PPAR ligands for metabolic disorders.
As master regulators of lipid metabolism the peroxisome proliferator activated receptor (PPAR) family controls a wide variety of cellular processes, and thus it is not surprising that a large effort has focussed on discovering agents to pharmacologically modulate activity of these receptors. Early generation PPAR ligands, such as the fibrates and the thiazolidinediones (TZDs), were discovered empirically through an in vivo structure activity relationship exercise, whereas currently PPAR ligands are more often identified through target based structural design using cloned and expressed receptors. Regardless of how they were discovered, the development and clinical use of PPAR ligands throughout the last decade has greatly advanced understanding of the physiological function and therapeutic value of modulating these receptors. This review will briefly examine the PPAR family and then outline in greater detail select PPAR ligands indicated for the treatment of metabolic disorders.
Etgen
Garret J
GJ
Lilly Research Laboratories, A Division of Eli Lilly & Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
Mantlo
Nathan
N
D000818:Animals; D006801:Humans; D008024:Ligands; D008659:Metabolic Diseases / Q000188:drug therapy* / Q000378:metabolism; D008958:Models, Molecular; D015394:Molecular Structure; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000502:physiology; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000502:physiology
D008024:Ligands; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors