Discovery of ligands for the nuclear peroxisome proliferator-activated receptors

The identification of high-affinity ligands for PPARγ has revealed the role of this receptor as the molecular target for the antidiabetic activity of the thiazolidinediones. The surprising observation that agonists of an adipogenic transcription factor reverse the obesity-associated disease of diabetes highlights the power of using potent and selective ligands to study receptor-mediated biology. Similarly, the observation that PGD₂ and its cyclopentenone metabolites compounds are μM PPAR ligands suggests that these receptors may have a physiological role in mediating prostaglandin signaling in the spleen.