Abstract
The peroxisome proliferator-activated receptor gamma (PPARγ), a member of the nuclear hormone receptor superfamily has classically been characterized for its implications in adipocyte differentiation and fat metabolism. Recently, PPARg has been implicated in the pathophysiology of inflammatory and immune responses possibly through inhibition of the mitogen-activated protein kinase (MAPK) pathways or the activation of the transcription nuclear factor kappa B (NF-κB). Thus, these agents might also have therapeutic potential in the treatment of gastrointestinal inflammatory disorders, such as ulcerative colitis and Crohns disease. The synthetic thiazolidinediones (TZDs), a novel class of insulin-sensitizing drugs, were the first class of compounds identified as PPARγ ligands, and represent a significant advance in anti-diabetic therapy. However, there is less information about endogenous ligands, although the prostaglandin (PG)J2 and the oxidized phosphatidylcholine have been suggested. Furthermore, PPARg ligands have been shown to be potent inhibitors of angiogenesis, a process necessary for tumor growth and metastasis, and protect against cellular transformation. Further work is needed to establish in detail the anti-proliferative and pro-differentiation mechanisms of PPARγ activators and their efficacy in certain cancers.
Keywords: pparg, thiazolidinedione, inflammation, diabetes, cancer
Current Pharmaceutical Design
Title: New Pharmacological Perspectives and Therapeutic Potential of PPAR-γ Agonists
Volume: 10 Issue: 28
Author(s): C. Alarcon de la Lastra, S. Sanchez-Fidalgo, I. Villegas and V. Motilva
Affiliation:
Keywords: pparg, thiazolidinedione, inflammation, diabetes, cancer
Abstract: The peroxisome proliferator-activated receptor gamma (PPARγ), a member of the nuclear hormone receptor superfamily has classically been characterized for its implications in adipocyte differentiation and fat metabolism. Recently, PPARg has been implicated in the pathophysiology of inflammatory and immune responses possibly through inhibition of the mitogen-activated protein kinase (MAPK) pathways or the activation of the transcription nuclear factor kappa B (NF-κB). Thus, these agents might also have therapeutic potential in the treatment of gastrointestinal inflammatory disorders, such as ulcerative colitis and Crohns disease. The synthetic thiazolidinediones (TZDs), a novel class of insulin-sensitizing drugs, were the first class of compounds identified as PPARγ ligands, and represent a significant advance in anti-diabetic therapy. However, there is less information about endogenous ligands, although the prostaglandin (PG)J2 and the oxidized phosphatidylcholine have been suggested. Furthermore, PPARg ligands have been shown to be potent inhibitors of angiogenesis, a process necessary for tumor growth and metastasis, and protect against cellular transformation. Further work is needed to establish in detail the anti-proliferative and pro-differentiation mechanisms of PPARγ activators and their efficacy in certain cancers.
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Cite this article as:
la Lastra Alarcon de C., Sanchez-Fidalgo S., Villegas I. and Motilva V., New Pharmacological Perspectives and Therapeutic Potential of PPAR-γ Agonists, Current Pharmaceutical Design 2004; 10 (28) . https://dx.doi.org/10.2174/1381612043382909
DOI https://dx.doi.org/10.2174/1381612043382909 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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