Bicyclic Substituted Hydroxyphenylmethanone Type Inhibitors of 17 β-Hydroxysteroid Dehydrogenase Type 1 (17 β-HSD1): The Role of the Bicyclic Moiety

ChemMedChem ◽  
2011 ◽  
Vol 6 (3) ◽  
pp. 476-487 ◽  
Author(s):  
Alexander Oster ◽  
Tobias Klein ◽  
Claudia Henn ◽  
Ruth Werth ◽  
Sandrine Marchais-Oberwinkler ◽  
...  
Keyword(s):  
Hydroxysteroid Dehydrogenase

The role of hepatic 11[b]-hydroxysteroid dehydrogenase type 1 in cholesterol homeostasis

2013 ◽  
pp. 1-1
Author(s):  
Kajal Manwani ◽  
Tak Y Man ◽  
Christopher J Kenyon ◽  
Ruth Andrew ◽  
Karen E Chapman ◽  
...  
Keyword(s):  
Hydroxysteroid Dehydrogenase ◽  
Cholesterol Homeostasis

Role of 17β-hydroxysteroid dehydrogenase type 1 in endocrine and intracrine estradiol biosynthesis

1995 ◽  
Vol 55 (5-6) ◽  
pp. 525-532 ◽  
Author(s):  
Matti Poutanen ◽  
Veli Isomaa ◽  
Hellevi Peltoketo ◽  
Reijo Vihko
Keyword(s):  
Hydroxysteroid Dehydrogenase

scholarly journals Getting to the heart of intracellular glucocorticoid regeneration: 11β-HSD1 in the myocardium

2017 ◽  
Vol 58 (1) ◽  
pp. R1-R13 ◽  
Author(s):  
Gillian A Gray ◽  
Christopher I White ◽  
Raphael F P Castellan ◽  
Sara J McSweeney ◽  
Karen E Chapman
Keyword(s):  
Myocardial Infarction ◽  
Heart Failure ◽  
Systemic Corticosteroid ◽  
Physiological Function ◽  
Pressure Overload ◽  
Hydroxysteroid Dehydrogenase ◽  
And Function ◽  
Glucocorticoid Metabolism

Corticosteroids influence the development and function of the heart and its response to injury and pressure overload via actions on glucocorticoid (GR) and mineralocorticoid (MR) receptors. Systemic corticosteroid concentration depends largely on the activity of the hypothalamic–pituitary–adrenal (HPA) axis, but glucocorticoid can also be regenerated from intrinsically inert metabolites by the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), selectively increasing glucocorticoid levels within cells and tissues. Extensive studies have revealed the roles for glucocorticoid regeneration by 11β-HSD1 in liver, adipose, brain and other tissues, but until recently, there has been little focus on the heart. This article reviews the evidence for glucocorticoid metabolism by 11β-HSD1 in the heart and for a role of 11β-HSD1 activity in determining the myocardial growth and physiological function. We also consider the potential of 11β-HSD1 as a therapeutic target to enhance repair after myocardial infarction and to prevent the development of cardiac remodelling and heart failure.

scholarly journals The Role of Placental 11-Beta Hydroxysteroid Dehydrogenase Type 1 and Type 2 Methylation on Gene Expression and Infant Birth Weight1

2015 ◽  
Vol 92 (6) ◽  
Author(s):  
Benjamin B. Green ◽  
David A. Armstrong ◽  
Corina Lesseur ◽  
Alison G. Paquette ◽  
Dylan J. Guerin ◽  
...  
Keyword(s):  
Gene Expression ◽  
Hydroxysteroid Dehydrogenase ◽  
Infant Birth

Suppression of 11β-hydroxysteroid dehydrogenase type 1 with RNA interference substantially attenuates 3T3-L1 adipogenesis

2008 ◽  
Vol 32 (3) ◽  
pp. 343-351 ◽  
Author(s):  
Yong Liu ◽  
Frank Park ◽  
Jennifer L. Pietrusz ◽  
Guangfu Jia ◽  
Ravinder J. Singh ◽  
...  
Keyword(s):  
Functional Role ◽  
Glucocorticoid Receptors ◽  
Local Level ◽  
Hydroxysteroid Dehydrogenase ◽  
Marker Genes ◽  
Nucleotide Substitutions ◽  
Hairpin Rna ◽  
Induction Of Differentiation

11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1), which regulates the local level of glucocorticoids, has been suggested to be involved in the development of obesity. A definitive functional role for 11β-HSD1 in adipogenesis, however, remains to be established. We developed 3T3-L1 cell lines stably transfected with a small hairpin RNA (shRNA) targeting 11β-HSD1. A shRNA containing two nucleotide substitutions was used as a control. Silencing of 11β-HSD1 substantially attenuated the accumulation of lipid droplets and the expression of adipogenesis marker genes, which was induced by a mixture containing either corticosterone or dexamethasone. Silencing of 11β-HSD1 increased the concentration of 11-dehydrocorticosterone in the culture supernatant but did not significantly affect the levels of corticosterone or dexamethasone. Translocation of glucocorticoid receptors to the nucleus in response to glucocorticoids was significantly attenuated by silencing 11β-HSD1. The number of cells entering the S phase of the cell cycle following the induction of adipogenesis was significantly reduced by silencing 11β-HSD1. 11β-HSD1 shRNA delivered by lentiviral vectors after the induction of differentiation, however, did not affect the progression of adipogenesis. These results indicate that 11β-HSD1 plays a significant functional role in the initiation of 3T3-L1 adipogenesis and provide new mechanistic insights into the role of 11β-HSD1 in the development of obesity and related diseases.

Hypothalamic Regulation of Adiposity: The Role of 11β-Hydroxysteroid Dehydrogenase Type 1

2004 ◽  
Vol 36 (06) ◽  
pp. 365-369 ◽  
Author(s):  
Z. Hochberg ◽  
M. Friedberg ◽  
L. Yaniv ◽  
T. Bader ◽  
D. Tiosano
Keyword(s):  
Hydroxysteroid Dehydrogenase ◽  
Hypothalamic Regulation

scholarly journals The role of the heterocycle in bis(hydroxyphenyl)triazoles for inhibition of 17β-Hydroxysteroid Dehydrogenase (17β-HSD) type 1 and type 2

2009 ◽  
Vol 301 (1-2) ◽  
pp. 212-215 ◽  
Author(s):  
Yaseen A. Al-Soud ◽  
Emmanuel Bey ◽  
Alexander Oster ◽  
Sandrine Marchais-Oberwinkler ◽  
Ruth Werth ◽  
...  
Keyword(s):  
Hydroxysteroid Dehydrogenase
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