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.
1. Cover image - p. i 2. Title page - p. ii 3. Table of Contents - p. iii 4. Copyright - p. iv 5. Contributors - p. xiii 6. Preface - p. xvii 7. Part I. GPCR structure - p. xvii 8. Chapter 1. Progress in GPCR structure determination - p. 3 9. Chapter 2. Structure, function and therapeutic potential of adhesion GPCRs - p. 23 10. Chapter 3. Structural diversity in ligand recognition by GPCRs - p. 43 11. Chapter 4. NMR-based approaches to the study of GPCRs and GPCR-ligand interactions - p. 65 12. Chapter 5. Supramolecular structure of opsins - p. 81 13. Chapter 6. Molecular determinants of GPCR oligomerization - p. 97 14. Chapter 7. Structure of G-protein-coupled receptor heteromers - p. 109 15. Chapter 8. Class A GPCR oligomerization: reasons of controversy - p. 121 16. Part II. GPCR function - p. 140 17. Chapter 9. Quantifying GPCR allostery and biased signaling - p. 143 18. Chapter 10. Kinetics of ligand binding and signaling - p. 171 19. Chapter 11. Allosteric modulators targeting GPCRs - p. 195 20. Chapter 12. Arrestin-mediated signaling at GPCRs - p. 243 21. Chapter 13. Organellar Gβγ signaling—GPCR signaling beyond the cell surface - p. 257 22. Part III. GPCRs in disease and targeted drug discovery - p. 267 23. Chapter 14. G protein-coupled receptor allosteric modulators: understanding modulator affinity and pharmacological dose - p. 271 24. Chapter 15. Computer-aided GPCR drug discovery - p. 283 25. Chapter 16. Tackling the complexities of orphan GPCR ligand discovery with rationally assisted approaches - p. 295 26. Chapter 17. G protein-coupled receptors in neurodegenerative diseases - p. 335 27. Chapter 18. GPCR targets in type 2 diabetes - p. 367 28. Chapter 19. GPCRs in thromboinflammation and hemostasis - p. 393 29. Chapter 20. Angiotensin II receptors: structure-function and drug discovery - p. 415 30. Chapter 21. GPCRs in innate and adaptive immune responses - p. 429 31. Chapter 22. Role of GPCRs in cancer - p. 463 32. Index - p. 475
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.
1. Cover image - p. i 2. Title page - p. ii 3. Table of Contents - p. iii 4. Copyright - p. iv 5. Contributors - p. xiii 6. Preface - p. xvii 7. Part I. GPCR structure - p. xvii 8. Chapter 1. Progress in GPCR structure determination - p. 3 9. Chapter 2. Structure, function and therapeutic potential of adhesion GPCRs - p. 23 10. Chapter 3. Structural diversity in ligand recognition by GPCRs - p. 43 11. Chapter 4. NMR-based approaches to the study of GPCRs and GPCR-ligand interactions - p. 65 12. Chapter 5. Supramolecular structure of opsins - p. 81 13. Chapter 6. Molecular determinants of GPCR oligomerization - p. 97 14. Chapter 7. Structure of G-protein-coupled receptor heteromers - p. 109 15. Chapter 8. Class A GPCR oligomerization: reasons of controversy - p. 121 16. Part II. GPCR function - p. 140 17. Chapter 9. Quantifying GPCR allostery and biased signaling - p. 143 18. Chapter 10. Kinetics of ligand binding and signaling - p. 171 19. Chapter 11. Allosteric modulators targeting GPCRs - p. 195 20. Chapter 12. Arrestin-mediated signaling at GPCRs - p. 243 21. Chapter 13. Organellar Gβγ signaling—GPCR signaling beyond the cell surface - p. 257 22. Part III. GPCRs in disease and targeted drug discovery - p. 267 23. Chapter 14. G protein-coupled receptor allosteric modulators: understanding modulator affinity and pharmacological dose - p. 271 24. Chapter 15. Computer-aided GPCR drug discovery - p. 283 25. Chapter 16. Tackling the complexities of orphan GPCR ligand discovery with rationally assisted approaches - p. 295 26. Chapter 17. G protein-coupled receptors in neurodegenerative diseases - p. 335 27. Chapter 18. GPCR targets in type 2 diabetes - p. 367 28. Chapter 19. GPCRs in thromboinflammation and hemostasis - p. 393 29. Chapter 20. Angiotensin II receptors: structure-function and drug discovery - p. 415 30. Chapter 21. GPCRs in innate and adaptive immune responses - p. 429 31. Chapter 22. Role of GPCRs in cancer - p. 463 32. Index - p. 475
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