Abstract
Because G protein-coupled receptors (GPCRs) are numerous, widely expressed and involved in major physiological responses, they represent a relevant therapeutic target for drug discovery, particularly regarding pharmacological treatments of neurological disorders. Among the biological phenomena regulating receptor function, GPCR heteromerization is an important emerging area of interest and investigation. There is increasing evidence showing that heteromerization contributes to the pharmacological heterogeneity of GPCRs by modulating receptor ontogeny, activation and recycling. Although in many cases the physiological relevance of receptor heteromerization has not been fully established, the unique pharmacological and functional properties of heteromers are likely to lead to new strategies in clinical medicine. This review describes the main GPCR heteromers and their implications for major neurological disorders such as Parkinsons disease, schizophrenia and addiction. A better understanding of molecular mechanisms underlying drug interactions related to the targeting of receptor heteromers could provide more specific and efficient therapeutic agents for the treatment of brain diseases.
Keywords: Heteromerization, heteromer, GPCR, neurological disorder, drug discovery
CNS & Neurological Disorders - Drug Targets
Title: Heteromerization of G Protein-Coupled Receptors: Relevance to Neurological Disorders and Neurotherapeutics
Volume: 9 Issue: 5
Author(s): Laura Albizu, Jose L. Moreno, Javier Gonzalez-Maeso and Stuart C. Sealfon
Affiliation:
Keywords: Heteromerization, heteromer, GPCR, neurological disorder, drug discovery
Abstract: Because G protein-coupled receptors (GPCRs) are numerous, widely expressed and involved in major physiological responses, they represent a relevant therapeutic target for drug discovery, particularly regarding pharmacological treatments of neurological disorders. Among the biological phenomena regulating receptor function, GPCR heteromerization is an important emerging area of interest and investigation. There is increasing evidence showing that heteromerization contributes to the pharmacological heterogeneity of GPCRs by modulating receptor ontogeny, activation and recycling. Although in many cases the physiological relevance of receptor heteromerization has not been fully established, the unique pharmacological and functional properties of heteromers are likely to lead to new strategies in clinical medicine. This review describes the main GPCR heteromers and their implications for major neurological disorders such as Parkinsons disease, schizophrenia and addiction. A better understanding of molecular mechanisms underlying drug interactions related to the targeting of receptor heteromers could provide more specific and efficient therapeutic agents for the treatment of brain diseases.
Export Options
About this article
Cite this article as:
Albizu Laura, L. Moreno Jose, Gonzalez-Maeso Javier and C. Sealfon Stuart, Heteromerization of G Protein-Coupled Receptors: Relevance to Neurological Disorders and Neurotherapeutics, CNS & Neurological Disorders - Drug Targets 2010; 9 (5) . https://dx.doi.org/10.2174/187152710793361586
DOI https://dx.doi.org/10.2174/187152710793361586 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
Call for Papers in Thematic Issues
Diagnosis and treatment of central nervous system infectious diseases
Infectious diseases of the central nervous system (CNS) can be divided into bacterial, tuberculous, viral, fungal, parasitic infections, etc. Early etiological treatment is often the most crucial means to reduce the mortality rate of patients with central nervous system infections, reduce complications and sequelae, and improve prognosis. The initial clinical ...read more
Techniques of Drug Repurposing: Delivering a new life to Herbs & Drugs
Of late, with the adaptation of innovative approaches and integration of advancements made towards medical sciences as well as the availability of a wide range of tools; several therapeutic challenges are being translated into viable clinical solutions, with a high degree of efficacy, safety, and selectivity. With a better understanding ...read more
Trends and perspectives in the rational management of CNS disorders
Central nervous system (CNS) diseases enforce a significant global health burden, driving ongoing efforts to improve our understanding and effectiveness of therapy. This issue investigates current advances in the discipline, focusing on the understanding as well as therapeutic handling of various CNS diseases. The issue covers a variety of diseases, ...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
Related Articles
-
Chromatin Modification and Senescence
Current Pharmaceutical Design IBD Modern Concepts, Nano Drug Delivery and Patents: An Update
Recent Patents on Nanomedicine Editorial (Thematic Issue: Current Management of Fetal and Neonatal Tumors)
Current Pediatric Reviews A New Approach Against Some Oral Pathogenic Bacteria Using a Chimeric Antimicrobial Peptide Derived from the Camel Milk; Lactoferrampin - Lactoferricin Chimer
Current Drug Discovery Technologies Aquaporin Biology and Nervous System
Current Neuropharmacology ABC Transporters in the Development of Multidrug Resistance in Cancer Therapy
Current Pharmaceutical Design Anti-GD2 Antibody Therapy for GD2-Expressing Tumors
Current Cancer Drug Targets Molecular Pathology of Sarcomas
Reviews on Recent Clinical Trials The Therapeutic Potential of Neuro-EPO Administered Nasally on Acute Cerebrovascular Disease
Current Psychopharmacology 1,2,4-Triazoles: A Review of Synthetic Approaches and the Biological Activity
Letters in Organic Chemistry Recommendations for Severe Hypertriglyceridemia Treatment, are there New Strategies?
Current Vascular Pharmacology Insulin Resistance, Oxidative Stress and Cardiovascular Complications: Role of Sirtuins
Current Pharmaceutical Design New Entrants into Clinical Trials for Targeted Therapy of Breast Cancer: An Insight
Anti-Cancer Agents in Medicinal Chemistry Defining the Cough Spectrum and Reviewing the Evidence for Treating Non-Specific Cough in Children
Current Pediatric Reviews Adenoviral Vectors for Cancer Gene Therapy
Current Genomics Reading and Writing the Blood-Brain Barrier: Relevance to Therapeutics
Recent Patents on CNS Drug Discovery (Discontinued) Hypoxia and Fetal Heart Development
Current Molecular Medicine Recent Development in Neuronal Migration Disorders: Clinical, Neuroradiologic and Genetics Aspects
Current Pediatric Reviews Male Fertility-Implications of Anticancer Treatment and Strategies to Mitigate Gonadotoxicity
Anti-Cancer Agents in Medicinal Chemistry Overview of Molecular Signal Transduction of Malignant Gliomas and Correlation with Responses to Targeted Therapy Recent advances in Molecular Characterization of Glioblastoma
Current Signal Transduction Therapy