GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms and New Directions [Hardcover]

G protein-coupled receptors (GPCRs) are a large protein family of transmembrane receptors vital in dictating cellular responses. GPCRs are involved in many diseases, but are also the target of around half of all modern medicinal drugs.? Shifting Paradigms in G Protein Coupled Receptors takes a look at the way GPCRs are examined today, how they react, how their mutations lead to disease, and the many ways in which they can be screened for compounds that modulate them. Chemists, pharmacologists, and biologists will find essential information in this comprehensive reference.Preface.

Contributors.

1. The Evolution of Receptors: From OnOff Switches to Microprocessors (Terry Kenakin).

1.1. Introduction.

1.2. The Receptor as an OnOff Switch.

1.3. Historical Background and Classical Receptor Theory.

1.4. The Operational Model of Drug Action.

1.5. Receptor Antagonism.

1.6. Specific Models of GPCRs (7TM Receptors).

1.7. The Receptor as Microprocessor: Ternary Complex Models.

1.8. Receptors as Basic Drug Recognition Units.

1.9. Receptor Structure.

1.10. Future Considerations.

References.

2. The Evolving Pharmacology of GPCRs 27 (Lauren T. May, Nicholas D. Holliday, and Stephen J. Hill).

2.1. Agonists, Neutral Antagonists, and Inverse Agonists.

2.2. LDTRS/Protean Agonism.

2.3. Molecular Mechanisms of GPCR Ligand Binding.

2.4. Two GPCR Ligands Binding at OnceConcept of Allosterism.

2.5. GPCR Dimerization.

2.6. Future Perspectives.

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