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Literature summary extracted from

  • Beck, K.R.; Inderbinen, S.G.; Kanagaratnam, S.; Kratschmar, D.V.; Jetten, A.M.; Yamaguchi, H.; Odermatt, A.
    11beta-Hydroxysteroid dehydrogenases control access of 7beta,27-dihydroxycholesterol to retinoid-related orphan receptor gamma (2019), J. Lipid Res., 60, 1535-1546 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.146 7-keto,27-hydroxycholesterol potent inhibitor of the isoform 11beta-HSD1-dependent oxoreduction of cortisone Homo sapiens
1.1.1.146 7beta,27-dihydroxycholesterol potent inhibitor of the isoform 11beta-HSD2-dependent oxidation of cortisol Homo sapiens
1.1.1.146 glycyrrhetinic acid inhibitor of isoform 11beta-HSD2 Homo sapiens
1.1.1.146 additional information 7alpha,27-dihydroxycholesterol does not inhibit the enzyme isoform 11beta-HSD1 activity at concentrations up to 0.01 mM; 7alpha,27-dihydroxycholesterol does not inhibit the enzyme isoform 11beta-HSD2 activity at concentrations up to 0.01 mM Homo sapiens
1.1.1.146 T0504 inhibitor of 11beta-HSD1 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.146 0.000039
-
 7-keto,27-hydroxycholesterol isoform 11beta-HSD1, at pH 7.4, temperature not specified in the publication Homo sapiens
1.1.1.146 0.000056
-
 7beta,27-dihydroxycholesterol isoform 11beta-HSD2, at pH 7.4, temperature not specified in the publication Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.146 microsome
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.146 7-keto,27-hydroxycholesterol + NADP+ Homo sapiens the reaction is catalyzed by isoform 11beta-HSD1 7beta,27-dihydroxycholesterol + NADPH + H+
-
 r
1.1.1.146 7-oxo-cholesterol + NADP+ Homo sapiens
-
 7beta-hydroxycholesterol + NADPH + H+
-
 ?
1.1.1.146 7beta,27-dihydroxycholesterol + NADH + H+ Homo sapiens the reaction is catalyzed by isoform 11beta-HSD2 7-keto,27-hydroxycholesterol + NAD+
-
 r
1.1.1.146 cortisol + NAD+ Homo sapiens the reaction is catalyzed by isoform 11beta-HSD2 cortisone + NADH + H+
-
 ?
1.1.1.146 cortisone + NADPH + H+ Homo sapiens the reaction is catalyzed by isoform 11beta-HSD1 cortisol + NADP+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.146 Homo sapiens P28845
-
-
1.1.1.146 Homo sapiens R4GN04
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.146 colonic cancer cell
-
 Homo sapiens
-
1.1.1.146 HEK-293 cell
-
 Homo sapiens
-
1.1.1.146 SW-620 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.146 7-keto,27-hydroxycholesterol + NADP+ the reaction is catalyzed by isoform 11beta-HSD1 Homo sapiens 7beta,27-dihydroxycholesterol + NADPH + H+
-
 r
1.1.1.146 7-oxo-cholesterol + NADP+
-
 Homo sapiens 7beta-hydroxycholesterol + NADPH + H+
-
 ?
1.1.1.146 7beta,27-dihydroxycholesterol + NADH + H+ the reaction is catalyzed by isoform 11beta-HSD2 Homo sapiens 7-keto,27-hydroxycholesterol + NAD+
-
 r
1.1.1.146 cortisol + NAD+ the reaction is catalyzed by isoform 11beta-HSD2 Homo sapiens cortisone + NADH + H+
-
 ?
1.1.1.146 cortisone + NADPH + H+ the reaction is catalyzed by isoform 11beta-HSD1 Homo sapiens cortisol + NADP+
-
 ?
1.1.1.146 additional information neither 7alpha-hydroxycholesterol nor 7betha-hydroxycholesterol is oxidized by isoform 11beta-HSD1 Homo sapiens ?
-
-

Synonyms

EC Number Synonyms Comment Organism
1.1.1.146 11beta-HSD1
-
 Homo sapiens
1.1.1.146 11beta-HSD2
-
 Homo sapiens
1.1.1.146 11beta-hydroxysteroid dehydrogenase type 1
-
 Homo sapiens
1.1.1.146 11beta-hydroxysteroid dehydrogenase type 2
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.146 0.000011
-
 isoform 11beta-HSD2, at pH 7.4, temperature not specified in the publication Homo sapiens 7beta,27-dihydroxycholesterol
1.1.1.146 0.000015
-
 isoform 11beta-HSD2, at pH 7.4, temperature not specified in the publication Homo sapiens 7-keto,27-hydroxycholesterol
1.1.1.146 0.000357
-
 isoform 11beta-HSD1, at pH 7.4, temperature not specified in the publication Homo sapiens 7-keto,27-hydroxycholesterol
1.1.1.146 0.003
-
 isoform 11beta-HSD1, at pH 7.4, temperature not specified in the publication Homo sapiens 7beta,27-dihydroxycholesterol

General Information

EC Number General Information Comment Organism
1.1.1.146 metabolism isoform 11beta-HSD1 controls retinoid-related orphan receptor gamma activity Homo sapiens
1.1.1.146 metabolism isoform 11beta-HSD2 controls retinoid-related orphan receptor gamma activity Homo sapiens