Structural Insight into PPARγ Activation Through Covalent Modification with Endogenous Fatty Acids

Peroxisome proliferator-activated receptor (PPAR) γ is a nuclear receptor that regulates lipid homeostasis, and several fatty acid metabolites have been identified as PPARγ ligands. Here, we present four crystal structures of the PPARγ ligand binding domain (LBD) covalently bound to endogenous fatty acids via a unique cysteine, which is reportedly critical for receptor activation. The structure analyses of the LBD complexed with...