title: GPCR Binding Technologies: An Overview.
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.
authors.forename: Christel
authors.initials: C
authors.lastname: Franchet
authors.affiliation: Domain Therapeutics SA, Bioparc, 850 Boulevard Sébastien Brant, 67400 Strasbourg-Illkirch, France. cfranchet@domaintherapeutics.com.
authors.forename: Ismet
authors.initials: I
authors.lastname: Dorange
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects; D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D055808:Drug Discovery; D006801:Humans; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*
chemical_list: D043562:Receptors, G-Protein-Coupled