GPCRs

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

Active researchers and students in biochemistry, molecular biology, pharmaceutical science, applied microbiology, and biotechnology; structural biologists, biophysicists; medical chemists; clinician scientists; specialists working in drug development in major health disciplines (cardiology, metabolic disorders, ophthalmology, oncology, neurology, immunology)

Part I GPCR structure
1. Progress in GPCR structure Determination
2. Structure, function and therapeutic potential of adhesion GPCRs
3. Structural diversity in ligand recognition by GPCRs
4. NMR-based approaches to the study of GPCRs and GPCR-ligand interactions
5. Supramolecular structure of opsins
6. Molecular determinants of GPCR oligomerization
7. Structure of G-protein-coupled receptor heteromers
8. Class A GPCR oligomerization: reasons of controversy

Part II GPCR function
9. Quantifying GPCR allostery and biased signaling
10. Kinetics of ligand binding and signaling
11. Allosteric modulators targeting GPCRs
12. Arrestin-mediated signaling at GPCRs
13. Organellar Gbγ signaling - GPCR signaling beyond the cell surface

Part III GPCRs in disease and targeted drug discovery
14. G protein-coupled receptor allosteric modulators: understanding modulator affinity and pharmacological dose
15. Computer-aided GPCR drug discovery
16. Tackling the complexities of orphan GPCR ligand discovery with rationally assisted approaches
17. G protein-coupled receptors in neurodegenerative diseases
18. GPCR targets in type 2 diabetes
19. GPCRs in thromboinflammation and hemostasis
20. Angiotensin II receptors: structure-function and drug discovery
21. GPCRs in innate and adaptive immune responses
22. Role of GPCRs in cancer