Article
11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors still improve metabolic phenotype in male 11β-HSD1 knockout mice suggesting off-target mechanisms.
Endocrinology - 1 Dec 2013
Harno Erika, Cottrell Elizabeth C, Yu Alice, DeSchoolmeester Joanne, Gutierrez Pablo Morentin, Denn Mark, Swales John G, Goldberg Fred W, Bohlooly-Y Mohammad, Andersén Harriet, Wild Martin J, Turnbull Andrew V, Leighton Brendan, White Anne
Abstract excerpt
The enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is a target for novel type 2 diabetes and obesity therapies based on the premise that lowering of tissue glucocorticoids will have positive effects on body weight, glycemic control, and insulin sensitivity. An 11β-HSD1 inhibitor (compound C) inhibited liver 11β-HSD1 by >90% but led to only small improvements in metabolic parameters in high-fat diet...
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