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  • ID: 4768585
  • Book
  • 552 Pages
  • Elsevier Science and Technology
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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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GPCRs Structure and Activation 1. GPCRs: Seven transmembrane helical receptors 2. Advances in methodological strategies to study GPCR structure 3. Single domain antibodies targeting GPCRs for structural studies 4. GPCRs: Structural diversity in ligand recognition 5. Dynamic range GPCR activation 6. Structural water network essential for GPCR activation

GPCRs Signaling
Structural determinants of GPCR
partner protein complexes
7. Origin of specificity in GPCR-G protein recognition 8. GPCR-G protein complex
a lesson from CryoEM 9. Structural determinants of GPCR-arrestin complex 10. Molecular assembly of GPCR-GRK complex

Multimeric organization of GPCRs in biological membranes 11. Class A
Visual receptors 12. Class A
Dopamine receptor 13. Class A
Muscarinic receptor  14. Class B
Serotonin receptor 15. Class C
GPCR heterodimers 16. Spatial inhomogeneity of GPCR dimers

GPCRs Allosteric Modulation and biased Agonism 17. Protease-activated receptors (PAR) 18. P2Y1 receptor 19. Adenosine A3 receptor 20. Free fatty acid receptors 21. Positive allosteric modulation of opioid receptors 22. Light activated positive allosteric modulators of GLP-1 receptor 23. Non-canonical signaling via GPCR-arrestin recruitment 24. GPCR-arrestin mediated signaling 25. GPCR-arrestin biased signaling activated by pepducins

GPCR targeted drug discovery and disease treatment 26. GPCR targeted treatment of retinal degenerative diseases 27. Regulation of CB1 and CB2
relevance for Alzheimer disease 28. Purinergic receptors
potential target for treatment Parkinson's disease 29. PAR1 modulators that suppress tumor progression 30. PAR2 promising target for breast cancer therapy 31. Divers activation of GPCRs
contribution to cancer 32. GPCRs
novel targets for type 2 diabetes 33. GPCRs
novel targets for diabetic nephropathy 34. Proteomic-based targeting new GPCRs ligands

Progress in GPCRs de-orphanization 35. Strategies to discover ligands targeting orphan GPCRs 36. GPCR-CoINPocket, a novel strategy for de-orphanization of GPCRs 37. Strategies targeting neuronal orphan GPCRs 38. Role of GPR158/179 in regulation of G protein signaling 39. Novel ligands for GRP171
potential therapeutics for food-related disorders (Gomez I, Devi LA, Icahn School of Medicine at Mount Sinai)

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Jastrzebska, Beata
Dr. Beata Jastrzebska is an Assistant Professor in the Department of Pharmacology, School of Medicine, Case Western Reserve University, Ohio. Her lab focuses on understanding the structure and function of the visual G protein coupled receptor (GPCR), rhodopsin. In particular, she is interested in delineating the rhodopsin supramolecular organization and its implications for binding with the cognate heterotrimeric G protein, transducin. Several mutations identified in the rhodopsin gene leading to the retinal degeneration in humans, such as retinitis pigmentosa (RP), could affect membrane oligomeric organization of this receptor. Therefore, efforts are directed towards understanding the molecular basis of rhodopsin gene associated retinal degradation in humans using biochemical, biophysical, and structural methods. Dr. Jastrzebska has published her research widely in peer reviewed journals and serials, including Biochemistry, Methods in Molecular Biology, JACS, and Methods in Enzymology.
Park, Paul S.H.
Dr. Park is an Associate Professor at the Department of Ophthalmology and Visual Sciences,
Case Western Reserve University, Ohio. He serves as Principle Investigator at the Park Lab, which focuses on molecular mechanisms underlying phototransduction and the determinants of photoreceptor cell health in the retina. Dr. Park and his team use advanced microscopy and spectroscopy methods in combination with more traditional biochemistry, microscopy, and cell biology methods. Dr. Park has published his research widely in peer reviewed journals, including Biochemistry, the Journal of Biological Chemistry, the Journal of Cell Biology, the Journal of Molecular Biology, and the European Journal of Pharmacology
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