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Literature summary extracted from

  • Atanasov, A.G.; Dzyakanchuk, A.A.; Schweizer, R.A.; Nashev, L.G.; Maurer, E.M.; Odermatt, A.
    Coffee inhibits the reactivation of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1: a glucocorticoid connection in the anti-diabetic action of coffee? (2006), FEBS Lett., 580, 4081-4085.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.146 expression of isozyme 11beta-HSD1 in HEK-293 cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.146 coffee Coffea arabica fruit extract, corresponding to an italian espresso, inhibits recombinant and endogenous isozyme 11beta-HSD1 in HEK-293 cells up by 80% at 2% of extract, the inhibitory component is heat-stable with considerable polarity, extract blocks 11beta-HSD1-dependent cortisol formation in vivo preventing the subsequent nuclear translocation of the glucocorticoid receptor and abolishes glucocorticoid-induced expression of the key gluconeogenic enzyme phosphoenolpyruvate carboxykinase, at least part of the anti-diabetic effects of coffee consumption is due to inhibition of 11beta-HSD1-dependent glucocorticoid reactivation, overview, the inhibitory effect on isozyme 11beta-HSD1 is 7-10fold higher compared to isozyme 11beta-HSD2 Homo sapiens
1.1.1.146 additional information no inhibition by caffeic acid, chlorogenic acid or trigonelline 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 cortisone + NADPH + H+ Homo sapiens isozyme 11beta-HSD1 cortisol + NADP+
-
 ?

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.146 cortisone + NADPH + H+ isozyme 11beta-HSD1 Homo sapiens cortisol + NADP+
-
 ?

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.146 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.146 7.4
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.146 NADPH
-
 Homo sapiens