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Allosteric Modulation of G Protein-Coupled Receptors

Editat de Robert Laprairie
en Limba Engleză Paperback – 10 feb 2022
Allosteric Modulation of G Protein-Coupled Receptors reviews fundamental information on G protein-coupled receptors (GPCRs) and allosteric modulation, presenting original research in the area and collectively providing a comprehensive description of key issues in GPCR allosteric modulation. The book provides background on core concepts of molecular pharmacology while also introducing the most important advances and studies in the area. It also discusses key methodologies. This is an essential book for researchers and advanced students engaged in pharmacology, toxicology and pharmaceutical sciences training and research.
Many of the GPCR-targeted drugs released in the past decade have specifically worked via allosteric mechanisms. Unlike direct orthosteric-acting compounds that occupy a similar receptor site to that of endogenous ligands, allosteric modulators alter GPCR-dependent signaling at a site apart from the endogenous ligand. Recent methodological and analytical advances have greatly improved our ability to understand the signaling mechanisms of GPCRs. We now know that allostery is a common regulatory mechanism for all GPCRs and not – as we once believed – unique to a few receptor subfamilies.


  • Introduces background on core concepts of molecular pharmacology, including statistical analyses, non-linear regression, complex models and GPCR-dependent signal transduction as they relate to allosteric modulation
  • Discusses critical advances and landmark studies, including discoveries in the area of GPCR allosteric modulation, which are reviewed for their importance in positive and negative regulation, protein-protein interactions, and small molecule drug discovery
  • Includes key methodologies used to study allosteric modulation at the in silico, in vitro, and in vivo levels of drug discovery and characterization
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Specificații

ISBN-13: 9780128197714
ISBN-10: 0128197714
Pagini: 212
Ilustrații: 70 illustrations (20 in full color)
Dimensiuni: 152 x 229 x 18 mm
Greutate: 0.35 kg
Editura: ELSEVIER SCIENCE

Public țintă

Researchers, graduate, and post-graduate students engaged in pharmacology, toxicology, neuropharmacology and pharmaceutical sciences training and research.
Advanced undergraduate students

Cuprins

Part I: Core Concepts
1. G Protein-Coupled Receptor-Dependent Signal Transduction: Orthosteric and Allosteric Mechanisms
2. Analysis of Allosteric Modulation: Curve-Fitting and Modelling
3. Critical Caveats: Probe-Dependence and Ligand Bias
4. Ions as Allosteric Modulators
5. Small Molecules as Allosteric Modulators
6. Oligomerization: Protein-Protein Allosteric Effects

Part II: Critical Advances
7. Crystal Structures of G Protein-Coupled Receptors in Complex with Allosteric Modulators
8. Receptor Subtype Selectivity: Muscarinic Receptors
9. Receptor Subtype Selectivity: Opioid Receptors
10. Lipid-based Allosteric Modulators
11. Moving from Cells to Animals: Challenges of Studying Allosteric Modulators In vivo
12. Disease Targets: Pain
13. Disease Targets: Anxiety
14. New Drug Targets: Clinical Translation of Allosteric Modulators, Cinacalcet

Part III: Key Methodologies
15. In silico Analysis of Allosteric Modulators
16. Mapping Structure-Activity Relationships for Allosteric Modulators
17. Kinetic Considerations of Allosteric Modulators
18. Binding and Ligand Affinity
19. Photoaffinity Ligands and the Metabotropic Glutamate Receptors
20. Biosensors for the Study of Allosteric Modulation