GPCR Binding Technologies: An Overview

Author(s): Christel Franchet, Ismet Dorange

Journal Name: Current Topics in Medicinal Chemistry

Volume 15 , Issue 24 , 2015

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Graphical 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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Article Details

Year: 2015
Published on: 29 August, 2015
Page: [2476 - 2483]
Pages: 8
DOI: 10.2174/1568026615666150701112710
Price: $65

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