Pharmacology of G protein coupled receptors /
G protein coupled receptors remain the most important class of therapeutic targets in medicine. In the last 5 years, tremendous advances have been made in our understanding of the structure and mechanism of this critical family of drug targets. The present volume explores the modern experimental and...
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| Format: | eBook |
| Language: | English |
| Published: |
San Diego, CA :
Elsevier,
©2011.
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| Series: | Advances in pharmacology (San Diego, Calif.) ;
v. 62. |
| Subjects: | |
| Online Access: | Connect to the full text of this electronic book |
Table of Contents:
- Front Cover; Pharmacology of G Protein Coupled Receptors; Copyright; Contents; Contributors; Preface; Chapter 1: The Use of GPCR Structures in Drug Design; I. Introduction; II. Technology Developments Enabling GPCR Structure Determination; A. Optimizing Expression, Purification, and Stability; B. New Techniques for GPCR Crystallization; III. GPCR Structures; A. Rhodopsin as the Prototypical Receptor; B. Aminergic Receptors; 1. Antagonist Binding; 2. Agonist Binding; C. Adenosine A2A Receptor; D. Chemokine Receptor CXCR4; E. Family B Extracellular Domain Structures
- IV. GPCR Structures in Drug DiscoveryA. Relevance of Information from GPCR Crystal Structures to Native GPCRs; B. Virtual Screening Approaches to GPCR Drug Discovery; C. Utilizing GPCR Structures in Lead Optimization; D. Using Structures to Enable Fragment Screening Approaches; V. Conclusion; Acknowledgments; References; Chapter 2: Allosteric Modulation of Metabotropic Glutamate Receptors; I. Introduction; II. Metabotropic Glutamate Receptors; A. Structural Features of Metabotropic Glutamate Receptors; B. Localization and Functional Roles of the mGlus; 1. Group I mGlus; 2. Group II mGlus
- 3. Group III mGlusIII. Pharmacological Profiles of mGlu Allosteric Modulators; A. Group I mGlus; B. Group II mGlus; C. Group III mGlus; IV. Quantifying Allosteric Interactions; V. Structural Determinants of mGlu Allosteric Modulator Binding; A. Common Allosteric Sites on the mGlus; B. Multiple Allosteric Sites Within a mGlu Subtype; VI. Functional Selectivity of mGlu Allosteric Modulation; VII. Therapeutic Potential of mGlu Allosteric Modulators; A. mGlu1 NAMs for Pain; B. mGlu5 NAMs for Anxiety, Depression, and Fragile X Syndrome; C. mGlu5 PAMs for Schizophrenia
- D. mGlu2 PAMs for Schizophrenia, Anxiety Disorders, and Drug DependenceE. mGlu3 PAMs for Neuroprotection; F. Group II NAMs for Cognitive Enhancement; G. mGlu4 PAMs for Parkinson's Disease; VIII. Conclusion; Acknowledgments; References; Chapter 3: Refining Efficacy: ExploitingFunctional Selectivity forDrug Discovery; I. Introduction; II. GPCRs as Conformational Ensembles; III. The Pluridimensional Nature of GPCR Efficacy; IV. Functionally Selective GPCR Agonism; A. Biased Activation of GPCR Effectors; B. Spatial and Temporal Bias of GPCR Signaling
- V. Functional Selectivity and Pharmaceutical DevelopmentVI. Functional Selectivity at the Parathyroid Hormone Receptor; A. The Biological Actions of Parathyroid Hormone; B. Biased Activation of the PTH1R by Synthetic PTH Analogues; C. PTH1R Functional Selectivity in vivo; VII. Conclusion; Acknowledgments; References; Chapter 4: Pharmacological Chaperones for Misfolded Gonadotropin-Releasing Hormone Receptors; I. Introduction; II. The Endoplasmic Reticulum Quality Control System; III. Misfolding of GPCRs and Disease; IV. Mutations in the Human GnRHR; A. Structural Features of the GnRHR