The 11-ketosteroid 11-ketodexamethasone is a glucocorticoid receptor agonist

• Published in: Molecular and cellular endocrinology Vol. 214; no. 1; pp. 27 - 37
• Main Authors: Rebuffat, Alexandre G, Tam, Steven, Nawrocki, Andrea R, Baker, Michael E, Frey, Brigitte M, Frey, Felix J, Odermatt, Alex
• Format: Journal Article
• Language: English
• Published: Ireland Elsevier Ireland Ltd 12.02.2004
• Subjects: 11β-Hydroxysteroid dehydrogenase; Active Transport, Cell Nucleus - drug effects; Animals; Binding Sites; Cell Line; Cortisol; Dexamethasone; Dexamethasone - analogs & derivatives; Dexamethasone - pharmacology; Glucocorticoid receptor; Humans; Hydrocortisone - pharmacology; Ketosteroids - pharmacology; Kinetics; Mineralocorticoid receptor; Protein Binding; Receptors, Glucocorticoid - agonists; Receptors, Glucocorticoid - metabolism; Receptors, Glucocorticoid - physiology; Transcriptional Activation; Cortisol; Dexamethasone; Mineralocorticoid receptor; Glucocorticoid receptor; 11β-Hydroxysteroid dehydrogenase

Dexamethasone (Dex) is a potent and long-acting glucocorticoid in terms of anti-inflammatory activity without substantial sodium retaining effect. Here, we examine the ability of the 11β-hydroxyglucocorticoids Dex and cortisol and their 11-keto forms 11-ketodexamethasone (11-ketoDex) and cortisone t...