Abstract
With the apparition of concepts such as allosteric modulation and functional selectivity the field of G-protein coupled receptors drug discovery has regained its momentum. To better address this paradigm shift new screening technologies were developed. To identify novel GPCR ligands the screening method of choice was based upon functional assay for the last decade and is now being complemented by several innovative binding technologies. An overview of these assays, as well as an example of a fully integrated platform aiming at identifying novel allosteric modulator with the appropriate profile are presented in this review.
Keywords: Allosteric ligand, Binding technology, G-protein-coupled receptors, Resonance Energy Transfer.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:GPCR Binding Technologies: An Overview
Volume: 15 Issue: 24
Author(s): Christel Franchet and Ismet Dorange
Affiliation:
Keywords: Allosteric ligand, Binding technology, G-protein-coupled receptors, Resonance Energy Transfer.
Abstract: With the apparition of concepts such as allosteric modulation and functional selectivity the field of G-protein coupled receptors drug discovery has regained its momentum. To better address this paradigm shift new screening technologies were developed. To identify novel GPCR ligands the screening method of choice was based upon functional assay for the last decade and is now being complemented by several innovative binding technologies. An overview of these assays, as well as an example of a fully integrated platform aiming at identifying novel allosteric modulator with the appropriate profile are presented in this review.
Export Options
About this article
Cite this article as:
Franchet Christel and Dorange Ismet, GPCR Binding Technologies: An Overview, Current Topics in Medicinal Chemistry 2015; 15 (24) . https://dx.doi.org/10.2174/1568026615666150701112710
DOI https://dx.doi.org/10.2174/1568026615666150701112710 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
-
Pharmacogenetics in Psychiatry - A Useful Clinical Tool or Wishful Thinking for the Future?
Current Pharmaceutical Design New Strategies for the Synthesis of Bio-medically Relevant Oligosaccharides: Recent Updates on 1,2-cis-O-Glycosylation and α-O-Sialylation
Current Organic Synthesis Nicotinic Receptors and the Treatment of Attentional and Cognitive Deficits in Neuropsychiatric Disorders: Focus on the α7 Nicotinic Acetylcholine Receptor as a Promising Drug Target for Schizophrenia
Central Nervous System Agents in Medicinal Chemistry Designing of Novel Carbonic Anhydrase Inhibitors and Activators
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Recent Patents in CNS Drug Discovery: The Management of Inflammation in the Central Nervous System
Recent Patents on CNS Drug Discovery (Discontinued) Translational Therapeutic Str ategies in Amyotrophic Lateral Sclerosis
Mini-Reviews in Medicinal Chemistry Protein Homeostasis as a Therapeutic Target for Diseases of Protein Conformation
Current Topics in Medicinal Chemistry Estrogen Receptor-Positive and Estrogen Receptor-Negative Human Breast Cancer Cells: Regulation of Expression of Cancer-Related Genes by Estradiol and Tamoxifen
Current Signal Transduction Therapy Glycogen Metabolism and Brain Pathologies
Central Nervous System Agents in Medicinal Chemistry Current Overview of Inorganic Nanoparticles for the Treatment of Central Nervous System (CNS) Diseases
Current Nanomaterials Hypoxia as an Initiator of Neuroinflammation: Microglial Connections
Current Neuropharmacology Neuropsychiatric and Cognitive Symptoms in Spinocerebellar Ataxia: Relationship to Neuropathological Differences
Current Psychiatry Reviews Commentary Research Highlights: Untangling Alzheimer Disease Pathology
CNS & Neurological Disorders - Drug Targets Patent Selections:
Recent Patents on CNS Drug Discovery (Discontinued) Naturally Inspired Pyrimidines Analogues for Alzheimer’s Disease
Current Neuropharmacology Tetracyclines: Drugs with Huge Therapeutic Potential
Mini-Reviews in Medicinal Chemistry Etiology of Neuroinflammatory Pathologies in Neurodegenerative Diseases: A Treatise
Current Psychopharmacology Motor and Anxiety Effects of PNU-282987, An Alpha7 Nicotinic Receptor Agonist, and Stress in an Animal Model of Alzheimer’s Disease
Current Alzheimer Research Amyloid β Oligomers Decrease Hippocampal Spontaneous Network Activity in an Age-Dependent Manner
Current Alzheimer Research Retraction Notice: Potential Application of Venom Proteins in Designing of Medicines for Treating Human Neurodegenerative Disorders
Protein & Peptide Letters