Allosteric Modulation of G Protein-Coupled Receptors

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

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ss-arrestin; Agonist; aGPCR; Allosteric; Allosteric modulator; Allosteric modulators; Allostery; Animal physiology; Antagonist; Behavioral pharmacology; Benzamidine; Bias; Biosensors; BLT1; Cell signaling; Computational biology; Conformation; Crystal structure; Endocannabinoid system; FFA1/GPR40; FFA4/GPR120; Free fatty acid; G protein; G protein-coupled receptor; G protein-coupled receptor (GPCR); G protein-coupled receptors; GPCR; GPCRs; GPR84; Inverse agonist; Leukotriene B4 receptor; Ligand bias; Molecular docking; Molecular pharmacology; NAM; Nanobodies; PAM; PAR; Pepducins; Probe-dependence; Rational design; Receptor heteromer; Signal transduction; Signaling; Sodium ion