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
-
From the Editors Perspective: Aquaporins to Apoptosis
Current Neurovascular Research The Role of Biologically Active Ingredients from Chinese Herbal Medicines in the Regulation of Autophagy in Treating Cardiovascular Diseases and Other Chronic Diseases
Current Pharmaceutical Design Peripheral Mononuclear Cell Rejuvenation for Senescence Surveillance in Alzheimer Disease
Current Pharmaceutical Design Combining Polymeric Devices and Stem Cells for the Treatment of Neurological Disorders: A Promising Therapeutic Approach
Current Drug Targets Molecular Chaperone Disorders: Defective Hsp60 in Neurodegeneration
Current Topics in Medicinal Chemistry Immunomodulatory Properties of Thalidomide Analogs: Pomalidomide and Lenalidomide, Experimental and Therapeutic Applications
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Exploring Nitrostyrene as a Scaffold for a New Class a of Monoamine Oxidase Inhibitors
Letters in Drug Design & Discovery Editorial [Hot Topic: Modulation, Absorption and Delivery of Xenobiotics: The Synergic Role of CYP450 and P-gp Activities (Guest Editor: Nicola Antonio Colabufo)]
Current Drug Metabolism Familial Mutations and Post-translational Modifications of UCH-L1 in Parkinson's Disease and Neurodegenerative Disorders
Current Protein & Peptide Science Amyloidogenesis of Natively Unfolded Proteins
Current Alzheimer Research NSAID Use and the Risk of Parkinsons Disease
Current Drug Safety Use of Fullerenes in Cosmetics
Recent Patents on Biotechnology Role of Complement Systems in IVIG Mediated Attenuation of Cognitive Deterioration in Alzheimer's Disease
Current Alzheimer Research Functional Roles of Synaptic and Extrasynaptic NMDA Receptors in Physiological and Pathological Neuronal Activities
Current Drug Targets Nicotine-Derived Compounds as Therapeutic Tools Against Post-Traumatic Stress Disorder
Current Pharmaceutical Design Evidence Linking Protein Misfolding to Quality Control in Progressive Neurodegenerative Diseases
Current Topics in Medicinal Chemistry Neuro-Inflammatory Mechanisms in Developmental Disorders Associated with Intellectual Disability and Autism Spectrum Disorder: A Neuro- Immune Perspective
CNS & Neurological Disorders - Drug Targets Small Molecule Natural Products and Alzheimer’s Disease
Current Topics in Medicinal Chemistry Mitophagy in Neurodegeneration: An Opportunity for Therapy?
Current Drug Targets Cognitive Improvement by Photic Stimulation in a Mouse Model of Alzheimer’s Disease
Current Alzheimer Research