Description
GPCRS: Structure, Function, and Drug Discovery provides a comprehensive overview of recent discoveries and our current understanding of GPCR structure, signaling, physiology, pharmacology and methods of study. In addition to the fundamental aspects of GPCR function and dynamics, international experts discuss crystal structures, GPCR complexes with partner proteins, GPCR allosteric modulation, biased signaling through protein partners, deorphanization of GPCRs, and novel GPCR-targeting ligands that could lead to the development of new therapeutics against human diseases. GPCR association with, and possible therapeutic pathways for, retinal degenerative diseases, Alzheimer's disease, Parkinson's disease, cancer and diabetic nephropathy, among other illnesses, are examined in-depth.- Addresses our current understanding and novel advances in the GPCR field, directing readers towards recent finding of key significance for translational medicine- Combines a thorough discussion of structure and function of GPCRs with disease association and drug discovery- Features chapter contributions from international experts in GPCR structure, signaling, physiology and pharmacology
Table of Contents
Part I GPCR structure1. Progress in GPCR structure Determination2. Structure, function and therapeutic potential of adhesion GPCRs3. Structural diversity in ligand recognition by GPCRs4. NMR-based approaches to the study of GPCRs and GPCR-ligand interactions5. Supramolecular structure of opsins6. Molecular determinants of GPCR oligomerization7. Structure of G-protein-coupled receptor heteromers8. Class A GPCR oligomerization: reasons of controversyPart II GPCR function9. Quantifying GPCR allostery and biased signaling10. Kinetics of ligand binding and signaling11. Allosteric modulators targeting GPCRs12. Arrestin-mediated signaling at GPCRs13. Organellar Gbγ signaling - GPCR signaling beyond the cell surfacePart III GPCRs in disease and targeted drug discovery14. G protein-coupled receptor allosteric modulators: understanding modulator affinity and pharmacological dose15. Computer-aided GPCR drug discovery16. Tackling the complexities of orphan GPCR ligand discovery with rationally assisted approaches17. G protein-coupled receptors in neurodegenerative diseases18. GPCR targets in type 2 diabetes19. GPCRs in thromboinflammation and hemostasis20. Angiotensin II receptors: structure-function and drug discovery21. GPCRs in innate and adaptive immune responses22. Role of GPCRs in cancer
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