Medium Chain Fatty Acids Are Selective Peroxisome Proliferator Activated Receptor (PPAR) γ Activators and Pan-PPAR Partial Agonists

@inproceedings{Liberato2012MediumCF,
  title={Medium Chain Fatty Acids Are Selective Peroxisome Proliferator Activated Receptor (PPAR) γ Activators and Pan-PPAR Partial Agonists},
  author={Marcelo Vizona Liberato and Alessandro S. Nascimento and Steven D. Ayers and Jean Z H Lin and Aleksandra Cvoro and Rodrigo L. Silveira and Leandro Mart{\'i}nez and Paulo Cesar Telles de Souza and Daniel Menezes Saidemberg and Tuo Deng and Angela Angelica Amato and Marie Togashi and Willa A. Hsueh and Kevin D Phillips and Mario Sergio Palma and Francisco de Assis Rocha Neves and Munir S. Skaf and Paul D. Webb and Igor Polikarpov},
  booktitle={PloS one},
  year={2012}
}
Thiazolidinediones (TZDs) act through peroxisome proliferator activated receptor (PPAR) γ to increase insulin sensitivity in type 2 diabetes (T2DM), but deleterious effects of these ligands mean that selective modulators with improved clinical profiles are needed. We obtained a crystal structure of PPARγ ligand binding domain (LBD) and found that the ligand binding pocket (LBP) is occupied by bacterial medium chain fatty acids (MCFAs). We verified that MCFAs (C8-C10) bind the PPARγ LBD in vitro… CONTINUE READING