
cortisol + NAD+
cortisone + NADH
isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+
-
-
ir
cortisol + NAD+
cortisone + NADH
-
isozyme 11beta-HSD2, inactivation of cortisol, which interacts with the mineralocorticoid receptor, isozyme 11beta-HSD2 inhibition leads to stimulation of sodium and water reabsorption and to an increase of the intravascular volume that suppresses renin and secondarily an increase of blood pressure
-
-
?
cortisol + NAD+
cortisone + NADH
-
isozyme 11beta-HSD2 catalyzes the reverse reaction 11beta-HSD1 with cofactor NAD+
-
-
ir
cortisol + NAD+
cortisone + NADH
-
isozyme 11beta-HSD2 catalyzes the reverse reaction of 11-beta-HSD1 with cofactor NAD+
-
-
ir
cortisone + NADPH + H+
cortisol + NADP+
isozyme 11beta-HSD1, activation
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
isozyme 11beta-HSD1, preferred substrate, high activity
-
-
r
dexamethasone + NAD+
11-dehydromethasone + NADH
-
isoform 11beta-HSD2
-
ir
dexamethasone + NAD+
11-dehydromethasone + NADH
-
isoform 11-beta-HSD2 shows significantly higher rate of conversion than isoform 11-betaHSD1
-
-
ir
additional information
?
-
-
enzyme inhibition affects the glucocorticoid- and dexamethasone-mediated regulation of surfactant protein A metabolism, overview
-
-
?
additional information
?
-
-
proinflammatory cytokines inhibit placental isozyme 11beta-HSD2 activity through Ca2+ and cAMP pathways, overview
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
isozyme 11beta-HSD1
-
-
?
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NAD+
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADH
-
i.e. cortisol
i.e. cortisone
-
r
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+
21-hydroxy-pregn-4-en-3,11,20-trione + NADH
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+
21-hydroxy-pregn-4-en-3,11,20-trione + NADH + H+
-
i.e. corticosterone
-
ir
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NAD+
cortisone + NADPH + H+
cortisol + NADP+
isozyme 11beta-HSD1, activation
-
-
?
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+
21-hydroxy-pregn-4-en-3,11,20-trione + NADH
-
i.e. corticosterone
-
-
r
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+
21-hydroxy-pregn-4-en-3,11,20-trione + NADH
-
i.e. corticosterone, clear but not exclusive preference for NAD+, only oxidative activity
-
-
ir
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+
21-hydroxy-pregn-4-en-3,11,20-trione + NADH
-
i.e. corticosterone, significant higher rate of conversion for 11-beta-HSD2 than for 11-beta-HSD1
-
-
ir
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NAD+
-
i.e. cortisone
i.e. cortisol
ir
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NAD+
-
important role in modulating mineralocorticoid and glucocorticoid receptor occupancy by glucocorticoids
i.e. cortisol
ir
cortisol + NAD+
cortisone + NADH
-
oxidase that inactivates glucocorticoids to their 11-oxo derivatives
-
-
?
cortisol + NAD+
cortisone + NADH
-
inactivation of the biologically active glucocorticoid
-
-
r
cortisol + NAD+
cortisone + NADH
-
isozyme 11beta-HSD2 catalyzes the oxidative reaction with cofactor NAD+
-
-
ir
cortisol + NAD+
cortisone + NADH
-
isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+
-
-
ir
cortisol + NAD+
cortisone + NADH
isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+
-
-
ir
cortisol + NAD+
cortisone + NADH
-
isozyme 11beta-HSD2, inactivation of cortisol, which interacts with the mineralocorticoid receptor, isozyme 11beta-HSD2 inhibition leads to stimulation of sodium and water reabsorption and to an increase of the intravascular volume that suppresses renin and secondarily an increase of blood pressure
-
-
?
cortisol + NAD+
cortisone + NADH
-
isozyme 11beta-HSD2 catalyzes the reverse reaction 11beta-HSD1 with cofactor NAD+
-
-
ir
cortisol + NAD+
cortisone + NADH
-
isozyme 11beta-HSD2 catalyzes the reverse reaction of 11-beta-HSD1 with cofactor NAD+
-
-
ir
additional information
?
-
-
enzyme inhibition affects the glucocorticoid- and dexamethasone-mediated regulation of surfactant protein A metabolism, overview
-
-
?
additional information
?
-
-
proinflammatory cytokines inhibit placental isozyme 11beta-HSD2 activity through Ca2+ and cAMP pathways, overview
-
-
?
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1S,2R,3S,5R,6R)-4-methylidene-1-([(1S,4aS,8aS)-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]heptane-2,3,5-triol
-
-
(1S,2R,5R,6R)-4-(hydroxymethyl)-1-([(1S,4aR,6S,8aR)-6-hydroxy-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]hept-3-ene-2,5-diol
-
-
(1S,2R,5R,6R)-4-(hydroxymethyl)-1-([(1S,4aS,8aS)-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]hept-3-ene-2,5-diol
-
-
(2E,4S)-4-hydroxy-5-[(1S,5S,6S)-6-(hydroxymethyl)-2-methylidenebicyclo[3.1.1]hept-6-yl]-2-methylpent-2-enoic acid
-
-
(3alpha,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
-
-
(3beta)-3-hydroxy-18,29-epoxyolean-12-ene-11,29-dione
IC50 value for isoform 11beta-HSD2 above 25 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(3beta)-3-[(3-carboxypropanoyl)oxy]urs-12-en-28-oic acid
IC50 value for isoform 11beta-HSD2 above 3 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(3beta)-30-[hydroxy(methyl)amino]-11,30-dioxoolean-12-en-3-yl acetate
IC50 value for isoform 11beta-HSD1 above 1 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(3beta,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
-
-
(3beta,18beta,20beta)-3-(2-carboxy-ethylsulfonylamino)-11-oxoolean-12-en-29-oic acid
-
-
(3beta,18beta,20beta)-3-(2-methoxycarbonyl-ethylsulfonylamino)-11-oxo-olean-12-en-29-oic acid
-
-
(3beta,18beta,20beta)-3-acetoxy-N-methyl-N-hydroxy-11-oxoolean-12-en-29-amide
-
-
(3beta,18beta,20beta)-3-acetylamino-N-hydroxy-N-methyl-11-oxoolean-12-en-29-amide
-
-
(3beta,18beta,20beta)-3-amino-11-oxoolean-12-en-29-oic acid, diphenylmethyl ester
-
-
(3beta,18beta,20beta)-N-hydroxy-N-methyl-11-oxo-3-[(trifluoromethylsulfonyl)amino]-olean-12-en-29-amide
-
-
(3beta,18beta,20beta)-N-hydroxy-N-methyl-3-methoxyamino-11-oxo-olean-12-en-29-amide
-
-
(3S,4aR,6aR,6bS,8aS,11S,12aR,14aR,14bS)-4,4,6a,6b,8a,11,14b-heptamethyl-11-[(methylsulfonyl)amino]-14-oxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,14,14a,14b-icosahydropicen-3-yl acetate
IC50 value for isoform 11beta-HSD1 above 40 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(4aS,5R,8aR)-5,6-bis(hydroxymethyl)-1,1,4a-trimethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol
-
-
(4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol
-
-
(4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-3,4,4a,5,8,8a-hexahydronaphthalen-2(1H)-one
-
-
11beta,21-dihydroxypregn-4-en-3,20-dione
-
11-beta-HSD2, 50% inhibition at 0.00001 mM
17beta-estradiol
-
decrease in isoform HSD2 protein in male, but not female, fetal lung explant
18beta-glycyrrhetinic acid
-
inhibits both 11beta-HSD1 and 11beta-HSD2, but preferentially inhibits 11beta-HSD2
3-((3r,5r,7r)-adamantan-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
isozyme 11beta-HSD1 IC50: 74 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(3,4,7-trimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
isozyme 11beta-HSD1 IC50: 180 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(3,4-dimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
isozyme 11beta-HSD1 IC50: 13 nM, isozyme 11beta-HSD2 IC50: 0.00255 mM
3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
isozyme 11beta-HSD1 IC50: 36 nM, isozyme 11beta-HSD2 IC50: 0.0176 mM
3-(3-bromotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
isozyme 11beta-HSD1 IC50: 23 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(3-fluorotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
isozyme 11beta-HSD1 IC50: 37 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(3-phenyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
isozyme 11beta-HSD1 IC50: 2.3 nM, isozyme 11beta-HSD2 IC50: 23 nM
3-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)tricyclo[3.3.1.13,7]decan-1-ol
isozyme 11beta-HSD1 IC50: 739 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
isozyme 11beta-HSD1 IC50: 7.8 nM, isozyme 11beta-HSD2 IC50: above 0.003 mM
3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
isozyme 11beta-HSD1 IC50: 7.7 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate
-
IC50 in the presence of NADP+: 0.12 mM, IC50 in the presence of NAD+: 5.6 mM; i.e. CHAPS
4-nonylphenol
-
inhibition of liver isozyme 11beta-HSD1 and kidney isozyme 11beta-HSD2, 11beta-HSD1 IC50: 49.3 mM, isozyme 11beta-HSD2 IC50: 0.0203 mM
adamantyl triazoles
eight derivatives of different ring size, IC50 of 1.4-2180 nM for isozyme 11beta-HSD1, and of 8.7-2000 nM for isozyme 11beta-HSD2, the IC50 value decreases with increasing ring size, overview
-
BVT-14225
-
isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2
Cd2+
the ERK1/2 inhibitor U0126 can block cadmium-induced inhibition of placental 11beta-HSD2. Cadmium does not alter activities of p38 MAPK, JNK, or PI3 kinase. Cadmium specifically activates the ERK1/2 signaling pathway in human trophoblast cells
curcumin
inhibitory against isoform 11beta-HSD2 in intact cells with IC50 value of 14.56 microM
interleukin-1beta
-
inhibits isozyme 11beta-HSD2, forskolin acts antagonistically strongly
-
interleukin-1beta or tissue necrosis factor-alpha simultaneously increase 11beta-HSD1 expression and down-regulate 11beta-HSD2
-
-
-
mono (2-ethylhexyl) phthalate
-
competitive inhibitor of 11beta-HSD2, possibly via competing with the cofactor NAD+
n-alkyl-substituted adamantyl triazoles
substituted with methyl to butyl groups, IC50: of 3-72 nM for isozyme 11beta-HSD1, and of about 0.004 mM for isozyme 11beta-HSD2, overview
-
sterenin A
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
sterenin B
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
sterenin C
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
sterenin D
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid
-
IC50 in the presence of NAD+: 0.000097 mM, IC50 in the presence of NADP+: 0.0003 mM; i.e. glycyrrhetinic acid
3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid
-
i.e. glycyrrhetinic acid; potent inhibition
dicyclohexyl phthalate
-
inhibition of kidney isozyme 11beta-HSD2, IC50: 0.0465 mM
additional information
-
inhibitory effects, antogonistic and agonistic effects of inhibitors and compounds, overview, no inhibition of isozyme 11beta-HSD2 by 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate
-
additional information
inhibitory effects in intact cells and IC50 values, overview, structure-based pharmacophore models for isozyme 11beta-HSD1 inhibitors using crystal structure 1XU7, 1XU9, and 2 BEL
-
additional information
inhibitory effects in intact cells and IC50 values, overview, structure-based pharmacophore models for isozyme 11beta-HSD1 inhibitors using crystal structure 1XU7, 1XU9, and 2 BEL
-
additional information
-
no effect on isoform HSD2 protein level: 5alpha-dihydrotestosterone
-
additional information
-
not inhibited by dimethyl phthalate, butylbenzyl phthalate, di(2-ethylhexyl) phthalate, di-n-heptyl phthalate, diisononyl phthalate, and diisodecyl phthalate
-
additional information
-
18alpha-glycyrrhetinic acid, selective inhibition of 11beta-HSD1, does not inhibit 11beta-HSD2 at concentrations up to 0.02 mM
-
additional information
the JNK inhibitor SP600125 has no effect on 11beta-HSD2 enzyme activity
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
dexamethasone
-
after application of dexamethasone, 11beta-HSD1 mRNA increases in muscle of both diabetic and control subjects, whereas 11beta-HSD2 mRNA decreases. 11beta-HSD1 activity increases in diabetic subjects, but not in controls, whereas 11beta-HSD2 activity does not change in either group
prostaglandin E2
-
stimulation of progesterone production and of 11beta-hydroxysteroid dehydrogenase activity via the prostaglandin E receptor 2-cAMP signalling pathway in luteinizing granulosa cells
additional information
-
interleukin-1beta or tissue necrosis factor-alpha simultaneously increase 11beta-HSD1 expression and down-regulate 11beta-HSD2
-
additional information
the JNK inhibitor SP600125 has no effect on 11beta-HSD2 enzyme activity
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00042
11-Dehydrocorticosterone
pH 7.4, 37°C, recombinant isozyme 11beta-HSD1
0.00089
17,21-dihydroxy-pregn-4-ene-3,11,20-trione
-
i.e. cortisone, temperature not specified in the publication, pH 5.5-6
0.0022
21-hydroxy-pregn-4-en-3,11,20-trione
-
temperature not specified in the publication, pH 5.5-6
0.0014
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione
-
i.e. cortisol, temperature not specified in the publication, pH 5.5-6
0.000084
11beta,21-dihydroxypregn-4-en-3,20-dione
-
temperature not specified in the publication, pH 5.5-6
0.0000044
NAD+
-
reduction of corticosterone, pH and temperature not specified in the publication
0.0000102
NAD+
-
kidney homogenate, pH and temperature not specified in the publication
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0049
2'-hydroxyflavanone
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of 11-dehydrocorticosterone reduction
0.017
2'-hydroxyflavanone
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of cortisone reduction
0.2
2'-hydroxyflavanone
above, pH 7.4, 37°C, isozyme 11beta-HSD2, inhibition of cortisol oxidation
0.0039
abietic acid
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of cortisone reduction
0.007
abietic acid
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of 11-dehydrocorticosterone reduction
0.011
abietic acid
pH 7.4, 37°C, isozyme 11beta-HSD2, inhibition of cortisol oxidation
0.00023
carbenoxolone
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of 11-dehydrocorticosterone reduction
0.00034
carbenoxolone
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of cortisone reduction
0.00059
carbenoxolone
pH 7.4, 37°C, isozyme 11beta-HSD2, inhibition of cortisol oxidation
0.0021
chenodeoxycholic acid
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of 11-dehydrocorticosterone reduction
0.003
chenodeoxycholic acid
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of cortisone reduction
0.02
chenodeoxycholic acid
pH 7.4, 37°C, isozyme 11beta-HSD2, inhibition of cortisol oxidation
0.015
flavanone
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of cortisone reduction
0.031
flavanone
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of 11-dehydrocorticosterone reduction
0.2
flavanone
above, pH 7.4, 37°C, isozyme 11beta-HSD2, inhibition of cortisol oxidation
0.000028
glycyrrhetinic acid
pH 7.4, 37°C, isozyme 11beta-HSD2, inhibition of cortisol oxidation
0.00029
glycyrrhetinic acid
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of cortisone reduction
0.0003
glycyrrhetinic acid
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of 11-dehydrocorticosterone reduction
0.000015
T0504
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of cortisone reduction
0.000025
T0504
pH 7.4, 37°C, isozyme 11beta-HSD1, inhibition of 11-dehydrocorticosterone reduction
0.0018
T0504
pH 7.4, 37°C, isozyme 11beta-HSD2, inhibition of cortisol oxidation
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0000049
(3alpha,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
Homo sapiens
-
pH not specified in the publication, 37°C
0.00075
(3beta)-3-(acetyloxy)-11-oxoolean-12-en-30-oic acid
Homo sapiens
-
pH not specified in the publication, 37°C
0.0000029
(3beta)-30-[hydroxy(methyl)amino]-11,30-dioxoolean-12-en-3-yl acetate
Homo sapiens
pH 7.4, 37°C
0.000122
(3beta)-N,3-dihydroxy-11-oxoolean-12-en-30-amide
Homo sapiens
-
pH not specified in the publication, 37°C
0.000458
(3beta,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oic acid
Homo sapiens
-
pH not specified in the publication, 37°C
0.0000611
(3beta,18beta,20beta)-3-acetoxy-N-hydroxy-11-oxo-olean-12-en-29-amide
Homo sapiens
-
pH not specified in the publication, 37°C
0.0000029
(3beta,18beta,20beta)-3-acetoxy-N-methyl-N-hydroxy-11-oxoolean-12-en-29-amide
Homo sapiens
-
pH not specified in the publication, 37°C
0.00213
(3beta,18beta,20beta)-3-hydroxy-N-methoxy-11-oxo-olean-12-en-29-amide
Homo sapiens
-
pH not specified in the publication, 37°C
0.0000145
(3beta,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
Homo sapiens
-
pH not specified in the publication, 37°C
0.000268
(3E)-3-(methoxyimino)-11-oxoolean-12-en-30-oic acid
Homo sapiens
-
pH not specified in the publication, 37°C
0.0000069
(3S,4aR,6aR,6bS,8aS,11S,12aR,14aR,14bS)-4,4,6a,6b,8a,11,14b-heptamethyl-11-[(methylsulfonyl)amino]-14-oxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,14,14a,14b-icosahydropicen-3-yl acetate
Homo sapiens
pH 7.4, 37°C
0.000061
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione
Homo sapiens
-
i.e. cortisol, pH and temperature not specified in the publication
0.0000051
11beta,21-dihydroxypregn-4-en-3,20-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.000329
3,11-dioxoolean-12-en-30-oic acid
Homo sapiens
-
pH not specified in the publication, 37°C
5.6
3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate
Homo sapiens
-
pH and temperature not specified in the publication
0.000097
3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0465
dicyclohexyl phthalate
Homo sapiens
-
inhibition of kidney isozyme 11beta-HSD2, pH 7.4, 37°C
0.00000071
glycyrrhizinic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00000071
glycyrrhizininc acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
additional information
(1S,2R,3S,5R,6R)-4-methylidene-1-([(1S,4aS,8aS)-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]heptane-2,3,5-triol
0.0000024
glycyrrhetinic acid
Homo sapiens
-
cell-based assay, pH not specified in the publication, temperature not specified in the publication
additional information
(1S,2R,3S,5R,6R)-4-methylidene-1-([(1S,4aS,8aS)-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]heptane-2,3,5-triol
Homo sapiens
-
IC50 = 0.0254 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(1S,2R,5R,6R)-4-(hydroxymethyl)-1-([(1S,4aR,6S,8aR)-6-hydroxy-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]hept-3-ene-2,5-diol
Homo sapiens
-
IC50 above 0.1 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(1S,2R,5R,6R)-4-(hydroxymethyl)-1-([(1S,4aS,8aS)-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]hept-3-ene-2,5-diol
Homo sapiens
-
IC50 = 0.0015 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(2E,4S)-4-hydroxy-5-[(1S,5S,6S)-6-(hydroxymethyl)-2-methylidenebicyclo[3.1.1]hept-6-yl]-2-methylpent-2-enoic acid
Homo sapiens
-
IC50 = 0.0106 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(2S)-5-(acetyloxy)-2-hydroxypentyl acetate
Homo sapiens
-
IC50 = 0.177 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(3alpha,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
Homo sapiens
-
50% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3alpha,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oicacid
Homo sapiens
-
4% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3alpha,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
Homo sapiens
-
4% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta)-3-hydroxy-11-oxoolean-12-en-30-amide
Homo sapiens
-
13% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-11-oxo-3-succinylamino-olean-12-en-29-oic acid
Homo sapiens
-
13% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
Homo sapiens
-
22% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3,N-dihydroxy-N-methyl-11-oxo-olean-12-en-29-amide
Homo sapiens
-
7% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-(2-carboxy-ethylsulfonylamino)-11-oxoolean-12-en-29-oic acid
Homo sapiens
-
40% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-(2-methoxycarbonyl-ethylsulfonylamino)-11-oxo-olean-12-en-29-oic acid
Homo sapiens
-
3% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-acetoxy-N-methoxy-11-oxo-olean-12-en-29-amide
Homo sapiens
-
36% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-acetylamino-N-hydroxy-N-methyl-11-oxoolean-12-en-29-amide
Homo sapiens
-
4% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-amino-11-oxoolean-12-en-29-oic acid, diphenylmethyl ester
Homo sapiens
-
42% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
Homo sapiens
-
4% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-N-hydroxy-N-methyl-11-oxo-3-[(trifluoromethylsulfonyl)amino]-olean-12-en-29-amide
Homo sapiens
-
44% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-N-hydroxy-N-methyl-3-methoxyamino-11-oxo-olean-12-en-29-amide
Homo sapiens
-
30% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(4aS,5R,8aR)-5,6-bis(hydroxymethyl)-1,1,4a-trimethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol
Homo sapiens
-
IC50 = 0.177 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol
Homo sapiens
-
IC50 = 0.22 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-3,4,4a,5,8,8a-hexahydronaphthalen-2(1H)-one
Homo sapiens
-
IC50 = 0.2 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
2-oxopentane-1,5-diyl diacetate
Homo sapiens
-
IC50 = 0.0051 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
5-hydroxy-4-oxopentyl acetate
Homo sapiens
-
IC50 = 0.0389 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
BVT-14225
Homo sapiens
-
isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2
additional information
carbenoxolone
Homo sapiens
-
2% residual activity at 0,001 mM, pH not specified in the publication, 37°C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
determination of activity of isozyme 11beta-HSD2 in ovarian cancer, overview
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
expression and activity of isozyme 11beta-HSD2 in probes of seven different women with ovarian cancer of different types, overview
-
at baseline, mRNA levels are similar in diabetic and control sugjects for 11beta-HSD1, 11beta-HSD2, and hexose-6-phosphate dehydrogenase. 11beta-HSD1 activity is reduced in diabetic subjects, while 11beta-HSD2 activity is increased. After application of dexamethasone, 11beta-HSD1 mRNA increases in both groups, whereas 11beta-HSD2 mRNA decreases. 11beta-HSD1 activity increases in diabetic subjects, but not in controls, whereas 11beta-HSD2 activity does not change in either group; mRNA levels are similar in diabetic and control subjects for 11beta-hydroxysteroid dehydrogenase 1 and 11beta-hydroxysteroid dehydrogenase 2. 11beta-Hydroxysteroid dehydrogenase 2-activity is higher in diabetic patients. After treatment with dexamethasone, 11beta-hydroxysteroid dehydrogenase 1-mRNA increases in both groups, whereas 11beta-hydroxysteroid dehydrogenase 2-mRNA decreases. 11beta-Hydroxysteroid dehydrogenase 1-activity increases in diabetic patients, but not in control, whereas 11beta-hydroxysteroid dehydrogenase 2-activity does not change in either group
-
isoform 11beta-HSD1 is clearly expressed while isoform 11beta-HSD2 is much less prominent, 11beta-HSD1 protein expression predominates in endothelial cells and varies during periods of growth
additional information
-
similar amounts of protein for both isoform 11beta-HSD1 and 11beta-HSD2. 11beta-HSD1 functions as a dehydrogenase with no significant reverse reductase activity and colocalizes with cyclooxygenase COX-2 in proximal tubule cells. No colocalization of COX-2 with isoform 11beta-HSD2 in cortical collecting duct
-
adult and fetal lung and cultured fetal lung explant contain similar amounts of isoform HSD2 mRNA. Higher levels of HSD2 protein are detected in fetal lung tissue than in adult lung, with expression being restricted to a subset of epithelial cells in the fetal lung tissue. Differentiated fetal lung explants express higher levels of enzyme protein than undifferentiated explants
-
constitutes an important barrier for 11-OH steroids during pregnancy between maternal and fetal organism, presence of two isoforms
-
the 11beta-HSD2 expression and activity is 7-8fold higher compared to 11beta-HSD1 in the chorionic plate of small gestational age placentas
additional information
-
normotensive persons and patients with low renin hypertension, LREH, expression and activity of isozyme 11beta-HSD2
additional information
-
low expression in liver, ovary, prostate gland, and testis
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
physiological function
additional information
species-specific differences of rat and human placental 11beta-HSD2 steroid turnover, species-specific expression of corticotropin-releasing hormone and steroids in human and rat term placenta
physiological function
the enzyme plays a key role in fetal development. p38 MAPK is a positive regulator of placental 11beta-HSD2, p38 MAPK upregulates placental 11b-HSD2 by increasing the half-life of 11beta-HSD2 mRNA. Also ERK1/2 signaling is involved in regulation of placental 11beta-HSD2, ERK1/2 inhibitor U0126 induces the enzyme expression in trophoblasts. siRNA-mediated knockdown of ERK1/2 expression leads to a similar increase in levels of 11beta-HSD2 protein, as seen in cells treated with the ERK1/2 pharmacological inhibitor
physiological function
the placenta acts as a master regulator for the fetal environment, mediating intrauterine exposures to stress through the activity of genes regulating glucocorticoids, including the 11beta-hydroxysteroid dehydrogenase (HSD11B) type 1 and 2 genes, variation in the genes are associated with infant birth weight. A significant association between methylation at a single CpG site within HSD11B1 and being born large for gestational age is detected. Correlations between methylation and gene expression. Methylation at a single CpG site within HSD11B1 is associated with infant birth weight, and that methylation at several different sites is correlated with gene expression. There is no sex-specific role of methylation in infant birth weight in either time points in pregnancy
physiological function
the placenta acts as a master regulator for the fetal environment, mediating intrauterine exposures to stress through the activity of genes regulating glucocorticoids, including the 11beta-hydroxysteroid dehydrogenase (HSD11B) type 1 and 2 genes, variation in the genes are associated with infant birth weight. Correlations between methylation and gene expression, including sex-specific transcriptional regulation of HSD11B2
physiological function
the placental enzyme 11beta-hydroxysteroid dehydrogenase type 2 (11b-HSD2) shields the fetus from maternal glucocorticoid excess by catalyzing the conversion of these hormones into biologically inactive derivatives
physiological function
the action of cortisol on the human feto-placental unit is regulated by 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2/HSD11B2) that converts cortisol into inactive cortisone. The mRNA expression of HSD11B2 correlates with indirect and direct cortisol turnover rates in C-section placentas only. In contrast to C-sections, corticotropin-releasing hormone, cortisol and cortisone levels are significantly increased in placental samples following spontaneous birth
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). DHI1_HUMAN
292
1
32401
Swiss-Prot
other Location (Reliability: 3)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-20°C, cytosol depleted fraction, 10 mM phosphate buffer, 0.25 M sucrose, stable for 2 days
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
gene HSD11B1, variation exists in placental DNA methylation of HSD11B1, the variation is associated with mRNA expression of the gene, real-time PCR expression analysis. No correlation between HSD11B1 CpG1 and expression, and a strong positive correlation between CpG2 and expression. HSD11B1 gene expression is positively correlated with a single CpG site
gene HSD11B2, DNA and amino acid sequence determination and analysis, microsatellite genotyping
-
gene HSD11B2, two-step real-time quantitative RT-PCR isozyme 11beta-HSD2 expression analysis
gene HSD11B2, variation exists in placental DNA methylation of HSD11B2, the variation is associated with mRNA expression of the gene, real-time PCR expression analysis. Sex-specific correlation between HSD11B2 methylation levels and expression, with females displaying a much stronger correlation between the two factors with no correlation for males, there is no sex-specific role of methylation in infant birth weight in either time points in pregnancy. HSD11B2 expression is negatively correlated with the mean methylation of four CpG sites within its promoter
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
expression of placental 11beta-HSD2 is regulated at both transcriptional and posttranscriptional levels. JNK inhibitor SP600125 has no effect on 11beta-HSD2 isozyme expression
p38 MAPK enhances placental 11beta-HSD2 expression by a posttranscriptional mechanism. ERK1/2 inhibitor U0126 induces the enzyme expression in trophoblasts. siRNA-mediated knockdown of ERK1/2 expression leads to a similar increase in levels of 11beta-HSD2 protein, as seen in cells treated with the ERK1/2 pharmacological inhibitor
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
the enzyme is a target for inhibitor design and development
medicine
medicine
-
11beta-HSD1 is a drug target for treatment of insulin resistance, diabetes and cardiovascular disease
medicine
-
age-related reduced 11beta-HSD2 activity contributes to the rising prevalence of arterial hypertension in elderly
medicine
-
at baseline, mRNA levels are similar in skeletal muscle of diabetic and control sugjects for 11beta-HSD1, 11beta-HSD2, and hexose-6-phosphate dehydrogenase. 11beta-HSD1 activity is reduced in diabetic subjects, while 11beta-HSD2 activity is increased. After application of dexamethasone, 11beta-HSD1 mRNA increases in both groups, whereas 11beta-HSD2 mRNA decreases. 11beta-HSD1 activity increases in diabetic subjects, but not in controls, whereas 11beta-HSD2 activity does not change in either group; mRNA levels are similar in diabetic and control subjects for 11beta-hydroxysteroid dehydrogenase 1 and 11beta-hydroxysteroid dehydrogenase 2. 11beta-Hydroxysteroid dehydrogenase 2-activity is higher in diabetic patients. After treatment with dexamethasone, 11beta-hydroxysteroid dehydrogenase 1-mRNA increases in both groups, whereas 11beta-hydroxysteroid dehydrogenase 2-mRNA decreases. 11beta-Hydroxysteroid dehydrogenase 1-activity increases in diabetic patients, but not in control, whereas 11beta-hydroxysteroid dehydrogenase 2-activity does not change in either group
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Ferrari, P.; Smith, R.E.; Funder, J.W.; Krozowski, Z.S.
Substrate and inhibitor specificity of the clones human 11beta-hydroxysteroid dehydrogenase type 2 isoform
Am. J. Physiol.
270
E900-904
1996
Homo sapiens
Blum , S.; Buhler, H.
Characterization of human placental 11beta-hydroxysteroid dehydrogenase, a key enzyme of cortocosteroid metabolism
Cell. Physiol. Biochem.
5
167-175
1995
Homo sapiens
-
Albiston, A.L.; Obeyesekere, V.R.; Smith, R.E.; Krozowski, Z.S.
Cloning and tissue distribution of the human 11beta-hydroxysteroid dehydrogenase type 2 enzyme
Mol. Cell. Endocrinol.
105
R11-R17
1994
Homo sapiens
Lakshim, V.; Nath, N.; Muneyyirci-Delale, O.
Characterization of 11beta-hydroxysteroid dehydrogenase of human placenta: Evidence for the existence of two species of 11beta-hydroxysteroid dehydrogenases
J. Steroid Biochem. Mol. Biol.
45
391-397
1993
Homo sapiens
Zbankova, S.; Bryndova, J.; Kment, M.; Pacha, J.
Expression of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in colorectal cancer
Cancer Lett.
210
95-100
2004
Homo sapiens
Kossintseva, I.; Wong, S.; Johnstone, E.; Guilbert, L.; Olson, D.M.; Mitchell, B.F.
Proinflammatory cytokines inhibit human placental 11beta-hydroxysteroid dehydrogenase type 2 activity through Ca2+ and cAMP pathways
Am. J. Physiol. Endocrinol. Metab.
290
E282-E288
2006
Homo sapiens
Garbrecht, M.R.; Schmidt, T.J.; Krozowski, Z.S.; Snyder, J.M.
11beta-Hydroxysteroid dehydrogenase type 2 and the regulation of surfactant protein A by dexamethasone metabolites
Am. J. Physiol. Endocrinol. Metab.
290
E653-E660
2006
Homo sapiens
Xiang, J.; Ipek, M.; Suri, V.; Massefski, W.; Pan, N.; Ge, Y.; Tam, M.; Xing, Y.; Tobin, J.F.; Xu, X.; Tam, S.
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I
Bioorg. Med. Chem. Lett.
15
2865-2869
2005
Homo sapiens
Olson, S.; Aster, S.D.; Brown, K.; Carbin, L.; Graham, D.W.; Hermanowski-Vosatka, A.; LeGrand, C.B.; Mundt, S.S.; Robbins, M.A.; Schaeffer, J.M.; Slossberg, L.H.; Szymonifka, M.J.; Thieringer, R.; Wright, S.D.; Balkovec, J.M.
Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
Bioorg. Med. Chem. Lett.
15
4359-4362
2005
Mus musculus (P51661), Homo sapiens (P80365)
Jang, C.; Obeyesekere, V.R.; Dilley, R.J.; Alford, F.P.; Inder, W.J.
11beta Hydroxysteroid dehydrogenase type 1 is expressed and is biologically active in human skeletal muscle
Clin. Endocrinol. (Oxf.)
65
800-805
2006
Homo sapiens
Ohshima, M.; Ohno, S.; Nakajin, S.
Inhibitory effects of some possible endocrine-disrupting chemicals on the isozymes of human 11beta-hydroxysteroid dehydrogenase and expression of their mRNA in gonads and adrenal glands
Environ. Sci.
12
219-230
2005
Homo sapiens
Carvajal, C.A.; Romero, D.G.; Mosso, L.M.; Gonzalez, A.A.; Campino, C.; Montero, J.; Fardella, C.E.
Biochemical and genetic characterization of 11 beta-hydroxysteroid dehydrogenase type 2 in low-renin essential hypertensives
J. Hypertens.
23
71-77
2005
Homo sapiens
Arampatzis, S.; Kadereit, B.; Schuster, D.; Balazs, Z.; Schweizer, R.A.; Frey, F.J.; Langer, T.; Odermatt, A.
Comparative enzymology of 11beta-hydroxysteroid dehydrogenase type 1 from six species
J. Mol. Endocrinol.
35
89-101
2005
Canis lupus familiaris, Cavia porcellus (Q6QLL4), Homo sapiens (P28845), Homo sapiens (P80365), Mesocricetus auratus (Q6R0J2), Mus musculus, Rattus norvegicus
Temkin, S.; Nacharaju, V.L.; Hellman, M.; Lee, Y.C.; Abulafia, O.
Type 2 11beta-hydroxysteroid dehydrogenase activity in human ovarian cancer
Steroids
7
1019-1023
2006
Homo sapiens
-
Ito-Kobayashi, M.; Aoyagi, A.; Tanaka, I.; Muramatsu, Y.; Umetani, M.; Takatsu, T.
Sterenin A, B, C and D, novel 11beta-hydroxysteroid dehydrogenase type 1 inhibitors from Stereum sp. SANK 21205
J. Antibiot.
61
128-135
2008
Homo sapiens
Jang, C.; Obeyesekere, V.R.; Dilley, R.J.; Krozowski, Z.; Inder, W.J.; Alford, F.P.
Altered activity of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in skeletal muscle confers metabolic protection in subjects with type 2 diabetes
J. Clin. Endocrinol. Metab.
92
3314-3320
2007
Homo sapiens
Gong, R.; Morris, D.J.; Brem, A.S.
Human renal 11beta-hydroxysteroid dehydrogenase 1 functions and co-localizes with COX-2
Life Sci.
82
631-637
2008
Homo sapiens
Garbrecht, M.R.; Klein, J.M.; McCarthy, T.A.; Schmidt, T.J.; Krozowski, Z.S.; Snyder, J.M.
11-beta Hydroxysteroid dehydrogenase type 2 in human adult and fetal lung and its regulation by sex steroids
Pediatr. Res.
62
26-31
2007
Homo sapiens
Chandras, C.; Harris, T.E.; Bernal, A.L.; Abayasekara, D.R.; Michael, A.E.
PTGER1 and PTGER2 receptors mediate regulation of progesterone synthesis and type 1 11beta-hydroxysteroid dehydrogenase activity by prostaglandin E2 in human granulosa-lutein cells
J. Endocrinol.
194
595-602
2007
Homo sapiens
Johansson, L.; Fotsch, C.; Bartberger, M.D.; Castro, V.M.; Chen, M.; Emery, M.; Gustafsson, S.; Hale, C.; Hickman, D.; Homan, E.; Jordan, S.R.; Komorowski, R.; Li, A.; McRae, K.; Moniz, G.; Matsumoto, G.; Orihuela, C.; Palm, G.; Veniant, M.; Wang, M.; Williams, M.; Zhang, J.
2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice
J. Med. Chem.
51
2933-2943
2008
Homo sapiens
Henschkowski, J.; Stuck, A.E.; Frey, B.M.; Gillmann, G.; Dick, B.; Frey, F.J.; Mohaupt, M.G.
Age-dependent decrease in 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) activity in hypertensive patients
Am. J. Hypertens.
21
644-649
2008
Homo sapiens
Zhao, B.; Chu, Y.; Huang, Y.; Hardy, D.O.; Lin, S.; Ge, R.S.
Structure-dependent inhibition of human and rat 11beta-hydroxysteroid dehydrogenase 2 activities by phthalates
Chem. Biol. Interact.
183
79-84
2010
Homo sapiens, Rattus norvegicus
Mericq, V.; Medina, P.; Kakarieka, E.; Marquez, L.; Johnson, M.C.; Iniguez, G.
Differences in expression and activity of 11beta-hydroxysteroid dehydrogenase type 1 and 2 in human placentas of term pregnancies according to birth weight and gender
Eur. J. Endocrinol.
161
419-425
2009
Homo sapiens
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
Classen-Houben, D.; Schuster, D.; Da Cunha, T.; Odermatt, A.; Wolber, G.; Jordis, U.; Kueenburg, B.
Selective inhibition of 11beta-hydroxysteroid dehydrogenase 1 by 18alpha-glycyrrhetinic acid but not 18beta-glycyrrhetinic acid
J. Steroid Biochem. Mol. Biol.
113
248-252
2009
Homo sapiens
Chapman, K.E.; Coutinho, A.E.; Gray, M.; Gilmour, J.S.; Savill, J.S.; Seckl, J.R.
The role and regulation of 11beta-hydroxysteroid dehydrogenase type 1 in the inflammatory response
Mol. Cell. Endocrinol.
301
123-131
2009
Homo sapiens, Mus musculus
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
Bos taurus, Homo sapiens, Rattus norvegicus
Stanetty, C.; Czollner, L.; Koller, I.; Shah, P.; Gaware, R.; Cunha, T.D.; Odermatt, A.; Jordis, U.; Kosma, P.; Classen-Houben, D.
Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11beta-hydroxysteroid dehydrogenase 2 inhibitors
Bioorg. Med. Chem.
18
7522-7541
2010
Homo sapiens
Kim, C.H.; Cho, Y.S.
Selection and optimization of MCF-7 cell line for screening selective inhibitors of 11beta-hydroxysteroid dehydrogenase 2
Cell Biochem. Funct.
28
440-447
2010
Homo sapiens
Xu, D.; Sheng, Y.; Zhou, Z.Y.; Liu, R.; Leng, Y.; Liu, J.K.
Sesquiterpenes from cultures of the basidiomycete Clitocybe conglobata and their 11 beta-hydroxysteroid dehydrogenase inhibitory activity
Chem. Pharm. Bull.
57
433-435
2009
Homo sapiens, Mus musculus
Zhang, L.; Shen, Y.; Zhu, H.J.; Wang, F.; Leng, Y.; Liu, J.K.
Pentanol derivatives from basidiomycete Catathelasma imperiale and their 11beta-hydroxysteroid dehydrogenases inhibitory activity
J. Antibiot.
62
239-242
2009
Homo sapiens, Mus musculus
Zhang, L.; Shen, Y.; Wang, F.; Leng, Y.; Liu, J.K.
Rare merosesquiterpenoids from basidiomycete Craterellus odoratus and their inhibition of 11beta-hydroxysteroid dehydrogenases
Phytochemistry
71
100-103
2010
Homo sapiens
Kratschmar, D.V.; Vuorinen, A.; Da Cunha, T.; Wolber, G.; Classen-Houben, D.; Doblhoff, O.; Schuster, D.; Odermatt, A.
Characterization of activity and binding mode of glycyrrhetinic acid derivatives inhibiting 11beta-hydroxysteroid dehydrogenase type 2
J. Steroid Biochem. Mol. Biol.
125
129-142
2011
Homo sapiens (P80365)
Zhao, B.; Lian, Q.; Chu, Y.; Hardy, D.O.; Li, X.K.; Ge, R.S.
The inhibition of human and rat 11beta-hydroxysteroid dehydrogenase 2 by perfluoroalkylated substances
J. Steroid Biochem. Mol. Biol.
125
143-147
2011
Rattus norvegicus, Homo sapiens (P80365)
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
Homo sapiens (P80365)
Guan, H.; Sun, K.; Yang, K.
The ERK1/2 signaling pathway regulates 11beta-hydroxysteroid dehydrogenase type 2 expression in human trophoblast cells through a transcriptional mechanism
Biol. Reprod.
89
92
2013
Homo sapiens (P80365)
Green, B.B.; Armstrong, D.A.; Lesseur, C.; Paquette, A.G.; Guerin, D.J.; Kwan, L.E.; Marsit, C.J.
The role of placental 11-beta hydroxysteroid dehydrogenase type 1 and type 2 methylation on gene expression and infant birth weight
Biol. Reprod.
92
149
2015
Homo sapiens (P28845), Homo sapiens (P80365)
Heussner, K.; Ruebner, M.; Huebner, H.; Rascher, W.; Menendez-Castro, C.; Hartner, A.; Fahlbusch, F.B.; Rauh, M.
Species differences of 11beta-hydroxysteroid dehydrogenase type 2 function in human and rat term placenta determined via LC-MS/MS
Placenta
37
79-84
2016
Homo sapiens (P80365), Rattus norvegicus, Rattus norvegicus Wistar
Huebner, H.; Heussner, K.; Ruebner, M.; Schmid, M.; Nadal, J.; Woelfle, J.; Hartner, A.; Menendez-Castro, C.; Rauh, M.; Beckmann, M.W.; Kehl, S.; Fahlbusch, F.B.
Influence of labor on direct and indirect determinants of placental 11beta-hydroxysteroid dehydrogenase activity
Arch. Gynecol. Obstet.
303
401-408
2021
Homo sapiens (P80365)
EXTERNAL LINKS (specific for EC-Number 1.1.1.B40)
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
