From the Human Genome to New Drugs: The Potential of Orphan G‐protein‐coupled Receptors

Introduction GPCRs and the Human Genome GPCR Architecture, Signaling and Drug Action Identification of GPCRs GPCRs in the Postgenomic Era: Orphan Receptors Ligand Hunting Reverse Pharmacology Approaches to oGPCRs In Silico Approaches Tissue Expression Expression of an oGPCR of Interest Screening Approaches Screening for oGPCR Ligands using Functional Assays GTPγS-binding Assays Measurements of cAMP Ca2+ Measurements The Cytosensor Microphysiometer Reporter Gene Assays GPCR–G-protein Coupling Ligand-independent GPCR Activity Novel Screening Strategies Future Prospects References