11β-Hydroxysteroid dehydrogenase 1: translational and therapeutic aspects

LL Gathercole, GG Lavery, SA Morgan… - Endocrine …, 2013 - academic.oup.com
Abstract 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) interconverts the inactive
glucocorticoid cortisone and its active form cortisol. It is widely expressed and, although …

11β-HSD1 inhibitors for the treatment of type 2 diabetes and cardiovascular disease

A Anderson, BR Walker - Drugs, 2013 - Springer
Inhibition of the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) has been
proposed as a novel therapeutic target for the treatment of type 2 diabetes mellitus. Over 170 …

The cardioprotective effects of mineralocorticoid receptor antagonists

TNA Van den Berg, GA Rongen, GM Fröhlich… - Pharmacology & …, 2014 - Elsevier
Despite state-of-the-art reperfusion therapy, morbidity and mortality remain significant in
patients with an acute myocardial infarction. Therefore, novel strategies to limit myocardial …

Modulation of 11β-hydroxysteroid dehydrogenase as a strategy to reduce vascular inflammation

PWF Hadoke, T Kipari, JR Seckl… - Current atherosclerosis …, 2013 - Springer
Atherosclerosis is a chronic inflammatory disease in which initial vascular damage leads to
extensive macrophage and lymphocyte infiltration. Although acutely glucocorticoids …

Cellular distribution and interaction between extended renin-angiotensin-aldosterone system pathways in atheroma

A Nehme, K Zibara - Atherosclerosis, 2017 - Elsevier
The importance of the renin-angiotensin-aldosterone system (RAAS) in the development of
atherosclerotic has been experimentally documented. In fact, RAAS components have been …

Transcriptome and molecular endocrinology aspects of epicardial adipose tissue in cardiovascular diseases: a systematic review and meta‐analysis of observational …

Z Maghbooli, A Hossein-Nezhad - BioMed research …, 2015 - Wiley Online Library
The objective of this study was to perform a systematic review of published literature on
differentially expressed genes (DEGs) in human epicardial adipose tissue (EAT) to identify …

The dehydrogenase hypothesis

C Woods, JW Tomlinson - … Signaling: From Molecules to Mice to Man, 2015 - Springer
Circulating glucocorticoid (GC) levels are controlled by the Hypothalamo–Pituitary–Adrenal
(HPA) axis, but within tissues, GC availability is controlled by the isoforms of 11β (Beta) …

Pro-inflammatory cytokine induction of 11β-hydroxysteroid dehydrogenase type 1 in A549 cells requires phosphorylation of C/EBPβ at Thr235

CL Esteves, M Verma, E Róg-Zielińska, V Kelly, S Sai… - PloS one, 2013 - journals.plos.org
11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) converts inert glucocorticoids into
active forms, thereby increasing intracellular glucocorticoid levels, important to restrain acute …

Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3′-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel …

XY Ye, SY Chen, S Wu, DS Yoon, H Wang… - Journal of Medicinal …, 2017 - ACS Publications
BMS-816336 (6n-2), a hydroxy-substituted adamantyl acetamide, has been identified as a
novel, potent inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β …

Cortisol metabolism as a regulator of the tissue-specifiC glucocorticoid action

E Sbardella, JW Tomlinson - The Hypothalamic-Pituitary-Adrenal Axis in …, 2017 - Springer
Glucocorticoids have a diverse array of functions affecting almost all tissues in the body.
While circulating cortisol levels are under the control of the hypothalamo–pituitary–adrenal …