Structure, Function, and Drug Discovery

1st Edition - September 11, 2019

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  • Editors: Beata Jastrzebska, Paul Park
  • Paperback ISBN: 9780128162286
  • eBook ISBN: 9780128167281

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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

  • 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

Product details

  • No. of pages: 500
  • Language: English
  • Copyright: © Academic Press 2019
  • Published: September 11, 2019
  • Imprint: Academic Press
  • Paperback ISBN: 9780128162286
  • eBook ISBN: 9780128167281

About the Editors

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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