G Protein-Coupled Receptors in Drug Discovery

With more than half of drug targets based on GPCRs, there is great interest in finding high-resolution structures for recombinantly expressed GPCRs, discovering novel drug interactions, and designing structure-based drug therapies that display improved efficacy and selectivity with lesser side effects. This book describes the physiological role of GPCRs and their involvement in various human diseases. It presents current approaches in drug discovery that include target selection, establishment of screening, functional assays for GPCRs, and the continuous de-orphanization process of orphan GPCRs. It also covers recombinant GPCR expression for drug screening and structural biology, and different methods to obtain structural information on GPCRs.