Literature DB >> 23659858

Evaluation of selective inhibitors of 11β-HSD1 for the treatment of hypertension.

David R Bauman1, Alan Whitehead, Lisa C Contino, Jisong Cui, Margarita Garcia-Calvo, Xin Gu, Nancy Kevin, Xiuying Ma, Lee-yuh Pai, Kashmira Shah, Xiaolan Shen, Sloan Stribling, Hratch J Zokian, Joe Metzger, Diane E Shevell, Sherman T Waddell.   

Abstract

In an effort to understand the origin of blood-pressure lowering effects observed in recent clinical trials with 11β-HSD1 inhibitors, we examined a set of 11β-HSD1 inhibitors in a series of relevant in vitro and in vivo assays. Select 11β-HSD1 inhibitors reduced blood pressure in our preclinical models but most or all of the blood pressure lowering may be mediated by a 11β-HSD1 independent pathway.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23659858     DOI: 10.1016/j.bmcl.2013.03.011

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).

Authors:  Jun Li; Lawrence J Kennedy; Haixia Wang; James J Li; Steven J Walker; Zhenqiu Hong; Stephen P O'Connor; Akbar Nayeem; Daniel M Camac; Paul E Morin; Steven Sheriff; Mengmeng Wang; Timothy Harper; Rajasree Golla; Ramakrishna Seethala; Thomas Harrity; Randolph P Ponticiello; Nathan N Morgan; Joseph R Taylor; Rachel Zebo; David A Gordon; Jeffrey A Robl
Journal:  ACS Med Chem Lett       Date:  2014-05-22       Impact factor: 4.345

Review 2.  11β-Hydroxysteroid Dehydrogenases and Hypertension in the Metabolic Syndrome.

Authors:  Matthew A Bailey
Journal:  Curr Hypertens Rep       Date:  2017-11-14       Impact factor: 5.369

Review 3.  Glucocorticoids and renal Na+ transport: implications for hypertension and salt sensitivity.

Authors:  Robert W Hunter; Jessica R Ivy; Matthew A Bailey
Journal:  J Physiol       Date:  2014-02-17       Impact factor: 5.182

4.  11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors still improve metabolic phenotype in male 11β-HSD1 knockout mice suggesting off-target mechanisms.

Authors:  Erika Harno; Elizabeth C Cottrell; Alice Yu; Joanne DeSchoolmeester; Pablo Morentin Gutierrez; Mark Denn; John G Swales; Fred W Goldberg; Mohammad Bohlooly-Y; Harriet Andersén; Martin J Wild; Andrew V Turnbull; Brendan Leighton; Anne White
Journal:  Endocrinology       Date:  2013-10-29       Impact factor: 4.736

  4 in total

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