The cortisol-cortisone shuttle and hypertension
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Genetic dissection of sodium and potassium transport along the aldosterone-sensitive distal nephron: Importance in the control of blood pressure and hypertension
2013, FEBS LettersCitation Excerpt :In vitro studies indicate that aldosterone occupies both MR and GR under physiological conditions to mediate the sodium transport response but cortisol or corticosterone may also occupy MR and GR under extreme stress [87]. HSD11B2 (11β-hydroxysteroid dehydrogenase type 2 = 11β-HSD2) controls ligand access to the mineralocorticoid receptor, and ablation (or inhibition by drug or toxic) of the enzyme causes severe hypertension in human (apparent mineralocorticoid excess = AME) [88]. Bailey et al. [89] generated a Hsd11b2 null mouse on an inbred C57BL/6J genetic background, allowing survival to adulthood.
Momordica charantia extract, a herbal remedy for type 2 diabetes, contains a specific 11β-hydroxysteroid dehydrogenase type 1 inhibitor
2012, Journal of Steroid Biochemistry and Molecular BiologyCitation Excerpt :Collectively, these findings emphasize the potential benefits of a specific inhibitor of human 11β-HSD1 in the treatment of obesity and type 2 diabetes. An important requirement for this inhibitor is selectivity, i.e. it must not equally inhibit 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), the enzyme catalyzing the reverse reaction in mineralocorticoid target tissues, as this leads to severe side effects such as renal sodium retention, hypokalaemia and hypertension [11,12]. Momordica charantia (also known as bitter melon or bitter gourd) belongs to the Cucurbitaceae family and has a long history of use as a hypoglycaemic agent amongst the indigenous populations of Asia, South America, the Caribbean, and East Africa [13,14].
11β-hydroxysteroid dehydrogenase type 1 - First part: Role of cortisol tissue exposure in the metabolic risk associated with obesity
2009, Medecine des Maladies MetaboliquesInhibition of 11ß-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target
2007, Drug Discovery TodayAngiotensin II, corticosteroids, type II diabetes and the metabolic syndrome
2007, Medical HypothesesA ligand-mediated hydrogen bond network required for the activation of the mineralocorticoid receptor
2005, Journal of Biological Chemistry