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Open AccessJournal ArticleDOI

Discovery of novel inhibitors of human 11β-hydroxysteroid dehydrogenase type 1

Xiangdong Su, +5 more
- 25 Mar 2009 - 
- Vol. 301, Iss: 1, pp 169-173
TLDR
In this paper, a series of adamantyl carboxamides were used as selective inhibitors of human 11β-hydroxysteroid dehydrogenases (11β-HSDs) in HEK-293 cells transfected with the HSD11B1 gene.
About: 
This article is published in Molecular and Cellular Endocrinology.The article was published on 2009-03-25 and is currently open access. It has received 19 citations till now. The article focuses on the topics: 11β-hydroxysteroid dehydrogenase type 1 & Hydroxysteroid dehydrogenase.

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Advances in the treatment of type 2 diabetes mellitus.

Zafar H Israili
- 01 Mar 2011 - 
TL;DR: A comprehensive and up-to-date information on the mechanism(s) of action, efficacy, pharmacokinetics, pleiotropic effects, drug interactions, and adverse effects of the newer antidiabetic drugs, including (1) peroxisome proliferator-activated-receptor-γ agonists (thiazolidinediones, pioglitazone, and rosiglitaze), (2) the incretin-mimetics, exenatide. and liraglutide), (3) inhibitors of di
Journal ArticleDOI

Medicinal Chemistry of Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)

James S. Scott, +2 more
- 12 Jun 2014 - 
TL;DR: The aim of this article is to review the medicinal chemistry literature around small molecule approaches to developing synthetic inhibitors of 11β-HSD1 and to highlight key compounds that have resulted from the efforts of both industrial and academic groups.
Journal ArticleDOI

Diabetes mellitus: new challenges and innovative therapies

Cristina M. Sena, +3 more
- 13 Mar 2010 - 
TL;DR: Treatment of diabetes faces now a new era that is characterized by a variety of innovative therapeutic approaches that will improve quality-life and allow personalized therapy-planning in the near future.
Journal ArticleDOI

Therapeutic targets to reduce cardiovascular disease in type 2 diabetes

Cyrus Desouza, +1 more
- 01 May 2009 - 
TL;DR: The background to and the implications of recent regulatory guidance on the development of new drugs for diabetes are reviewed, and the potential cardiovascular effects of selected classes of diabetes drugs that are currently being investigated are discussed.
Journal ArticleDOI

CaL-B a highly selective biocatalyst for the kinetic resolution of furylbenzthiazole-2-yl-ethanols and acetates

László Csaba Bencze, +4 more
- 23 Aug 2010 - 
TL;DR: In this paper, a highly stereoselective kinetic resolution of novel substituted racemic furylbenzthiazole-2-yl-ethanols and their acetates has been developed.
References
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Journal ArticleDOI

The Protein Data Bank

Helen M. Berman, +7 more
- 01 Jan 2000 - 
TL;DR: The goals of the PDB are described, the systems in place for data deposition and access, how to obtain further information and plans for the future development of the resource are described.
Journal ArticleDOI

11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response.

Jeremy W. Tomlinson, +7 more
- 01 Oct 2004 - 
TL;DR: It is speculated that hexose-6-phosphate dehydrogenase activity and therefore reduced nicotinamide-adenine dinucleotide phosphate supply may be crucial in determining the directionality of 11beta-HSD1 activity.
Journal ArticleDOI

11β-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice

Anne Hermanowski-Vosatka, +26 more
- 15 Aug 2005 - 
TL;DR: These data provide the first evidence that pharmacologic inhibition of intracellular GC activation can effectively treat atherosclerosis, the key clinical consequence of metabolic syndrome, in addition to its salutary effect on multiple aspects of the metabolic syndrome itself.
Journal ArticleDOI

Carbenoxolone increases hepatic insulin sensitivity in man: a novel role for 11-oxosteroid reductase in enhancing glucocorticoid receptor activation.

Brian R. Walker, +4 more
- 01 Nov 1995 - 
TL;DR: It is inferred that carbenoxolone, by inhibiting hepatic 11 beta-reductase and reducing intrahepatic cortisol concentration, increases hepatic insulin sensitivity and decreases glucose production, and plasma cortisone provides an inactive pool that can be converted to active glucocorticoids at sites where 11 Beta-Reductase is expressed.
Journal ArticleDOI

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

Katherine Hughes, +2 more
- 25 Mar 2008 - 
TL;DR: This article focuses on the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1), which amplifies glucocorticoid concentrations in key metabolic tissues including liver and adipose tissue and discusses the properties of the class leaders and their potential as the next generation of drugs with multiple benefits in metabolic syndrome.
Related Papers (5)

The 11-Beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitor INCB13739 Improves Hyperglycemia in Patients with Type 2 Diabetes Inadequately Controlled By Metformin Monotherapy

Julio Rosenstock, +11 more
- 01 Jul 2010 - 

Inhibitors of 17β-hydroxysteroid dehydrogenase type 1, 2 and 14: Structures, biological activities and future challenges.

Mohamed Salah, +2 more
- 01 Jun 2019 - 

A challenge for medicinal chemistry by the 17β-hydroxysteroid dehydrogenase superfamily: an integrated biological function and inhibition study.

S.-X. Lin, +2 more
- 01 May 2013 - 

11β-Hydroxysteroid dehydrogenase 1: Regeneration of active glucocorticoids is only part of the story.

Alex Odermatt, +1 more
- 01 Jul 2015 - 

Discovery of a novel enzyme mediating glucocorticoid catabolism in fish: 20beta-hydroxysteroid dehydrogenase type 2.

Janina Tokarz, +5 more
Frequently Asked Questions (1)
Q1. What are the contributions mentioned in the paper "Discovery of novel inhibitors of human 11β-hydroxysteroid dehydrogenase type 1" ?

Here the authors report the discovery of a series of novel adamantyl carboxamides as selective inhibitors of human 11β-HSD1 in HEK-293 cells transfected with the HSD11B1 gene.