Angewandte Chemie International Edition · 2010 · 50 citations · 19 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryStructural BiologyDrug-receptor InteractionsLigand BindingLigand-based DesignProtein-ligand InteractionsReceptor BindingReceptor-ligand InteractionsG Protein-coupled Receptor BindingG Protein-coupled Receptor Structure-function RelationshipsG-protein-coupled ReceptorsLigand Design For ReceptorsMultiple Ligand AlignmentMultivalent LigandsReceptor-g Protein CouplingReceptors
A nonradioactive binding assay relying on NMR methods has been devised for a G-protein-coupled receptor; in addition the INPHARMA methods give access to the relative orientation of multiple ligands and supports ligand-based drug design (see picture of superimposed ligands). The method is fast and does not require any structural information from protein crystal structures.
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Drug Discovery: A Historical Perspective
Jürgen Drews · Science · 2000 · 2.7K citations
Free fatty acids regulate insulin secretion from pancreatic β cells through GPR40
Yasuaki Itoh, Yuji Kawamata, Masataka Harada et al. · Nature · 2003 · 1.5K citations
Structure of a β1-adrenergic G-protein-coupled receptor
Tony Warne, María J. Serrano‐Vega, Jillian G. Baker et al. · Nature · 2008 · 1.3K citations · Full text