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David P Marciano, Dana S Kuruvilla, Siddaraju V Boregowda, Alice Asteian, Travis S Hughes, Ruben Garcia-Ordonez, Cesar A Corzo, Tanya M Khan, Scott J Novick, HaJeung Park, Douglas J Kojetin, Donald G Phinney, John B Bruning, Theodore M Kamenecka, Patrick R Griffin
The nuclear receptor peroxisome proliferator-activated receptor gamma (PPARγ) is the master regulator of adipogenesis and the pharmacological target of the thiazolidinedione (TZD) class of insulin sensitizers. Activation of PPARγ by TZDs promotes adipogenesis at the expense of osteoblast formation, contributing to their associated adverse effects on bone. Recently, we reported the development of PPARγ antagonist SR1664, designed to block the obesity-induced phosphorylation of serine 273 (S273) in the absence of classical agonism, to derive insulin-sensitizing efficacy with improved therapeutic index...
2015: Nature Communications
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