The broad range of G protein-coupled receptors (GPCRs) encompasses all areas of modern medicine and have an enormous impact on the process of drug development. Using disease-oriented methods to cover everything from screening to expression and crystallization, G Protein-Coupled Receptors in Drug Discovery describes the physiological roles of GPCRs and their involvement in various human diseases.

The book presents current approaches in drug discovery that include target selection, establishment of screening and functional assays. It also covers recombinant GPCR expression for drug screening and structural biology, different methods for structural characterization of GPCRs, and the importance of bioinformatics. The book has been carefully edited to avoid overlapping information, some duplication has been intentionally permitted so that each chapter can function as an independent unit. Providing in-depth discussions on structure and dynamics of GPCRs, this book outlines the importance of the GPCRs to drug discovery in general and drug targets specifically.

The contributors of these 16 papers use disease-oriented methods to describe the physiological roles of G protein-coupled receptors (GPRs) and their roles in target selection, screening and functional arrays. Topics include the biology of GPRs, their use as targets in cardiovascular drugs and metabolic disease, the possibilities for them in drug history, their use in molecular bioinformatics, their structures and dynamics, crystallization, novel solid-state NMR methods for structural studies, structural genomics, a molecular basis of dimerization, and orphan receptors as promising targets.
Annotation ©2006 Book News, Inc., Portland, OR (booknews.com)

The contributors of these 16 papers use disease-oriented methods to describe the physiological roles of G protein-coupled receptors (GPRs) and their roles in target selection, screening and functional arrays. Topics include the biology of GPRs, their use as targets in cardiovascular drugs and metabolic disease, the possibilities for them in drug history, their use in molecular bioinformatics, their structures and dynamics, crystallization, novel solid-state NMR methods for structural studies, structural genomics, a molecular basis of dimerization, and orphan receptors as promising targets. Annotation ©2006 Book News, Inc., Portland, OR (booknews.com)

With more than half of drug targets based on GPCRs, translating into billions in worldwide sales, there is great interest in finding high-resolution structures for recombinantly expressed GPCRs, discovering novel drug interactions, and designing tailor-made, 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. Chapters present 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. The book also covers recombinant GPCR expression for drug screening and structural biology, different methods to obtain structural information on GPCRs, and the importance of bioinformatics.