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Informationen zum Autor Annette Gilchrist, PhD, is Assistant Professor of Pharmaceutical Sciences at Midwestern Univeristy's Chicago of Pharmacy, and Adjunct Professor at Northwestern University in the Department of Molecular Pharmacology and Biological Chemistry. Previously, she cofounded and was chief scientific officer for Caden Biosciences, and cofounded and was president of Cue BIOtech, companies committed to GPCR discovery efforts. A life sciences industry consultant and regular speaker at ACS, SBS, DIA, BIO, and CHI conferences, she has twenty-four peer-reviewed publications and four issued patents. Klappentext The fundamental guide on the basic concepts and medical significance of GPCRsThe 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 activityGPCR 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. Zusammenfassung * G protein-coupled receptors (GPCRs), are a large protein family of transmembrane receptors that sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses. GPCRs are involved in many diseases, but are also the target of around half of all modern medicinal drugs. Inhaltsverzeichnis Preface. Contributors. 1. The Evolution of Receptors: From On-Off Switches to Microprocessors ( Terry Kenakin ) . 1.1. Introduction. 1.2. The Receptor as an On-Off Switch. 1.3. Historical Background and Classical Receptor Theory. 1.4. The Operational Model of Drug Action. 1.5. Receptor Antagonism. 1.6. Specific Models of GPCRs (7TM Receptors). 1.7. The Receptor as Microprocessor: Ternary Complex Models. 1.8. Receptors as Basic Drug Recognition Units. 1.9. Receptor Structure. 1.10. Future Considerations. References. 2. The Evolving Pharmacology of GPCRs 27 ( Lauren T. May, Nicholas D. Holliday, and Stephen J. Hill ) . 2.1. Agonists, Neutral Antagonists, and Inverse Agonists. 2.2. LDTRS/Protean Agonism. <...
