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.
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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.
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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 |
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