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Literature summary for 1.1.1.146 extracted from

  • Blum, A.; Favia, A.D.; Maser, E.
    11beta-Hydroxysteroid dehydrogenase type 1 inhibitors with oleanan and ursan scaffolds (2009), Mol. Cell. Endocrinol., 301, 132-136.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
isozyme 11beta-HSD1 is expressed in Pichia pastoris Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2alpha,3beta,5xi,6beta,9xi,18xi)-2,3,6,23-tetrahydroxyurs-12-en-28-oate
-
Homo sapiens
(2alpha,3beta,5xi,9xi,18xi)-2,3,23-trihydroxyurs-12-en-28-oate
-
Homo sapiens
(2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
-
Homo sapiens
(2R,4aS,6aS,12bR,14aS)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2-carboxylate
-
Homo sapiens
(3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
-
Homo sapiens
(3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol
-
Homo sapiens
(3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
-
Homo sapiens
(3beta,5xi,9xi,18xi)-3-(acetyloxy)-11-oxours-12-en-24-oate
-
Homo sapiens
(3beta,5xi,9xi,18xi)-3-(acetyloxy)urs-12-en-24-oate
-
Homo sapiens
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
-
Homo sapiens
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
-
Homo sapiens
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxours-12-en-28-oate
-
Homo sapiens
(3beta,5xi,9xi,18xi)-3-hydroxyolean-12-en-28-oate
-
Homo sapiens
(5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
-
Homo sapiens
carbenoxolone
-
Homo sapiens
ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
-
Homo sapiens
methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
adipocyte
-
Homo sapiens
-
liver isozyme 11beta-HSD1 Homo sapiens
-
muscle fibre
-
Homo sapiens
-
placenta isozyme 11beta-HSD2 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cortisol + NADP+
-
Homo sapiens cortisone + NADPH
-
?

Synonyms

Synonyms Comment Organism
11beta-HSD1 isozyme Homo sapiens
11beta-HSD2 isozyme Homo sapiens
11beta-hydroxysteroid dehydrogenase type 1
-
Homo sapiens
11beta-hydroxysteroid dehydrogenase type 2
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000008
-
11beta-HSD2, cortisol oxidation Homo sapiens (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.000012
-
11beta-HSD1, cortisol oxidation Homo sapiens (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.000012
-
11beta-HSD1, cortisone reduction Homo sapiens (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.000049
-
11beta-HSD1, cortisol oxidation Homo sapiens (3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
0.000056
-
11beta-HSD1, cortisol oxidation Homo sapiens (2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
0.000061
-
11beta-HSD1, cortisol oxidation Homo sapiens methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.000068
-
11beta-HSD1, cortisol oxidation Homo sapiens ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.000074
-
11beta-HSD1, cortisol oxidation Homo sapiens (5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
0.000119
-
11beta-HSD1, cortisone reduction Homo sapiens methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.000122
-
11beta-HSD1, cortisone reduction Homo sapiens (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
0.000124
-
11beta-HSD1, cortisone reduction Homo sapiens (5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
0.000141
-
11beta-HSD1, cortisone reduction Homo sapiens ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.000149
-
11beta-HSD1, cortisone reduction Homo sapiens (3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
0.000177
-
11beta-HSD1, cortisol oxidation Homo sapiens (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
0.000244
-
11beta-HSD1, cortisone reduction Homo sapiens (2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
0.001
-
11beta-HSD1, cortisol oxidation Homo sapiens (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxours-12-en-28-oate
0.002
-
11beta-HSD1, cortisol oxidation Homo sapiens (3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
0.002
-
11beta-HSD1, cortisol oxidation Homo sapiens (3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol
0.003
-
11beta-HSD1, cortisol oxidation Homo sapiens (2alpha,3beta,5xi,6beta,9xi,18xi)-2,3,6,23-tetrahydroxyurs-12-en-28-oate
0.005
-
11beta-HSD1, cortisol oxidation Homo sapiens (2alpha,3beta,5xi,9xi,18xi)-2,3,23-trihydroxyurs-12-en-28-oate
0.009
-
11beta-HSD1, cortisol oxidation Homo sapiens (3beta,5xi,9xi,18xi)-3-(acetyloxy)urs-12-en-24-oate
0.011
-
11beta-HSD1, cortisol oxidation Homo sapiens (3beta,5xi,9xi,18xi)-3-(acetyloxy)-11-oxours-12-en-24-oate
0.012
-
11beta-HSD2, cortisol oxidation Homo sapiens (2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
0.016
-
11beta-HSD2, cortisol oxidation Homo sapiens (3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
0.016
-
11beta-HSD2, cortisol oxidation Homo sapiens (5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
0.025
-
11beta-HSD2, cortisol oxidation Homo sapiens (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
0.037
-
11beta-HSD1, cortisone reduction Homo sapiens (3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol
0.039
-
11beta-HSD1, cortisone reduction Homo sapiens (3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
0.068
-
11beta-HSD1, cortisone reduction Homo sapiens (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxours-12-en-28-oate
0.074
-
11beta-HSD1, cortisone reduction Homo sapiens (3beta,5xi,9xi,18xi)-3-(acetyloxy)-11-oxours-12-en-24-oate
0.112
-
11beta-HSD1, cortisone reduction Homo sapiens (2alpha,3beta,5xi,6beta,9xi,18xi)-2,3,6,23-tetrahydroxyurs-12-en-28-oate
0.2
-
11beta-HSD1, cortisol oxidation , IC50 above 0.2 mM Homo sapiens (3beta,5xi,9xi,18xi)-3-hydroxyolean-12-en-28-oate
0.2
-
11beta-HSD1, cortisone reduction, IC50 above 0.2 mM Homo sapiens (3beta,5xi,9xi,18xi)-3-hydroxyolean-12-en-28-oate
0.2
-
11beta-HSD1, cortisone reduction, IC50 above 0.2 mM Homo sapiens (3beta,5xi,9xi,18xi)-3-(acetyloxy)urs-12-en-24-oate
0.2
-
11beta-HSD1, cortisone reduction, IC50 above 0.2 mM Homo sapiens (2alpha,3beta,5xi,9xi,18xi)-2,3,23-trihydroxyurs-12-en-28-oate
0.2
-
11beta-HSD2, cortisol oxidation, IC50 above 0.2 mM Homo sapiens methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.2
-
11beta-HSD2, cortisol oxidation, IC50 above 0.2 mM Homo sapiens ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.2
-
11beta-HSD2, cortisol oxidation, IC50 above 0.2 mM Homo sapiens (3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
0.2
-
11beta-HSD2, cortisol oxidation, IC50 above 0.2 mM Homo sapiens (3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol