GPCRs - 1st Edition - ISBN: 9780128162286


1st Edition

Structure, Function, and Drug Discovery

Editors: Beata Jastrzebska Paul Park
Paperback ISBN: 9780128162286
Imprint: Academic Press
Published Date: 1st October 2019
Page Count: 552
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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.

Key Features

  • 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)

Table of Contents

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 of 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


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© Academic Press 2020
Academic Press
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About the Editor

Beata Jastrzebska

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.

Affiliations and Expertise

Assistant Professor, Department of Pharmacology, School of Medicine, Case Western Reserve University, OH, USA

Paul Park

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

Affiliations and Expertise

Associate Professor, Principle Investigator, Department of Ophthalmology and Visual Sciences, Case Western Reserve University, OH, USA

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