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Vinh Q Lam, Jie Zheng, Patrick R Griffin
The nuclear receptor PPARγ regulates adipogenesis and plays a central role in lipid and glucose homeostasis, and is the molecular target of the glitazones (TZDs), therapeutics used to treat insulin resistance and type-2 diabetes (T2D). Although the TZDs, which are PPARγ agonists, demonstrated robust clinical efficacy in T2D, their use has been hampered by an array of untoward side effects. Paradoxically, partial agonists ( e.g. MRL24), antagonists ( e.g. SR1664), and inverse agonists ( e.g. SR10171 and SR2595), possess similar insulin-sensitizing efficacy as the TZDs in obese diabetic mice...
December 2017: Molecular & Cellular Proteomics: MCP
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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