Abstract
Peroxisome proliferator-activated receptors (PPARs) are ligand dependent transcription factors. The three mammalian PPARs are key regulators of fatty acid and lipoprotein metabolism, glucose homeostasis, cellular proliferation/ differentiation and the immune response. PPARs are therefore important targets in the treatment of metabolic disorders such as insulin resistance and type 2 diabetes mellitus, and are also of interest in relation to chronic inflammatory diseases such as atherosclerosis, arthritis, chronic pulmonary inflammation, pancreatitis, inflammatory bowel disease, and psoriasis. Recent advances have attributed novel functions to PPARs in blood pressure regulation, neuroinflammation, nerve-cell protection, inflammatory pain reduction, and the hypothalamic control of metabolism. The abundant pleiotropic actions of PPARs suggest that PPAR agonists have enormous therapeutic potential. However, current PPAR-based therapies often have undesired side effects due to the concomitant activation of PPARs in non-target cells. There is therefore growing interest in the development of cell-specific PPAR agonists and improvement of the clinical use of PPAR ligands. This review gives an overview of PPAR functions and discusses the current and potential medical implications of PPAR ligands in various pathologies, ranging from metabolic disorders to cardiovascular disease, chronic inflammation, neurodegenerative disorders and cancer.
Keywords: Nuclear receptors, PPAR, transcription, metabolism, inflammation, cardiovascular disease, neuroinflammation, cancer, lipoprotein metabolism, glucose homeostasis, insulin resistance, type 2 diabetes mellitus, atherosclerosis, arthritis, chronic pulmonary inflammation, inflammatory bowel disease
Current Topics in Medicinal Chemistry
Title: Biology and Therapeutic Applications of Peroxisome Proliferator- Activated Receptors
Volume: 12 Issue: 6
Author(s): Maria P. Menendez-Gutierrez, Tamas Roszer and Mercedes Ricote
Affiliation:
Keywords: Nuclear receptors, PPAR, transcription, metabolism, inflammation, cardiovascular disease, neuroinflammation, cancer, lipoprotein metabolism, glucose homeostasis, insulin resistance, type 2 diabetes mellitus, atherosclerosis, arthritis, chronic pulmonary inflammation, inflammatory bowel disease
Abstract: Peroxisome proliferator-activated receptors (PPARs) are ligand dependent transcription factors. The three mammalian PPARs are key regulators of fatty acid and lipoprotein metabolism, glucose homeostasis, cellular proliferation/ differentiation and the immune response. PPARs are therefore important targets in the treatment of metabolic disorders such as insulin resistance and type 2 diabetes mellitus, and are also of interest in relation to chronic inflammatory diseases such as atherosclerosis, arthritis, chronic pulmonary inflammation, pancreatitis, inflammatory bowel disease, and psoriasis. Recent advances have attributed novel functions to PPARs in blood pressure regulation, neuroinflammation, nerve-cell protection, inflammatory pain reduction, and the hypothalamic control of metabolism. The abundant pleiotropic actions of PPARs suggest that PPAR agonists have enormous therapeutic potential. However, current PPAR-based therapies often have undesired side effects due to the concomitant activation of PPARs in non-target cells. There is therefore growing interest in the development of cell-specific PPAR agonists and improvement of the clinical use of PPAR ligands. This review gives an overview of PPAR functions and discusses the current and potential medical implications of PPAR ligands in various pathologies, ranging from metabolic disorders to cardiovascular disease, chronic inflammation, neurodegenerative disorders and cancer.
Export Options
About this article
Cite this article as:
P. Menendez-Gutierrez Maria, Roszer Tamas and Ricote Mercedes, Biology and Therapeutic Applications of Peroxisome Proliferator- Activated Receptors, Current Topics in Medicinal Chemistry 2012; 12 (6) . https://dx.doi.org/10.2174/156802612799436669
DOI https://dx.doi.org/10.2174/156802612799436669 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Reactive Oxygen Species in Vascular Wall
Cardiovascular & Hematological Disorders-Drug Targets Assessment of Glomerular and Tubular Function
Current Pediatric Reviews Coronary Pressure Measurement Based Decision Making for Percutaneous Coronary Intervention
Current Cardiology Reviews Imidazoline Receptor Agonists in Obesity-Related Hypertension: Therapeutic Targeting of the Sympathetic Nervous System
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Early-life Programming of Type 2 Diabetes Mellitus: Understanding the Association between Epigenetics/Genetics and Environmental Factors
Current Genomics Surrogates of Insulin Sensitivity and Indices of Cardiometabolic Profile in Obesity
Current Vascular Pharmacology Hypertriglyceridemia: An Infrequent, Difficult-to-predict, Severe Metabolic and Vascular Problem Associated with Estrogen Administration
Current Vascular Pharmacology Unmet Needs in Schizophrenia
CNS & Neurological Disorders - Drug Targets Biomarkers of Oxidative Stress and Cataract. Novel Drug Delivery Therapeutic Strategies Targeting Telomere Reduction and the Expression of Telomerase Activity in the Lens Epithelial Cells with N-Acetylcarnosine Lubricant Eye Drops: Anti-Cataract which Helps to Prevent and Treat Cataracts in the Eyes of Dogs and other Animals
Current Drug Delivery Synchronized Fast SPE and UFLC Methods for the Analyses of Eight Antidiabetic Drugs in Human Plasma
Combinatorial Chemistry & High Throughput Screening Reduction of Myocardial Ischemia-Reperfusion Injury with Pre- and Postconditioning: Molecular Mechanisms and Therapeutic Targets
Cardiovascular & Hematological Disorders-Drug Targets Type 2 Diabetes, Insulin Secretion and β-Cell Mass
Current Molecular Medicine Recent Medicinal Chemistry Studies for Multitarget Agents-Part II
Current Drug Targets Sex Steroids Regulation of Appetitive Behavior
Mini-Reviews in Medicinal Chemistry ABT-450: A Novel Protease Inhibitor for the Treatment of Hepatitis C Virus Infection
Current Medicinal Chemistry New Concept of Vascular Calcification and Metabolism
Current Vascular Pharmacology Evaluation of the Effect of Nimodipine o.d. (Extended Release) vs Nimodipine t.i.d. in the Treatment of Peripheral Vertigo
Current Drug Delivery “Something is Wrong in the Ras Kingdom” - Evidence for the Involvement of p21Ras/MAP Kinase in Autoimmune Diseases
Current Rheumatology Reviews T-Regulatory Cell Subsets in Children with Type 1 Diabetes Mellitus: Relation to Control of the Disease
Endocrine, Metabolic & Immune Disorders - Drug Targets Overview of Hyperuricaemia and Gout
Current Pharmaceutical Design