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Literature summary for 1.1.1.146 extracted from

  • 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 (2011), J. Steroid Biochem. Mol. Biol., 125, 129-142.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in HEK-293 cell Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(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 Homo sapiens
(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 Homo sapiens
(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 Homo sapiens
(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 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845 isoform 11beta-HSD1
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000025
-
pH 7.4, 37°C Homo sapiens (3beta)-3-[(3-carboxypropanoyl)oxy]urs-12-en-28-oic acid
0.000049
-
pH 7.4, 37°C Homo sapiens (3beta)-3-hydroxy-18,29-epoxyolean-12-ene-11,29-dione