GPCR Based Drug Discovery

Dear Colleagues,

Multiple G protein-coupled receptors (GPCRs) are present on the cell surface of every cell type, form complexes with other receptors and proteins, and transmit signals into the intracellular lumen to regulate key physiological events. Dysregulated GPCR signaling is causative for pathophysiological conditions, and targeting of GPCRs is hence widely utilized for therapeutic intervention. The recent advancements towards purification, in vitro reconstitution, and structural determination of GPCRs open up new avenues for biochemical –and physical strategies to complement classical cellular drug discovery approaches. Emerging cellular signaling aspects of GPCRs include new temporal and spatial insights, and emerging concepts on G_12/13 and MAPK pathways, adenylyl cyclase isoform-specific signaling, and ligand pharmacology. Physiological cell systems containing native GPCRs and signaling environments become more important in early drug discovery to identify GPCR ligands with activities projectable to in vivo disease models and related pharmacodynamic readouts. The purpose of this special issue is to capture these novel facets of GPCR drug discovery.

Dr. Sandra Siehler
Guest Editor

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