Abstract
CB1 receptors are G-protein coupled receptors (GPCRs) abundant in neurons, in which they modulate neurotransmission. The CB1 receptor influence on memory and learning is well recognized, and disease states associated with CB1 receptors are observed in addiction disorders, motor dysfunction, schizophrenia, and in bipolar, depression, and anxiety disorders. Beyond the brain, CB1 receptors also function in liver and adipose tissues, vascular as well as cardiac tissue, reproductive tissues and bone. Signal transduction by CB1 receptors occurs through interaction with Gi/o proteins to inhibit adenylyl cyclase, activate mitogen-activated protein kinases (MAPK), inhibit voltage-gated Ca2+ channels, activate K+ currents (Kir), and influence nitric oxide (NO) signaling. CB1 receptors are observed in internal organelles as well as plasma membrane. β-Arrestins, adaptor protein AP-3, and G-protein receptor-associated sorting protein 1 (GASP1) modulate cellular trafficking. Cannabinoid Receptor Interacting Protein1a (CRIP1a) is an accessory protein whose function has not been delineated. Factor Associated with Neutral sphingomyelinase (FAN) regulates ceramide signaling. Such diversity in cellular signaling and modulation by interacting proteins suggests that agonists and allosteric modulators could be developed to specifically regulate unique, cell type-specific responses.
Keywords: Anandamide (arachidonylethanolamide), AP-3, 2-arachidonoylglycerol (2-AG), β-arrestin, CP55940, CRIP-1a, endocannabinoids, G-protein coupled receptors (GPCRs), GASP, rimonabant (SR141716), Δ 9-tetrahydrocannabinol (THC), WIN55212-2
Current Medicinal Chemistry
Title: CB1 Cannabinoid Receptors and their Associated Proteins
Volume: 17 Issue: 14
Author(s): Allyn C. Howlett, Lawrence C. Blume and George D. Dalton
Affiliation:
Keywords: Anandamide (arachidonylethanolamide), AP-3, 2-arachidonoylglycerol (2-AG), β-arrestin, CP55940, CRIP-1a, endocannabinoids, G-protein coupled receptors (GPCRs), GASP, rimonabant (SR141716), Δ 9-tetrahydrocannabinol (THC), WIN55212-2
Abstract: CB1 receptors are G-protein coupled receptors (GPCRs) abundant in neurons, in which they modulate neurotransmission. The CB1 receptor influence on memory and learning is well recognized, and disease states associated with CB1 receptors are observed in addiction disorders, motor dysfunction, schizophrenia, and in bipolar, depression, and anxiety disorders. Beyond the brain, CB1 receptors also function in liver and adipose tissues, vascular as well as cardiac tissue, reproductive tissues and bone. Signal transduction by CB1 receptors occurs through interaction with Gi/o proteins to inhibit adenylyl cyclase, activate mitogen-activated protein kinases (MAPK), inhibit voltage-gated Ca2+ channels, activate K+ currents (Kir), and influence nitric oxide (NO) signaling. CB1 receptors are observed in internal organelles as well as plasma membrane. β-Arrestins, adaptor protein AP-3, and G-protein receptor-associated sorting protein 1 (GASP1) modulate cellular trafficking. Cannabinoid Receptor Interacting Protein1a (CRIP1a) is an accessory protein whose function has not been delineated. Factor Associated with Neutral sphingomyelinase (FAN) regulates ceramide signaling. Such diversity in cellular signaling and modulation by interacting proteins suggests that agonists and allosteric modulators could be developed to specifically regulate unique, cell type-specific responses.
Export Options
About this article
Cite this article as:
Howlett C. Allyn, Blume C. Lawrence and Dalton D. George, CB1 Cannabinoid Receptors and their Associated Proteins, Current Medicinal Chemistry 2010; 17 (14) . https://dx.doi.org/10.2174/092986710790980023
DOI https://dx.doi.org/10.2174/092986710790980023 |
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
-
The Therapeutic Potential of Toll-Like Receptor 7 Stimulation in Asthma
Inflammation & Allergy - Drug Targets (Discontinued) Cyclin-Dependent Kinase as a Novel Therapeutic Target: An Endless Story
Current Chemical Biology Cancer Stem Cells and their Management in Cancer Therapy
Recent Patents on Anti-Cancer Drug Discovery Rho GTPase Activating Proteins in Cancer Phenotypes
Current Protein & Peptide Science The Emerging Role of Stereotactic Radiosurgery in the Treatment of Glioblastoma Multiforme
Current Radiopharmaceuticals Radiolabeled Probes Targeting G-Protein-Coupled Receptors for Personalized Medicine
Current Pharmaceutical Design Heat Shock Proteins in Cancer: Signaling Pathways, Tumor Markers and Molecular Targets in Liver Malignancy
Protein & Peptide Letters Pharmacological Strategies that Affect HIF-1 in the Ischemic Brain: Focus on Hydroxylases Activity and Protein Kinase Pathways
Current Signal Transduction Therapy Role of Natural Plant Products Against Alzheimer’s Disease
CNS & Neurological Disorders - Drug Targets Novel Patents Targeting Interleukin-17A; Implications in Cancer and Inflammation
Recent Patents on Anti-Cancer Drug Discovery Discovery of Small Molecules that Target Autophagy for Cancer Treatment
Current Medicinal Chemistry Molecular Targeting Agents in Renal Cell Carcinoma: Present Strategies and Future Perspectives
Current Pharmaceutical Design Research Advances in the Treatment of Melanoma by Treat Melanoma
Current Topics in Medicinal Chemistry Histidine Rich Glycoprotein, an Endogenous Regulator of Macrophage and Endothelial Biology
Current Angiogenesis (Discontinued) The Role of ING Tumor Suppressors in UV Stress Response and Melanoma Progression
Current Drug Targets Preparation and Biodistribution of Technetium-99m-Labeled Bis- Misonidazole (MISO) as an Imaging Agent for Tumour Hypoxia
Medicinal Chemistry Stability Testing During Development of Nanopharmaceuticals
Pharmaceutical Nanotechnology Emerging Use of Nanotechnology in the Treatment of Neurological Disorders
Current Pharmaceutical Design Targeting Mitochondria in Fighting Cancer
Current Pharmaceutical Design Editorial [Hot Topic: SOD Enzymes and Their Mimics in Cancer:Pro- vs Anti-Oxidative Mode of Action-Part II (Guest Editor: Ines Batinic-Haberle)]
Anti-Cancer Agents in Medicinal Chemistry