Abstract
Peroxisome proliferator-activated receptors (PPARs) alpha, gamma and delta (beta) are ligandactivated transcription factors of the nuclear hormone receptor superfamily which have been shown to play key roles in maintaining glucose and lipid homeostasis. The physiological effects of several marketed drugs for the treatment of dyslipidemia (fenofibrate and gemfibrozil) and diabetes (rosiglitazone and pioglitazone) have now been shown to be mediated through PPARalpha and PPARgamma respectively. Over the past few years our understanding of how PPAR ligands and receptors modulate gene expression has greatly increased; this knowledge is being used to design even more potent and efficacious PPAR ligands for the treatment of diabetes, dyslipidemia, atherosclerosis and obesity. This review is a brief survey of the PPAR field which highlights recent progress, with an emphasis on new ligands with novel PPAR profiles, particularly compounds which are co-agonists of PPAa, g and b (d).
Keywords: transcription factors, nuclear hormone receptor, ppar isoforms, retinoid x receptors, gluconeogenesis, knockout mice, signaling pathway, transrepression
Mini-Reviews in Medicinal Chemistry
Title: PPARs as Targets for Metabolic and Cardiovascular Diseases
Volume: 5 Issue: 8
Author(s): Peter T.W. Cheng and Ranjan Mukherjee
Affiliation:
Keywords: transcription factors, nuclear hormone receptor, ppar isoforms, retinoid x receptors, gluconeogenesis, knockout mice, signaling pathway, transrepression
Abstract: Peroxisome proliferator-activated receptors (PPARs) alpha, gamma and delta (beta) are ligandactivated transcription factors of the nuclear hormone receptor superfamily which have been shown to play key roles in maintaining glucose and lipid homeostasis. The physiological effects of several marketed drugs for the treatment of dyslipidemia (fenofibrate and gemfibrozil) and diabetes (rosiglitazone and pioglitazone) have now been shown to be mediated through PPARalpha and PPARgamma respectively. Over the past few years our understanding of how PPAR ligands and receptors modulate gene expression has greatly increased; this knowledge is being used to design even more potent and efficacious PPAR ligands for the treatment of diabetes, dyslipidemia, atherosclerosis and obesity. This review is a brief survey of the PPAR field which highlights recent progress, with an emphasis on new ligands with novel PPAR profiles, particularly compounds which are co-agonists of PPAa, g and b (d).
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Cite this article as:
Cheng T.W. Peter and Mukherjee Ranjan, PPARs as Targets for Metabolic and Cardiovascular Diseases, Mini-Reviews in Medicinal Chemistry 2005; 5 (8) . https://dx.doi.org/10.2174/1389557054553758
DOI https://dx.doi.org/10.2174/1389557054553758 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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