Abstract
A number of integral membrane G protein-coupled receptors (GPCRs) share common structural features (including palmytoilated aminoacid residues and consensus sequences specific for interaction with cholesterol) that allow them to interact with lipid rafts, membrane cholesterol-rich microdomains able to regulate GPCR signalling and functions. Among GPCRs, type-1 and type-2 cannabinoid receptors, the molecular targets of endocannabinoids (eCBs), control many physiological and pathological processes through the activation of several signal transduction pathways. Recently, the orphan GPR55 receptor has been proved to be activated by many eCBs, thus leading to the hypothesis that it might be the “type-3” cannabinoid receptor. While the biological activity of eCBs and the influence of membrane lipids on their functions are rather well established, information regarding GPR55 is still scarce and often controversial. Based on this background, here we shall review current data about GPR55 pharmacology and signalling, highlighting its involvement in several pathophysiological conditions. We shall also outline the structural features that allow GPR55 to interact with cholesterol and to associate with lipid rafts; how the latter lipid microdomains impact the biological activity of GPR55 is also addressed, as well as their potential for the discovery of new therapeutics useful for the treatment of those human diseases that might be associated with alterations of GPR55 activity.
Keywords: Cannabinoid receptors, cholesterol, endocannabinoids, GPR55, lipid rafts, plasma membranes, integral membrane, G protein-coupled receptors (GPCRs), aminoacid residues, consensus sequences
Current Medicinal Chemistry
Title:GPR55 and its Interaction with Membrane Lipids: Comparison with Other Endocannabinoid-Binding Receptors
Volume: 20 Issue: 1
Author(s): V. Gasperi, E. Dainese, S. Oddi, A. Sabatucci and M. Maccarrone
Affiliation:
Keywords: Cannabinoid receptors, cholesterol, endocannabinoids, GPR55, lipid rafts, plasma membranes, integral membrane, G protein-coupled receptors (GPCRs), aminoacid residues, consensus sequences
Abstract: A number of integral membrane G protein-coupled receptors (GPCRs) share common structural features (including palmytoilated aminoacid residues and consensus sequences specific for interaction with cholesterol) that allow them to interact with lipid rafts, membrane cholesterol-rich microdomains able to regulate GPCR signalling and functions. Among GPCRs, type-1 and type-2 cannabinoid receptors, the molecular targets of endocannabinoids (eCBs), control many physiological and pathological processes through the activation of several signal transduction pathways. Recently, the orphan GPR55 receptor has been proved to be activated by many eCBs, thus leading to the hypothesis that it might be the “type-3” cannabinoid receptor. While the biological activity of eCBs and the influence of membrane lipids on their functions are rather well established, information regarding GPR55 is still scarce and often controversial. Based on this background, here we shall review current data about GPR55 pharmacology and signalling, highlighting its involvement in several pathophysiological conditions. We shall also outline the structural features that allow GPR55 to interact with cholesterol and to associate with lipid rafts; how the latter lipid microdomains impact the biological activity of GPR55 is also addressed, as well as their potential for the discovery of new therapeutics useful for the treatment of those human diseases that might be associated with alterations of GPR55 activity.
Export Options
About this article
Cite this article as:
Gasperi V., Dainese E., Oddi S., Sabatucci A. and Maccarrone M., GPR55 and its Interaction with Membrane Lipids: Comparison with Other Endocannabinoid-Binding Receptors, Current Medicinal Chemistry 2013; 20 (1) . https://dx.doi.org/10.2174/0929867311302010008
DOI https://dx.doi.org/10.2174/0929867311302010008 |
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
-
ABC Transporters, Bile Acids, and Inflammatory Stress in Liver Cancer
Current Pharmaceutical Biotechnology Serum Zinc and β D Glucuronidase Enzyme Level in Type 2 Diabetes Mellitus with Periodontitis
Current Diabetes Reviews Ethnobotanical Survey of Medicinal Plants used to Treat Cardiovascular Disorders in Ghasemloo Valley of Urmia City
Cardiovascular & Hematological Agents in Medicinal Chemistry Statins and Contrast-Induced Nephropathy: A Systematic Review and Meta-Analysis
Current Pharmaceutical Design The Pathophysiology of CTGs and Types of Intrapartum Hypoxia
Current Women`s Health Reviews Serotonin-2 Receptor Agonists as Novel Ocular Hypotensive Agents and their Cellular and Molecular Mechanisms of Action: Novel Drug Targets for Glaucoma Treatment
Current Drug Targets The Promises and Challenges of the Use of Genomics in the Prescription of Exercise for Hypertension: The 2013 Update
Current Hypertension Reviews Agonists and Antagonists of Protease Activated Receptors (PARs)
Current Medicinal Chemistry Evidence that Cortical Dopamine is a Co-Transmitter in Noradrenergic Neurons
Current Psychiatry Reviews Lactic Acidosis, Hypotension, and Sensorineural Hearing Loss Following Intentional Metformin Overdose
Current Drug Safety Effects of <I>Gentiana lutea</I> Root on Vascular Diseases
Current Vascular Pharmacology Anabolic Androgenic Steroids Abuse and Liver Toxicity
Mini-Reviews in Medicinal Chemistry A Rare Case of Azathioprine-Induced Sweet`s Syndrome in a Patient with Crohn`s Disease
Current Drug Safety Long-Acting Antipsychotic Medications
Current Drug Targets Erectile Dysfunction as a Cardiovascular Risk Factor: Time to Step Up?
Current Vascular Pharmacology Synthesis, Cytotoxicity and Molecular Docking Simulation of Novel bis-1,4-Dihydropyridines Linked to Aliphatic or Arene Core via Amide or Ester-Amide Linkages
Mini-Reviews in Medicinal Chemistry Sleep and Antidepressant Treatment
Current Pharmaceutical Design Fibromyalgia Syndrome: Which Antidepressant Drug Should We Choose
Current Pharmaceutical Design The Development of Topically Acting Carbonic Anhydrase Inhibitors as Antiglaucoma Agents
Current Pharmaceutical Design Iron Chelators in Medicinal Applications - Chemical Equilibrium Considerations in Pharmaceutical Activity
Current Medicinal Chemistry