Literature DB >> 18363514

11-Beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors in type 2 diabetes mellitus and obesity.

Katherine A Hughes1, Scott P Webster, Brian R Walker.   

Abstract

BACKGROUND: Glucocorticoids such as cortisol are important regulators of fuel metabolism during starvation and stress. Chronic glucocorticoid excess induces obesity with multiple features of the metabolic syndrome.
OBJECTIVE: In this article, we review the importance of glucocorticoids in metabolic syndrome and the approaches that have been explored to reduce glucocorticoid action as the basis for novel therapy of Type 2 diabetes and obesity.
METHOD: We focus on the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1), which amplifies glucocorticoid concentrations in key metabolic tissues including liver and adipose tissue. RESULTS/
CONCLUSION: Several 11beta-HSD1 inhibitors are in late preclinical or early clinical development and we review here the properties of the class leaders and their potential as the next generation of drugs with multiple benefits in metabolic syndrome.

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Year:  2008        PMID: 18363514     DOI: 10.1517/13543784.17.4.481

Source DB:  PubMed          Journal:  Expert Opin Investig Drugs        ISSN: 1354-3784            Impact factor:   6.206


  30 in total

1.  Labisia pumila extract down-regulates hydroxysteroid (11-beta) dehydrogenase 1 expression and corticosterone levels in ovariectomized rats.

Authors:  Mansor Fazliana; Harvest F Gu; Claes-Göran Östenson; Mashitah Mohd Yusoff; W M Wan Nazaimoon
Journal:  J Nat Med       Date:  2011-08-11       Impact factor: 2.343

Review 2.  Investigational anti-hyperglycemic agents: the future of type 2 diabetes therapy?

Authors:  Sachin K Majumdar; Silvio E Inzucchi
Journal:  Endocrine       Date:  2013-01-25       Impact factor: 3.633

3.  Formation of threohydrobupropion from bupropion is dependent on 11β-hydroxysteroid dehydrogenase 1.

Authors:  Arne Meyer; Anna Vuorinen; Agnieszka E Zielinska; Petra Strajhar; Gareth G Lavery; Daniela Schuster; Alex Odermatt
Journal:  Drug Metab Dispos       Date:  2013-06-26       Impact factor: 3.922

Review 4.  Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery.

Authors:  Mark P Thomas; Barry V L Potter
Journal:  Future Med Chem       Date:  2011-03       Impact factor: 3.808

Review 5.  Therapeutic manipulation of glucocorticoid metabolism in cardiovascular disease.

Authors:  Patrick W F Hadoke; Javaid Iqbal; Brian R Walker
Journal:  Br J Pharmacol       Date:  2009-02-23       Impact factor: 8.739

6.  Cortisol release from adipose tissue by 11beta-hydroxysteroid dehydrogenase type 1 in humans.

Authors:  Roland H Stimson; Jonas Andersson; Ruth Andrew; Doris N Redhead; Fredrik Karpe; Peter C Hayes; Tommy Olsson; Brian R Walker
Journal:  Diabetes       Date:  2008-10-13       Impact factor: 9.461

7.  Overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in hepatic and visceral adipose tissue is associated with metabolic disorders in morbidly obese patients.

Authors:  René Baudrand; Cristian A Carvajal; Arnoldo Riquelme; Mauricio Morales; Nancy Solis; Margarita Pizarro; Alex Escalona; Camilo Boza; Gustavo Pérez; Angélica Domínguez; Marco Arrese; Carlos E Fardella
Journal:  Obes Surg       Date:  2009-08-19       Impact factor: 4.129

8.  Impaired oxidoreduction by 11β-hydroxysteroid dehydrogenase 1 results in the accumulation of 7-oxolithocholic acid.

Authors:  Carlos A Penno; Stuart A Morgan; Anna Vuorinen; Daniela Schuster; Gareth G Lavery; Alex Odermatt
Journal:  J Lipid Res       Date:  2013-08-09       Impact factor: 5.922

9.  Hypothalamic-pituitary-adrenal axis abnormalities in response to deletion of 11beta-HSD1 is strain-dependent.

Authors:  R N Carter; J M Paterson; U Tworowska; D J Stenvers; J J Mullins; J R Seckl; M C Holmes
Journal:  J Neuroendocrinol       Date:  2009-07-07       Impact factor: 3.627

10.  Synergistic induction of local glucocorticoid generation by inflammatory cytokines and glucocorticoids: implications for inflammation associated bone loss.

Authors:  K Kaur; R Hardy; M M Ahasan; M Eijken; J P van Leeuwen; A Filer; A M Thomas; K Raza; C D Buckley; P M Stewart; E H Rabbitt; M Hewison; M S Cooper
Journal:  Ann Rheum Dis       Date:  2009-06-22       Impact factor: 19.103

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