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GPCRs
Structure, Function, and Drug Discovery
Offers a comprehensive overview of recent discoveries and our current understanding of G protein-coupled receptors (GPCR)
Beata Jastrzebska (Edited by), Paul S.-H. Park (Edited by)
9780128162286, Elsevier Science
Paperback, published 12 September 2019
500 pages
27.6 x 21.5 x 3.1 cm, 1.31 kg
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.
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 Gb? 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
