Willson T M, Lehmann J M, Kliewer S A
Department of Medicinal Chemistry, Glaxo Research Institute, Research Triangle Park, North Carolina 27709, USA.
Ann N Y Acad Sci. 1996 Dec 27;804:276-83. doi: 10.1111/j.1749-6632.1996.tb18622.x.
The identification of high-affinity ligands for PPAR gamma 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 microM PPAR ligands suggests that these receptors may have a physiological role in mediating prostaglandin signaling in the spleen.
