Abstract
Peroxisome proliferator-activated receptors (PPARs) have long been known as mediators of several physiological functions, among which the best characterized are lipid metabolism, energy balance and anti-inflammation. Their rather large and promiscuous ligand binding site has been recently discovered to accommodate, among a plethora of lipid molecules and metabolic intermediates, endocannabinoids and their cognate compounds, specifically belonging to the Nacylethanolamine group. In fact, oleoylethanolamide, palmitoylethanolamide and probably anandamide bind with relatively high affinity to PPARs and have now been included among their endogenous ligands. Through activation of PPARs these molecules exert a variety of physiological processes. Particularly, both long-term effects via genomic mechanisms and rapid non-genomic actions have been described, which in several instances are opposite to those evoked by activation of “classical” surface cannabinoid receptors. In this review, we describe how these effects are relevant under diverse physiological and pathophysiological circumstances, such as lipid metabolism and feeding behaviour, neuroprotection and epilepsy, circadian rhythms, addiction and cognition. A picture is emerging where nuclear receptors are involved in anorexiant, anti-inflammatory, neuroprotective, anti-epileptic, wakefulness- and cognitive-enhancing, and anti-addicting properties of endocannabinoid-like molecules. Further studies are necessary to fully understand cellular mechanisms underlying the interactions between endocannabinoids and PPARs, but also between their surface and nuclear receptors, and to exploit their potential therapeutic applications.
Keywords: Endocannabinoids, peroxisome-proliferator-activated receptors, feeding, inflammation, neuroprotection, epilepsy, addiction, circadian rhythms
Current Medicinal Chemistry
Title: From Surface to Nuclear Receptors: The Endocannabinoid Family Extends its Assets
Volume: 17 Issue: 14
Author(s): M. Pistis and M. Melis
Affiliation:
Keywords: Endocannabinoids, peroxisome-proliferator-activated receptors, feeding, inflammation, neuroprotection, epilepsy, addiction, circadian rhythms
Abstract: Peroxisome proliferator-activated receptors (PPARs) have long been known as mediators of several physiological functions, among which the best characterized are lipid metabolism, energy balance and anti-inflammation. Their rather large and promiscuous ligand binding site has been recently discovered to accommodate, among a plethora of lipid molecules and metabolic intermediates, endocannabinoids and their cognate compounds, specifically belonging to the Nacylethanolamine group. In fact, oleoylethanolamide, palmitoylethanolamide and probably anandamide bind with relatively high affinity to PPARs and have now been included among their endogenous ligands. Through activation of PPARs these molecules exert a variety of physiological processes. Particularly, both long-term effects via genomic mechanisms and rapid non-genomic actions have been described, which in several instances are opposite to those evoked by activation of “classical” surface cannabinoid receptors. In this review, we describe how these effects are relevant under diverse physiological and pathophysiological circumstances, such as lipid metabolism and feeding behaviour, neuroprotection and epilepsy, circadian rhythms, addiction and cognition. A picture is emerging where nuclear receptors are involved in anorexiant, anti-inflammatory, neuroprotective, anti-epileptic, wakefulness- and cognitive-enhancing, and anti-addicting properties of endocannabinoid-like molecules. Further studies are necessary to fully understand cellular mechanisms underlying the interactions between endocannabinoids and PPARs, but also between their surface and nuclear receptors, and to exploit their potential therapeutic applications.
Export Options
About this article
Cite this article as:
Pistis M. and Melis M., From Surface to Nuclear Receptors: The Endocannabinoid Family Extends its Assets, Current Medicinal Chemistry 2010; 17 (14) . https://dx.doi.org/10.2174/092986710790980014
DOI https://dx.doi.org/10.2174/092986710790980014 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
-
5-HT7 Receptors
Current Drug Targets - CNS & Neurological Disorders The Effects of Creatine Supplementation and Physical Exercise on Traumatic Brain Injury
Mini-Reviews in Medicinal Chemistry Animal Models in Neurology: Drawbacks and Opportunities
Current Pharmaceutical Design Structural MRI Biomarkers of Mild Cognitive Impairment from Young Elders to Centenarians
Current Alzheimer Research Influence of CYP3A5 Polymorphism on the Pharmacokinetics of Psychiatric Drugs
Current Drug Metabolism Neuroprotective Methodologies in the Treatment of Multiple Sclerosis Current Status of Clinical and Pre-clinical Findings
Current Drug Discovery Technologies Psychotropics and Methadone in Acquired Long QT Syndrome
Current Psychopharmacology Insights into the Molecular Mechanism of hERG1 Channel Activation and Blockade by Drugs
Current Medicinal Chemistry The Effects of Hydroalcoholic Extract of Pinus eldarica on Hippocampal Tissue Oxidative Damage in Pentylenetetrazole-Induced Seizures in Rat
Current Nutrition & Food Science Cell Culture Models of Oxidative Stress and Injury in the Central Nervous System
Current Neurovascular Research A panoramic view of chronic liver diseases and natural remedies reported in Traditional Persian Medicine
Current Pharmaceutical Design Rat Resources in Biomedical Research
Current Pharmaceutical Biotechnology Neuroprotective Effects of Drug-Induced Therapeutic Hypothermia in Central Nervous System Diseases
Current Drug Targets Synthesis and Evaluation of the Anticonvulsant Activity of 5-alkylthio-4- phenyl-2,4-dihydro-3H-1,2,4-triazol-3-one Derivatives
Letters in Drug Design & Discovery Diabetes Mellitus: Novel Insights, Analysis and Interpretation of Pathophysiology and Complications Management with Imidazole-Containing Peptidomimetic Antioxidants
Recent Patents on Drug Delivery & Formulation Strategies of Functional Foods Promote Sleep in Human Being
Current Signal Transduction Therapy Treatment of Central Nervous System Tuberculosis Infections and Neurological Complications of Tuberculosis Treatment
Current Pharmaceutical Design CNS Transporters and Drug Delivery in Epilepsy
Current Pharmaceutical Design Delirium Secondary to Lamotrigine Toxicity
Current Drug Safety Adenosine and the Auditory System
Current Neuropharmacology