GPCRs: Dawn of a New Era?

Table of Contents

Chapter 1

• INTRODUCTION: THE UNTAPPED PHARMACOLOGIC POTENTIAL OF GPCRS
• 1.1. Research Advances Stimulating GPCR-Based Drug Discovery
• 1.2. Goals and Organization of Report

Chapter 2

• SCIENTIFIC BACKGROUND AND TECHNOLOGIES
• 2.1. Nature of GPCRs
• GPCRs as Drug Targets
• GPCR Classification
• 2.2. Compound Selection
• Functional Assays for GPCR Signaling
  • *Calcium Assays
  • *Cellular Dielectric Spectroscopy
  • *Beta-Arrestin Assays
• Structure-Based Drug Discovery

Chapter 3

• GPCR PHARMACOLOGY: KEY ADVANCES IN BASIC RESEARCH
• 3.1. Significance of GPCR Structures
• X-Ray Crystallographic Structure of the Beta2-Adrenergic Receptor・ ・ ・ Solved
• Implications for Structure-Based Drug Design for GPCRs
• 3.2. Deorphanization
• 3.3. Allosteric Modulators
• 3.4. Dimers and Oligomers
• 3.5. Functional Selectivity

Chapter 4

• APPLIED RESEARCH
• 4.1. Small Companies Push the Limits of GPCR Pharmacology
• 7TM Pharma
• Acadia Pharmaceuticals
• Actelion
• AcurePharma
• Addex Pharmaceuticals
• Adenosine Therapeutics (Acquired by Clinical Data)
• Arena Pharmaceuticals
• Cara Therapeutics
• Dimerix Bioscience
• EPIX Pharmaceuticals
• Trevena
• 4.2. The GPCR Pipeline
• Serotonin Receptors
  • *5-HT1 Receptor
  • *5-HT2 Receptor
  • *5-HT4 to 5-HT7 Receptors
• Adenosine Receptors
  • *A1 Receptor
  • *A2 and A3 Receptors
• Adrenergic Receptors
  • *Alpha Adrenergic Receptor
  • *Beta Adrenergic Receptor
• Angiotensin II Receptor
• Arginine Vasopressin Receptor
• Bradykinin Receptors
• Calcitonin Receptors
• Cannabinoid Receptor
• Chemokine Receptors
• Cholecystokinin Receptor
• Muscarinic Acetylcholine Receptor
• Coagulation Factor II Receptor
• Corticotropin-Releasing Hormone Receptor 1
• Dopamine Receptors
• Endothelin Receptor Type A
• GABAB Receptor
• Glucagon Receptor Family
• Metabotropic Glutamate Receptors
• Gonadotropin-Releasing Hormone Receptor
• Ghrelin Receptor
• Histamine Receptor
• Interleukin 8 Receptor
• Melanin-Concentrating Hormone Receptor 1
• Melanocortin Receptor
• Motilin Receptor
• Opiate Receptor-Like 1 and Opioid Receptors
• Oxytocin Receptor
• Prostaglandin Receptors
• GPCR44
• Purinergic P2Y Receptors
• Sphingosine-1-Phosphate Receptor 1
• Tachykinin Receptors
• Additional GPCR Modulators

Chapter 5

• DEALS, OBSERVATIONS, AND CONCLUSIONS
• 5.1. Selected GPCR-Related Deals
• 5.2. Strengths and Weaknesses of GPCRs as a Target Class
• Strengths
• Weaknesses
• 5.3. General Observations and Findings
• Diversity of GPCRs for Drug Discovery and Development
• Translation of Basic Research and New Technologies
• Functional Versus Ligand-Binding Screening Assays
  • * Cell Impedance Screening Technology
• Role of Allostery in Drug Discovery and Development
• Role of Dimers and Oligomers in Drug Discovery and Development
• Relationship of Signaling Pathway to Disease
• Deorphanization and Unfamiliar GPCRs
• Structure-Based Drug Design
• 5.4. Conclusions

Chapter 6

• EXPERT INTERVIEWS
• 6.1. Annette Gilchrist, PhD
• Adjunct Professor; Northwestern University
• 6.2. Graeme Milligan, PhD
• Professor of Molecular Pharmacology; Joint Research Director, Faculty of Biomedical and Life Sciences; University of Glasgow
• 6.3. Anonymous
• Screening and Profiling Director; Major Pharmaceutical Company X
• 6.4. P. Jeffrey Conn, PhD
• Lee E. Limbird Professor of Pharmacology; Director, Vanderbilt Program in Drug Discovery; Vanderbilt University Medical Center
• 6.5. Sidney Topiol, PhD
• Associate Director, Computational Chemistry; Lundbeck Research
• 6.6. Vincent Mutel, PhD
• CEO, Vice Chairman, and Co-Founder; Addex Pharmaceuticals