GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms and New Directions

“. . . scientists whose area of research is (or will be) connected with GPCRs … will get a comprehensive overview of current state-of-the-art research in this broad and rapidly developing field.” (ChemMedChem, 1 February 2011)

The focus of this book, G protein-coupled receptors (GPCRs) are a large protein family of transmembrane proteins that sense molecules outside the cell and relay the information, thus initiating cellular responses. When this molecular process breaks down, GPCRs become the culprit of many diseases, making them the target of nearly half of all modern medicinal drugs.

GPCR Molecular Pharmacology and Drug Targeting examines the complex inner workings of these proteins by balancing basic research concepts with practical aspects relevant to drug discovery. Throughout, it answers key questions surrounding research into GPCR function—how they get activated; how they signal across the cell membrane; how they couple to intracellular signaling partners; how they communicate to each other as well as to other receptors and other membrane proteins; and how their mutations lead to disease. At the same time, it explores the many ways in which the receptors can be screened at each of these critical steps for compounds that modulate their action. This book:

• Details major developments in the field of GPCR research and applications, including recent progress in crystallography and label-free screening approaches

• Provides vital information for scientists working to identify compounds that selectively target GPCRs

• Covers key topics including structure-based drug design, deorphanization, dimerization, functional selectivity, and accessory proteins

• Presents detailed methods on how to express and manipulate GPCRs, as well as established and emerging methods to measure their activity

GPCR Molecular Pharmacology and Drug Targeting provides the historical groundwork and acts as an essential resource for any scientists working with this important and therapeutically relevant family. The in-depth discussions on recent findings and extensive coverage of screening approaches provide the necessary framework for encouraging exploration into malfunctioning GPCRs and identifying novel medicinal solutions.