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Literature summary for 1.1.1.146 extracted from

  • Latif, S.A.; Pardo, H.A.; Hardy, M.P.; Morris, D.J.
    Endogenous selective inhibitors of 11beta-hydroxysteroid dehydrogenase isoforms 1 and 2 of adrenal origin (2005), Mol. Cell. Endocrinol., 243, 43-50.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(11beta)-11-hydroxyallopregnanolone
-
Homo sapiens
(11beta)-11-hydroxyprogesterone
-
Homo sapiens
(3alpha,5alpha)-3,11,21-trihydroxypregn-11-en-20-one
-
Homo sapiens
11-dehydrocortisterone
-
Ovis aries
11-oxo-3alpha,5alpha-tetrahydrotestosterone
-
Homo sapiens
11-oxo-3beta,5alpha-tetrathydrotestosterone
-
Ovis aries
11-oxo-allopregnanolone
-
Homo sapiens
11-oxo-allopregnanolone
-
Ovis aries
11-oxo-androstenedione
-
Homo sapiens
11-oxo-progesterone
-
Homo sapiens
11-oxo-progesterone
-
Ovis aries
11-oxo-testosterone
-
Homo sapiens
11-oxo-testosterone
-
Ovis aries
11beta-hydroxy-allopregnanolone
-
Ovis aries
11beta-hydroxy-androstanediol
-
Homo sapiens
11beta-hydroxy-testosterone
-
Homo sapiens
11beta-hydroxyandrostanediol
-
Ovis aries
11beta-hydroxyandrostenedione
-
Ovis aries
11beta-hydroxyprogesterone
-
Ovis aries
11beta-hydroxytestosterone
-
Ovis aries
3alpha,5alpha-tetrahydro-dehydrocortisterone
-
Ovis aries
3alpha,5alpha-tetrahydroaldosterone
-
Ovis aries
3alpha,5alpha-tetrahydrocorticosterone
-
Homo sapiens
3alpha,5alpha-tetrahydrocorticosterone
-
Ovis aries
3alpha,5alpha-tetrahydrocortisol
-
Ovis aries
5alpha-dihydrocorticosterone
-
Homo sapiens
5alpha-dihydrocorticosterone
-
Ovis aries
additional information steroid hormones, adrenocorticosteroid derivatives, progesteron and androgen steroid hormones, with 5alpha-ring A reduced-configuration selectively inhibit isozyme 11beta-HSD2, while 5beta-derivatives are inactive Ovis aries

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1,2-dehydrocortisol + NADP+ Homo sapiens
-
1,2-dehydrocortisone + NADPH
-
r

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Ovis aries
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
adrenal gland
-
Ovis aries
-
kidney
-
Ovis aries
-
Leydig cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1,2-dehydrocortisol + NADP+
-
Homo sapiens 1,2-dehydrocortisone + NADPH
-
r

Synonyms

Synonyms Comment Organism
11beta-HSD1
-
Homo sapiens
11beta-HSD1
-
Ovis aries
11beta-hydroxysteroid dehydrogenase isoforms 1
-
Homo sapiens
11beta-hydroxysteroid dehydrogenase isoforms 1
-
Ovis aries

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens
37
-
assay at Ovis aries

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8.4
-
assay at Homo sapiens
8.4
-
assay at Ovis aries

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00005
-
pH 8.4, 37°C Ovis aries 11beta-hydroxyprogesterone
0.00012
-
pH 8.4, 37°C Ovis aries 11beta-hydroxy-allopregnanolone
0.00015
-
pH 8.4, 37°C Ovis aries 5alpha-dihydrocorticosterone
0.00026
-
pH 8.4, 37°C Ovis aries 3alpha,5alpha-tetrahydrocorticosterone
0.00035
-
pH 8.4, 37°C Ovis aries 11beta-hydroxytestosterone
0.0004
-
pH 8.4, 37°C Ovis aries 11-oxo-progesterone
0.00047
-
pH 8.4, 37°C Ovis aries 11-dehydrocortisterone
0.0005
-
pH 8.4, 37°C Ovis aries 3alpha,5alpha-tetrahydroaldosterone
0.00065
-
reductase reaction, pH 8.4, 37°C Homo sapiens 11-oxo-3alpha,5alpha-tetrahydrotestosterone
0.0007
-
reductase reaction, pH 8.4, 37°C Homo sapiens (3alpha,5alpha)-3,11,21-trihydroxypregn-11-en-20-one
0.0008
-
pH 8.4, 37°C Ovis aries 3alpha,5alpha-tetrahydro-dehydrocortisterone
0.0008
-
reductase reaction, pH 8.4, 37°C Homo sapiens 11-oxo-allopregnanolone
0.0013
-
dehydrogenase reaction, pH 8.4, 37°C Homo sapiens 3alpha,5alpha-tetrahydrocorticosterone
0.00135
-
pH 8.4, 37°C Ovis aries 11-oxo-testosterone
0.0015
-
pH 8.4, 37°C Ovis aries 11-oxo-allopregnanolone
0.0021
-
dehydrogenase reaction, pH 8.4, 37°C Homo sapiens 5alpha-dihydrocorticosterone
0.003
-
dehydrogenase reaction, pH 8.4, 37°C Homo sapiens (11beta)-11-hydroxyallopregnanolone
0.0045
-
pH 8.4, 37°C Ovis aries 11beta-hydroxyandrostanediol
0.005
-
dehydrogenase reaction, dehydrogenase reaction, pH 8.4, 37°C Homo sapiens 11beta-hydroxy-androstanediol
0.0056
-
dehydrogenase reaction, pH 8.4, 37°C Homo sapiens (11beta)-11-hydroxyprogesterone
0.0063
-
reductase reaction, pH 8.4, 37°C Homo sapiens 5alpha-dihydrocorticosterone
0.0078
-
pH 8.4, 37°C Ovis aries 11beta-hydroxyandrostenedione
0.008
-
pH 8.4, 37°C Ovis aries 3alpha,5alpha-tetrahydrocortisol
0.008
-
pH 8.4, 37°C Ovis aries 11-oxo-3beta,5alpha-tetrathydrotestosterone
0.008
-
dehydrogenase reaction, pH 8.4, 37°C Homo sapiens (3alpha,5alpha)-3,11,21-trihydroxypregn-11-en-20-one
0.009
-
dehydrogenase reaction, pH 8.4, 37°C Homo sapiens 11beta-hydroxy-testosterone
0.0095
-
pH 8.4, 37°C Homo sapiens 11-oxo-progesterone
0.0115
-
reductase reaction, pH 8.4, 37°C Homo sapiens 11beta-hydroxy-androstanediol
0.018
-
reductase reaction, pH 8.4, 37°C Homo sapiens 11-oxo-testosterone
0.021
-
reductase reaction, pH 8.4, 37°C Homo sapiens 11-oxo-androstenedione
0.05
-
dehydrogenase reaction, pH 8.4, 37°C Homo sapiens 11-oxo-3alpha,5alpha-tetrahydrotestosterone
0.05
-
reductase reaction, pH 8.4, 37°C Homo sapiens 3alpha,5alpha-tetrahydrocorticosterone