Abstract
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.
Keywords: ppar Ligands, ppar family, thiazolidinediones, peroxisome proliferator activated receptor, metabolic disorders
Current Topics in Medicinal Chemistry
Title: PPAR Ligands for Metabolic Disorders
Volume: 3 Issue: 14
Author(s): Garret J. Etgen and Nathan Mantlo
Affiliation:
Keywords: ppar Ligands, ppar family, thiazolidinediones, peroxisome proliferator activated receptor, metabolic disorders
Abstract: 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.
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Cite this article as:
Etgen J. Garret and Mantlo Nathan, PPAR Ligands for Metabolic Disorders, Current Topics in Medicinal Chemistry 2003; 3 (14) . https://dx.doi.org/10.2174/1568026033451673
| DOI https://dx.doi.org/10.2174/1568026033451673 |
Print ISSN 1568-0266 |
| Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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