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.
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Table of Contents
Part I: Core Concepts1. 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
