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
-
Sodium Carbonate Sesquiperhydrate (2Na2CO3-3H2O2) Catalysed One-pot Synthesis of Biologically Dynamic Novel Substituted Spirooxirane Dicarboxamides
Current Catalysis Amniotic Fluid Embolism: What Level of Scientific Evidence can be Drawn? A Systematic Review
Current Pharmaceutical Biotechnology Immunosuppressive Therapy for Myelodysplastic Syndromes
Current Pharmaceutical Design Current Evidence Regarding Low-carb Diets for The Metabolic Control of Type-2 Diabetes
Current Diabetes Reviews Natriuretic Peptide Guided Heart Failure Management
Current Clinical Pharmacology A Study of the Relaxed Mechanisms Induced by Novokinin in the Isolated Porcine Coronary Artery Ring Segments
Protein & Peptide Letters Analgesic and Anti-Inflammatory Activities of Extracts and Fatty Acids from Celtis australis L
The Natural Products Journal Effects of Statins on Blood Pressure: A Review of the Experimental and Clinical Evidence.
Current Vascular Pharmacology Lipotoxicity on the Basis of Metabolic Syndrome and Lipodystrophy in HIV-1-Infected Patients Under Antiretroviral Treatment
Current Pharmaceutical Design Stress Echocardiography
Current Pharmaceutical Design Conventional Chemotherapy and Emerging Targeted Therapy for Advanced Adrenocortical Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Mechanisms in the Bed Nucleus of the Stria Terminalis Involved in Control of Autonomic and Neuroendocrine Functions: A Review
Current Neuropharmacology Genetic Diversity Among Saudi Peganum harmala and Rhazya stricta Populations Using Chemical and ISSR Markers
Current Pharmaceutical Biotechnology Is Peri-Operative Isolated Systolic Hypertension (ISH) a Cardiac Risk Factor?
Current Cardiology Reviews Dietary Fatty Acids in Metabolic Syndrome, Diabetes and Cardiovascular Diseases
Current Diabetes Reviews Vascular Endothelin and Hypertension - From Receptors to Medicine
Current Hypertension Reviews Registered and Investigational Drugs for the Treatment of Methicillin-Resistant Staphylococcus aureus Infection
Recent Patents on Anti-Infective Drug Discovery Mexiletine Metabolites: A Review
Current Medicinal Chemistry Hypertension in Peripheral Arterial Disease
Current Pharmaceutical Design Utilizing Amines and Carbon Disulfide to Obtain Nitrogen- and Sulfur-containing Compounds under Green Conditions: A Review
Current Organic Chemistry