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G Protein Coupled Receptors in Drug Discovery
Kenneth H. Lundstrom

G Protein Coupled Receptors in Drug Discovery presents current approaches in drug discovery that include target selection, establishment of screening and functional assays.


  • Describes the principal mechanisms for signal transduction through activation of GPCRs and their interactions with G proteins and other cellular proteins
  • Demonstrates the signal transduction mechanisms in detail with various examples
  • Covers specific areas of medicine such as cardiovascular disease, cancer, metabolic disease, and neurodegeneration and psychiatry
  • Explores high throughput screening methods for GPCRs that naturally play important roles in drug discovery
  • Discusses applied expression systems and in silico methods including application of bioinformatics and molecular modeling as tools to support structural biology approaches
  • Provides insight into the structural characterization and dynamics of GPCRs using rhodopsin as a model protein
  • Delineates the problems and recent development in crystallization of GPCRs and demonstrates how novel NMR methods can potentially be applied to GPCRs
  • Elucidates the importance of dimerization in relation to drug discovery
  • Contains a chapter on the continuous de-orphanization process of orphan GPCRs


Biology of G Protein-Coupled Receptors

  • Introduction
  • Families of GPCRs
  • Coupling to G Proteins
  • GPCR Desensitization
  • Other Signaling Pathways
  • Trafficking of GPCRs
  • Resensitization
  • Conclusions

G Protein Coupled Receptors as Targets for Drug Discovery

  • Introduction
  • GPCR Family Overview
  • GPCR Tractability: Current Therapeutics
  • GPCR Drug Discovery
  • Novel GPCR Features and Impact on Drug Discovery Approaches
  • Conclusions

G Protein-Coupled Receptors as Cardiovascular Drug Targets

  • Cardiovascular Physiology, Pharmacology, and Therapeutics
  • Drugs in Development and Novel Drugs Targets
  • Receptor Subtypes as Novel Targets
  • Receptor Gene Polymorphisms
  • Concluding Remarks

G Protien-Coupled Receptors and Cancer

  • Introduction
  • Family A GPCRs
  • Family C GPCRs
  • Frizzled/Smoothened Family of GPCRs
  • Virally Encoded GPCRs
  • Orphan GPCRs
  • Conclusions

G Protein-Coupled Receptors in Metabolic Disease

  • Introduction
  • Central Mediation of Feeding and Energy Homeostasis
  • Peripheral Signals Affecting Nutrient Sensing and Utilization
  • Conclusions

G Protien-Coupled Receptors in CNS Drug Discovery

  • Introduction
  • Psychiatric Diseases
  • Pain and Analgesia
  • Neurodegeneration
  • Neuroendocrine Function
  • Orphan GPCRs in the CNS
  • Conclusions

Recombinant G Protien-Coupled Receptors for Drug Discovery

  • Introduction
  • Cell-Free Translation
  • E. coli Expression
  • Other Prokaryotic Systems
  • Yeast Expression
  • Insect Cells
  • Mammalian Expression
  • Comparison of Expression Systems
  • Conclusions

High Troughput Screening Assays for G Protein-Coupled Receptors

  • Introduction
  • Source of Material and Assay Diversity
  • High Throughput Screening
  • Receptor Binding Assays-General Considerations
  • Functional GPCR Assays
  • Inverse Agonists and Constitutive Activities
  • Microphysiometer Assays
  • Screening for Modulators of Orphan Receptors
  • Conclusions

Molecular Bioinformatics of Receptor Binding and Activation

  • Not All 7TM Receptors are GPCRs
  • Receptor Classification by Ligand Size
  • Ligand Diversity Conforms to Receptor Phylogeny
  • Structural Flexibilities of Membrane Receptors
  • Molecular Bioinformatics in Drug Discovery
  • Sequence and Structural Searches for an Activation Mechanism
  • The Cysteine Shuffle
  • Redox Control of Receptor Activation
  • Smells Rank as the Smallest 7TMR Agonists
  • Bioinformatics with Biological Sense

Structure and Dynamics of G Protein-Coupled Receptors

  • Introduction
  • Structure, Stability, Dynamics, and Conformational Changes of Rhodopsin
  • Structures, Dynamics, and Conformational Changes of GPCRs
  • Conclusions

Towards Crystallization of G Protein-Coupled Receptors

  • Introduction
  • Overexpression and Purification
  • Detergent Selection
  • Sample Preparation
  • Crystallization Methods
  • Micelles and Bicelles
  • Lipidic Mesophases
  • Bicelles, Lipopeptides, and Nanodiscs
  • Crystallization
  • Case Study: Rhodopsin
  • Conclusions

Novel Solid-State NMR Methods for Structural Studies on G Protein-Coupled Receptors

  • Introduction
  • High-Resolution Solid State NMR
  • Sample Preparation
  • Applications
  • Conclusions and Outlook

Structural Genomics Initiatives

  • Introduction
  • Structural Genomics Programs on Membrane Proteins
  • Structural Genomics Initiatives Including GPCRs
  • MePNet Approach
  • Conclusions

Molecular Basis of Dimerization of Family A G Protein-Coupled Receptors

  • Introduction
  • Quarternary Structure of Family A GPCRs
  • Consequences of the Dimerization of the Family A GPCRs
  • The Mechanisms of Dimerization of the Family A GPCRs
  • Conclusions

Orphan Receptors: Promising Targets for Drug Discovery

  • Introduction
  • Search for Endogenous Ligands of Orphan GPCRs
  • Example of Deorphanization: The MCH Systems and Its Impact on Drug Discovery
  • Conclusions and Perspectives


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G Protein Coupled Receptors in Drug Discovery
Kenneth H. Lundstrom
2005 376 pages $138.95 + shipping
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