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Literature summary for 1.1.1.146 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)

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

Inhibitors

Inhibitors Comment Organism Structure
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
additional information no inhibition by caffeic acid, chlorogenic acid or trigonelline Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cortisone + NADPH + H+ Homo sapiens isozyme 11beta-HSD1 cortisol + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens