Literature DB >> 18311666

11beta-hydroxysteroid dehydrogenase type 1 inhibitors for metabolic syndrome.

Christine G Schnackenberg1.   

Abstract

The metabolic syndrome is a constellation of interrelated metabolic risk factors that appear to promote the development of diabetes and cardiovascular disease. These risk factors include abdominal obesity, insulin resistance, hypertension and dyslipidemia. 11beta-Hydroxysteroid dehydrogenase (11beta-HSD) catalyzes the interconversion of glucocorticoids through the activity of two isozymes: type 1 (11beta-HSD1) and type 2 (11beta-HSD2). 11beta-HSD1 converts inactive glucocorticoid to the active form, whereas 11beta-HSD2 converts active glucocorticoid to the inactive form. It is well established that reduced 11beta-HSD2 activity causes hypertension and electrolyte abnormalities. More recently, the pathophysiological role of 11beta-HSD1 has been explored and studies suggest that increased 11beta-HSD1 activity within target tissues may promote insulin resistance, obesity, hypertension and dyslipidemia. This review will discuss the evidence that inhibition of 11beta-HSD1 may be therapeutic in the treatment of the metabolic syndrome.

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Year:  2008        PMID: 18311666

Source DB:  PubMed          Journal:  Curr Opin Investig Drugs        ISSN: 1472-4472


  4 in total

1.  Discovery of adamantyl heterocyclic ketones as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors.

Authors:  Xiangdong Su; Nigel Vicker; Mark P Thomas; Fabienne Pradaux-Caggiano; Heather Halem; Michael D Culler; Barry V L Potter
Journal:  ChemMedChem       Date:  2011-05-23       Impact factor: 3.466

2.  Adamantyl ethanone pyridyl derivatives: potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1.

Authors:  Xiangdong Su; Fabienne Pradaux-Caggiano; Nigel Vicker; Mark P Thomas; Heather Halem; Michael D Culler; Barry V L Potter
Journal:  ChemMedChem       Date:  2011-06-28       Impact factor: 3.466

3.  11βHSD1 Inhibition with AZD4017 Improves Lipid Profiles and Lean Muscle Mass in Idiopathic Intracranial Hypertension.

Authors:  Rowan S Hardy; Hannah Botfield; Keira Markey; James L Mitchell; Zerin Alimajstorovic; Connar S J Westgate; Michael Sagmeister; Rebecca J Fairclough; Ryan S Ottridge; Andreas Yiangou; Karl-Heinz H Storbeck; Angela E Taylor; Lorna C Gilligan; Wiebke Arlt; Paul M Stewart; Jeremy W Tomlinson; Susan P Mollan; Gareth G Lavery; Alexandra J Sinclair
Journal:  J Clin Endocrinol Metab       Date:  2021-01-01       Impact factor: 5.958

4.  Chronic inhibition of 11 β -hydroxysteroid dehydrogenase type 1 activity decreases hypertension, insulin resistance, and hypertriglyceridemia in metabolic syndrome.

Authors:  Christine G Schnackenberg; Melissa H Costell; Daniel J Krosky; Jianqi Cui; Charlene W Wu; Victor S Hong; Mark R Harpel; Robert N Willette; Tian-Li Yue
Journal:  Biomed Res Int       Date:  2013-03-18       Impact factor: 3.411

  4 in total

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