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GPCRs: Structure, Function, and Drug Discovery

Editat de Beata Jastrzebska, Paul S.-H. Park
en Limba Engleză Paperback – 11 sep 2019
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
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Specificații

ISBN-13: 9780128162286
ISBN-10: 0128162287
Pagini: 500
Dimensiuni: 216 x 276 mm
Greutate: 1.57 kg
Editura: ELSEVIER SCIENCE

Public țintă

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)

Cuprins

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