Abstract
A number of G-protein-coupled receptors (GPCRs) are currently under consideration as potential therapeutic targets for drugs acting in the central nervous system (CNS). Attempts to discover new medications have operated under the assumption that GPCRs are monomers and that a specific drug activates one single receptor coupled to one single signal transduction mechanism. In the neuronal membrane, GPCRs are now known to be arranged into homo- and hetero-oligomers; drugs acting on a single receptor within a specific heteromer context are thought to induce a particular downstream signaling. However, there is recent evidence showing that heteromertailored drugs can be designed that display different affinities for a given receptor depending on the receptor partners contained within the heteromer. It can therefore be predicted that customized drugs targeting a specific receptor heteromer in the CNS might imporove safety and efficacy for their therapeutic targets. Finally, it will be important to identify receptor heteromers that are involved in the pathogenesis of diseases, such as the recently discovered dopamine D1-D3 receptor heteromer, which might play a key role in L-DOPA-induced dyskinesia in Parkinsons disease.
Keywords: G-protein-coupled receptors, CNS, homo and hetero-oligomers, heteromer-tailored drugs, dopamine D1-D3 receptor heteromer, Parkinson's disease
CNS & Neurological Disorders - Drug Targets
Title: Prime Time for G-Protein-Coupled Receptor Heteromers as Therapeutic Targets for CNS disorders: The Dopamine D1-D3 Receptor Heteromer
Volume: 9 Issue: 5
Author(s): Sergi Ferre, Carmen Lluis, Jose Luis Lanciego and Rafael Franco
Affiliation:
Keywords: G-protein-coupled receptors, CNS, homo and hetero-oligomers, heteromer-tailored drugs, dopamine D1-D3 receptor heteromer, Parkinson's disease
Abstract: A number of G-protein-coupled receptors (GPCRs) are currently under consideration as potential therapeutic targets for drugs acting in the central nervous system (CNS). Attempts to discover new medications have operated under the assumption that GPCRs are monomers and that a specific drug activates one single receptor coupled to one single signal transduction mechanism. In the neuronal membrane, GPCRs are now known to be arranged into homo- and hetero-oligomers; drugs acting on a single receptor within a specific heteromer context are thought to induce a particular downstream signaling. However, there is recent evidence showing that heteromertailored drugs can be designed that display different affinities for a given receptor depending on the receptor partners contained within the heteromer. It can therefore be predicted that customized drugs targeting a specific receptor heteromer in the CNS might imporove safety and efficacy for their therapeutic targets. Finally, it will be important to identify receptor heteromers that are involved in the pathogenesis of diseases, such as the recently discovered dopamine D1-D3 receptor heteromer, which might play a key role in L-DOPA-induced dyskinesia in Parkinsons disease.
Export Options
About this article
Cite this article as:
Ferre Sergi, Lluis Carmen, Luis Lanciego Jose and Franco Rafael, Prime Time for G-Protein-Coupled Receptor Heteromers as Therapeutic Targets for CNS disorders: The Dopamine D1-D3 Receptor Heteromer, CNS & Neurological Disorders - Drug Targets 2010; 9 (5) . https://dx.doi.org/10.2174/187152710793361603
DOI https://dx.doi.org/10.2174/187152710793361603 |
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
-
Neuroprotective Strategies for Neurological Disorders by Natural Products: An update
Current Neuropharmacology Antipsychotic Drug Effects in Schizophrenia: A Review of Longitudinal fMRI Investigations and Neural Interpretations
Current Medicinal Chemistry The Effectiveness of Treatments for Cocaine Dependence in Schizophrenic Patients: A Systematic Review
Current Neuropharmacology Biophysics of Parkinsons Disease: Structure and Aggregation of α- Synuclein
Current Protein & Peptide Science Possible Neuroprotective Strategies for Huntingtons Disease
Current Neuropharmacology Antipsychotic Augmentation Strategies to Ameliorate Negative and Cognitive Symptoms in Schizophrenia; Implications for Future Research
Central Nervous System Agents in Medicinal Chemistry Susceptibility Genes for the Side Effect of Antipsychotics on Body Weight and Obesity
Current Drug Targets Parkinson’s Disease: Is there a Role for Dietary and Herbal Supplements?
CNS & Neurological Disorders - Drug Targets Alpha-synuclein, Proteotoxicity and Parkinson's Disease: Search for Neuroprotective Therapy
Current Neuropharmacology Targeting Transient Receptor Potential Channels in Cardiometabolic Diseases and Myocardial Ischemia Reperfusion Injury
Current Drug Targets Autoimmune Channelopathies of the Nervous System
Current Neuropharmacology Adenosine A2A Receptor Antagonists and Parkinsons Disease: State of the Art and Future Directions
Current Pharmaceutical Design Adult Neural Stem Cell Therapy: Expansion In Vitro, Tracking In Vivo and Clinical Transplantation
Current Drug Targets Omega-3 Fatty Acids Supplementation in Psychiatric Disorders: A Systematic Review
Current Psychopharmacology Neural Stem Cells Transplanted in a Mouse Model of Parkinson’s Disease Differentiate to Neuronal Phenotypes and Reduce Rotational Deficit
CNS & Neurological Disorders - Drug Targets Glycine Site Modulators and Glycine Transporter-1 Inhibitors as Novel Therapeutic Targets for the Treatment of Schizophrenia
Current Neuropharmacology Road to Future: iPSC Clinical Application in Parkinson’s Disease Treatment
Current Molecular Medicine n-3 Fatty Acids: Role in Neurogenesis and Neuroplasticity
Current Medicinal Chemistry The Treatment of Behavioral and Psychological Symptoms of Dementia: Weighing Benefits and Risks
Current Alzheimer Research Pharmacological Aspects of (-)-Deprenyl
Current Medicinal Chemistry