The syntheses of [13 C6 ] and [phenyl-14 C(U)]BMS-816336, an inhibitor of 11β-hydroxysteroid dehydrogenase type 1, for type 2 diabetes

2017 ◽  
Vol 60 (8) ◽  
pp. 357-365
Author(s):  
Brad D. Maxwell
Keyword(s):  
Type 2 Diabetes ◽  
Hydroxysteroid Dehydrogenase

scholarly journals 11?-Hydroxysteroid dehydrogenase Type 1 in obesity and Type 2 diabetes

Diabetologia ◽  
2004 ◽  
Vol 47 (1) ◽  
pp. 1-11 ◽  
Author(s):  
T. M. Stulnig ◽  
W. Waldh�usl
Keyword(s):  
Type 2 Diabetes ◽  
Hydroxysteroid Dehydrogenase

scholarly journals Relationship of 11β-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase gene polymorphisms with metabolic syndrome and type 2 diabetes

2011 ◽  
Vol 58 (11) ◽  
pp. 949-959 ◽  
Author(s):  
Seong-Su Moon ◽  
Young-Sil Lee ◽  
Jung-Guk Kim ◽  
Su-Won Kim ◽  
Ji-Yun Jeong ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Metabolic Syndrome ◽  
Gene Polymorphisms ◽  
Hydroxysteroid Dehydrogenase ◽  
Dehydrogenase Gene ◽  
Relationship Of

scholarly journals The 11- -Hydroxysteroid Dehydrogenase Type 1 Inhibitor INCB13739 Improves Hyperglycemia in Patients With Type 2 Diabetes Inadequately Controlled by Metformin Monotherapy

Diabetes Care ◽  
2010 ◽  
Vol 33 (7) ◽  
pp. 1516-1522 ◽  
Author(s):  
J. Rosenstock ◽  
S. Banarer ◽  
V. A. Fonseca ◽  
S. E. Inzucchi ◽  
W. Sun ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Hydroxysteroid Dehydrogenase ◽  
Metformin Monotherapy

scholarly journals Increased Whole-Body and Sustained Liver Cortisol Regeneration by 11β-Hydroxysteroid Dehydrogenase Type 1 in Obese Men With Type 2 Diabetes Provides a Target for Enzyme Inhibition

Diabetes ◽  
2011 ◽  
Vol 60 (3) ◽  
pp. 720-725 ◽  
Author(s):  
Roland H. Stimson ◽  
Ruth Andrew ◽  
Norma C. McAvoy ◽  
Dhiraj Tripathi ◽  
Peter C. Hayes ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Enzyme Inhibition ◽  
Hydroxysteroid Dehydrogenase ◽  
Whole Body

scholarly journals Functional Effects of Polymorphisms in the Human Gene Encoding 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1): A Sequence Variant at the Translation Start of 11β-HSD1 Alters Enzyme Levels

Endocrinology ◽  
2010 ◽  
Vol 151 (1) ◽  
pp. 195-202 ◽  
Author(s):  
Elise L. V. Malavasi ◽  
Val Kelly ◽  
Nikita Nath ◽  
Alessandra Gambineri ◽  
Rachel S. Dakin ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Hydroxysteroid Dehydrogenase ◽  
In Vitro Translation ◽  
Metabolic Phenotype ◽  
Sequence Variant ◽  
Gene Encoding ◽  
Functional Consequences

Abstract Regeneration of active glucocorticoids within liver and adipose tissue by the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) may be of pathophysiological importance in obesity and metabolic syndrome and is a therapeutic target in type 2 diabetes. Polymorphisms in HSD11B1, the gene encoding 11β-HSD1, have been associated with metabolic phenotype in humans, including type 2 diabetes and hypertension. Here, we have tested the functional consequences of two single nucleotide polymorphisms located in contexts that potentially affect tissue levels of 11β-HSD1. We report no effect of allelic variation at rs846910, a polymorphism within the 5′-flanking region of the gene on HSD11B1 promoter activity in vitro. However, compared with the common G allele, the A allele of rs13306421, a polymorphism located two nucleotides 5′ to the translation initiation site, gave higher 11β-HSD1 expression and activity in vitro and was translated at higher levels in in vitro translation reactions, possibly associated with a lower frequency of “leaky scanning.” These data suggest that this polymorphism may have direct functional consequences on levels of 11β-HSD1 enzyme activity in vivo. However, the rs13306421 A sequence variant originally reported in other ethnic groups may be of low prevalence because it was not detected in a population of 600 European Caucasian women.

scholarly journals Association of 11beta-hydroxysteroid dehydrogenase type 1 (HSD11B1) gene polymorphism with Type 2 Diabetes Mellitus in a sample Egyptian Population

2021 ◽  
Vol 83 (1) ◽  
pp. 1050-1055
Author(s):  
Salah Hussein Elhalawany ◽  
, Raef Malak Botros ◽  
Laila Mahmoud Ali Hendawy ◽  
Eman Mohamed Eman Mohamed Fahmy ◽  
Alaa Tarek Younis
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Gene Polymorphism ◽  
Hydroxysteroid Dehydrogenase ◽  
Egyptian Population
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