GPCR Molecular Pharmacology and Drug Targeting examines the complex inner working of these proteins by balancing basic research concepts with practical aspects relevant to drug discovery.

Features:

• Details major developments in the field of GPCR research and applications, including recent progress in crystallography and label-free screening approaches
• Provides vital information for scientists working to identify compounds that selectively target GPCRs
• and much more!

Contents

1. The Evolution of Receptors: From On–Off Switches to Microprocessors
2. The Evolving Pharmacology of GPCRs
3. The Emergence of Allosteric Modulators for G Protein-Coupled Receptors
4. Receptor-Mediated G Protein Activation: How, How Many, and Where?
5. Molecular Pharmacology of Frizzleds—with Implications for Possible Therapy
6. Secretin Receptor Dimerization: A Possible Functionally Important Paradigm for Family B G Protein-Coupled Receptors
7. Past and Future Strategies for GPCR Deorphanization
8. High-Throughput GPCR Screening Technologies and the Emerging Importance of the Cell Phenotype
9. Are "Traditional" Biochemical Techniques Out of Fashion in the New Era of GPCR Pharmacology?
10. Fluorescence and Resonance Energy Transfer Shine New Light on GPCR Function
11. Integration of Label-Free Detection Methods in GPCR Drug Discovery
12. Screening for Allosteric Modulators of G Protein-Coupled Receptors
13. Ultra-High-Throughput Screening Assays for GPCRs
14. New Techniques to Express and Crystallize G Protein-Coupled Receptors
15. Structure and Modeling of GPCRs: Implications for Drug Discovery
16. X-Ray Structure Developments for GPCR Drug Targets
17. Pharmacological Chaperones: Potential for the Treatment of Hereditary Diseases Caused by Mutations in G Protein-Coupled Receptors

Index

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