Abstract
Peroxisome proliferator-activated receptor-γ (PPAR-γ) is a nuclear transcription factor which is involved in the differentiation of fibroblasts to adipocytes in vitro. PPAR-γ also plays a pivotal role in inflammation and macrophage activation. Furthermore, type 2 diabetes mellitus (T2DM), a condition in which an individual's ability to respond to insulin is lowered, is treated by drugs called thiazolidinediones (TZDs) that are known to activated PPAR-γ, thus augmenting insulin signaling and glucose uptake by adipose tissue. Unfortunately, these otherwise effective drugs are responsible for side effects such as obesity and cardiovascular diseases. The ligand-binding ability of PPAR-γ is different from other nuclear receptors since it can bind to a wide variety of ligands. Although a number of compounds have been shown to activate PPAR-γ, knowledge of its endogenous ligands and their physiological functions is lacking. The known ligands were either ambiguous or found to produce ill effects in vivo. In this review we discuss the structure and functions of PPAR-γ, ligands discovered so far, and focus on the importance of identification of physiologically relevant endogenous ligands.
Keywords: Adipogenesis, endogenous ligands, inflammation, macrophage, PPAR-γ, thiazolidinediones, type 2 diabetes.
Endocrine, Metabolic & Immune Disorders - Drug Targets
Title:The Need for Physiologically Relevant Peroxisome Proliferator-Activated Receptor-gamma (PPAR-γ) Ligands
Volume: 13 Issue: 2
Author(s): Parasuraman Aiya Subramani, Madhava C. Reddy and Venkata R. Narala
Affiliation:
Keywords: Adipogenesis, endogenous ligands, inflammation, macrophage, PPAR-γ, thiazolidinediones, type 2 diabetes.
Abstract: Peroxisome proliferator-activated receptor-γ (PPAR-γ) is a nuclear transcription factor which is involved in the differentiation of fibroblasts to adipocytes in vitro. PPAR-γ also plays a pivotal role in inflammation and macrophage activation. Furthermore, type 2 diabetes mellitus (T2DM), a condition in which an individual's ability to respond to insulin is lowered, is treated by drugs called thiazolidinediones (TZDs) that are known to activated PPAR-γ, thus augmenting insulin signaling and glucose uptake by adipose tissue. Unfortunately, these otherwise effective drugs are responsible for side effects such as obesity and cardiovascular diseases. The ligand-binding ability of PPAR-γ is different from other nuclear receptors since it can bind to a wide variety of ligands. Although a number of compounds have been shown to activate PPAR-γ, knowledge of its endogenous ligands and their physiological functions is lacking. The known ligands were either ambiguous or found to produce ill effects in vivo. In this review we discuss the structure and functions of PPAR-γ, ligands discovered so far, and focus on the importance of identification of physiologically relevant endogenous ligands.
Export Options
About this article
Cite this article as:
Subramani Aiya Parasuraman, Reddy C. Madhava and Narala R. Venkata, The Need for Physiologically Relevant Peroxisome Proliferator-Activated Receptor-gamma (PPAR-γ) Ligands, Endocrine, Metabolic & Immune Disorders - Drug Targets 2013; 13 (2) . https://dx.doi.org/10.2174/18715303113139990003
DOI https://dx.doi.org/10.2174/18715303113139990003 |
Print ISSN 1871-5303 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3873 |
- 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
-
Neural Pathways and Neuropeptides Mediate the Therapeutic Actions of DPP IV Inhibitors in Type-2 Diabetes
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Metabolic Evidence of Diminished Lipid Oxidation in Women With Polycystic Ovary Syndrome
Current Metabolomics Risk Factors for Hyperemesis Gravidarum
Current Women`s Health Reviews The Utility of Oral Diabetes Medications in Type 2 Diabetes of the Young
Current Diabetes Reviews Heart Failure in Diabetes Mellitus: An Updated Review
Current Pharmaceutical Design Hypertension, Anti-Hypertensive Therapy and Neoplasia
Current Pharmaceutical Design Diet and Contaminants: Driving the Rise to Obesity Epidemics?
Current Medicinal Chemistry Disulfide Stress and its Targets in Acute Pancreatitis
Inflammation & Allergy - Drug Targets (Discontinued) Challenges with Insulin Use Among Patients with Type 2 Diabetes Mellitus: Focus on a Tertiary Healthcare Setting in South-East Nigeria
Current Diabetes Reviews Detection of a Left Atrial Thrombus Under Fondaparinux Treatment: A Case Report
Current Drug Safety Lipoprotein(a): Medical Treatment Options for an Elusive Molecule
Current Pharmaceutical Design The PIK3CA Gene as a Mutated Target for Cancer Therapy
Current Cancer Drug Targets The Ignored Role of Intraoperative Hypotension in Producing Postoperative Acute Kidney Injury-An Obligatory Appeal for More Preventative Nephrology
Current Hypertension Reviews Antiglycation Activity of Quinoline Derivatives- A New Therapeutic Class for the Management of Type 2 Diabetes Complications
Medicinal Chemistry Photodynamic Therapy and Periodontal Treatment
Clinical Anti-Inflammatory & Anti-Allergy Drugs (Discontinued) Treating Dyslipidemias: Is Inflammation the Missing Link?
Medicinal Chemistry Postprandial Hypertriglyceridaemia Revisited in the Era of Non-Fasting Lipid Profile Testing: A 2019 Expert Panel Statement, Narrative Review
Current Vascular Pharmacology Metabolomics Reveals Hyperlipidemic Biomarkers and Antihyperlipidemic Effect of Poria cocos
Current Metabolomics Cardiovascular effect of Nigella sativa L. Aqueous Extract in Normal Rats
Cardiovascular & Hematological Disorders-Drug Targets Human Urotensin II Promotes Hypertension and Atherosclerotic Cardiovascular Diseases
Current Medicinal Chemistry