Literature DB >> 16181035

Inhibition of 11beta-HSD1 as a novel treatment for the metabolic syndrome: do glucocorticoids play a role?

Rolf Thieringer1, Anne Hermanowski-Vosatka.   

Abstract

The metabolic syndrome (syndrome X) is a cluster of risk factors and a common cause of cardiovascular disease in humans. Although the underlying mechanism for metabolic syndrome is still poorly understood, recent clinical data and studies with transgenic animals implicate elevated intracellular glucocorticoid tone in the etiology of metabolic syndrome. Development of selective inhibitors of 11beta-hydroxysteroid dehydrogenase (11beta-HSD)-1 and their use in rodent animal disease models encompassing several aspects of metabolic syndrome indicate the possibility of therapeutic intervention. This review will focus on recent advances in our understanding of the role of 11beta-HSD1 in metabolic disorders and other disease processes.

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 16181035     DOI: 10.1586/14779072.3.5.911

Source DB:  PubMed          Journal:  Expert Rev Cardiovasc Ther        ISSN: 1477-9072


  9 in total

Review 1.  11beta-HSD1, inflammation, metabolic disease and age-related cognitive (dys)function.

Authors:  Karen E Chapman; Jonathan R Seckl
Journal:  Neurochem Res       Date:  2007-10-25       Impact factor: 3.996

2.  Synthesis, in Vitro Covalent Binding Evaluation, and Metabolism of (14)C-Labeled Inhibitors of 11β-HSD1.

Authors:  Daqing Sun; Qiuping Ye; Xuelei Yan; Yosup Rew; Peter Fan; Xiao He; Min Jiang; Dustin L McMinn; Mario Monshouwer; Hua Tu; Jay P Powers
Journal:  ACS Med Chem Lett       Date:  2014-09-23       Impact factor: 4.345

3.  Pharmacokinetic-pharmacodynamic studies of the 11β-hydroxysteroid dehydrogenase type 1 inhibitor MK-0916 in healthy subjects.

Authors:  D Hamish Wright; Julie A Stone; Tami M Crumley; Larissa Wenning; Wei Zheng; Kerri Yan; Amy Yifan Yang; Li Sun; Caroline Cilissen; Steven Ramael; Anne Hermanowski-Vosatka; Ronald B Langdon; Keith M Gottesdiener; John A Wagner; Eseng Lai
Journal:  Br J Clin Pharmacol       Date:  2013-12       Impact factor: 4.335

4.  A novel NADP(+)-dependent dehydrogenase activity for 7alpha/beta- and 11beta-hydroxysteroids in human liver nuclei: A third 11beta-hydroxysteroid dehydrogenase.

Authors:  B Robinzon; R A Prough
Journal:  Arch Biochem Biophys       Date:  2009-05-03       Impact factor: 4.013

5.  Discovery of adamantyl heterocyclic ketones as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors.

Authors:  Xiangdong Su; Nigel Vicker; Mark P Thomas; Fabienne Pradaux-Caggiano; Heather Halem; Michael D Culler; Barry V L Potter
Journal:  ChemMedChem       Date:  2011-05-23       Impact factor: 3.466

6.  Adamantyl ethanone pyridyl derivatives: potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1.

Authors:  Xiangdong Su; Fabienne Pradaux-Caggiano; Nigel Vicker; Mark P Thomas; Heather Halem; Michael D Culler; Barry V L Potter
Journal:  ChemMedChem       Date:  2011-06-28       Impact factor: 3.466

7.  Zuogui Jiangtang Jieyu Formulation Prevents Hyperglycaemia and Depressive-Like Behaviour in Rats by Reducing the Glucocorticoid Level in Plasma and Hippocampus.

Authors:  YuHong Wang; Hui Yang; Wei Li; Pan Meng; YuanShan Han; Xiuli Zhang; DeLiang Cao; Yuansheng Tan
Journal:  Evid Based Complement Alternat Med       Date:  2015-07-27       Impact factor: 2.629

8.  Adamantyl carboxamides and acetamides as potent human 11β-hydroxysteroid dehydrogenase type 1 inhibitors.

Authors:  Xiangdong Su; Heather A Halem; Mark P Thomas; Cecile Moutrille; Michael D Culler; Nigel Vicker; Barry V L Potter
Journal:  Bioorg Med Chem       Date:  2012-09-12       Impact factor: 3.641

Review 9.  The scientific impact of the Structural Genomics Consortium: a protein family and ligand-centered approach to medically-relevant human proteins.

Authors:  Opher Gileadi; Stefan Knapp; Wen Hwa Lee; Brian D Marsden; Susanne Müller; Frank H Niesen; Kathryn L Kavanagh; Linda J Ball; Frank von Delft; Declan A Doyle; Udo C T Oppermann; Michael Sundström
Journal:  J Struct Funct Genomics       Date:  2007-10-12
  9 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.