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G Protein-Coupled Receptors as Drug Targets
Analysis of Activation and Constitutive Activity
edited by Roland Seifert

G Protein-Coupled Receptors as Drug Targets discusses an important biological process that has not yet been covered in such depth in any other existing books on GPCRs.


  • Addresses in detail current models and concepts, to introduce medicinal chemists, physiologists, pharmacologists, and medical researchers into the advances in the understanding of GPCR activation and constitutive activity
  • Provides an overview on methods of investigating constitutive GPCR activity
  • Well illustrated by selected experimental data and schemes
  • Covers general mechnisms, methodological approaches and cover selected important GPCR systems


Historical Background and Introduction

The Nature of Constitutive Activity and Inverse Agonism

  • Historical Perspective
  • Theoretical Basis of Inverse Agonism: Relevance of Receptor Type
  • The Interaction of Systems with Ligands
  • Inverse Agonism as a Phenotypic Behavior

Molecular Mechanisms of GPCR Activation

  • GPCR Structure and Ligand Recognition
  • Conformational Changes in the GPCR Activation Process
  • Conversion to the Active Receptor State Involves Release of Stabilizing Intramolecular Interactions
  • Kinetics of Agonist Binding and Receptor Activation
  • GPCR Activation in an Oligomeric Context

Molecular and Cellular Determinants of GPCR Splice Variant Constitutive Activity

  • Constitutive Activation of Second Messenger Production by C-Terminal Splice Variants of GPCRs
  • Differential Constitutive Internalization of C-t GPCR Splice Variants

Naturally Occurring Constitutively Active Receptors: Physiological and Pharmacological Implications

  • Wild-type Interspecies Homologues
  • Wild-type Receptor Subtypes within a Given Species
  • Wild-type Alternatively Spliced Receptors
  • Polymorphisms in GPCRs
  • GPCR Mutation-induced Disease

The Impact of G Proteins on Constitutive GPCR Activity

  • The Contribution of G proteins to Constitutive Activity
  • GPCR–G Protein Fusion Proteins

(Patho)physiological and Therapeutic Relevance of Constitutive Activity and Inverse Agonism at G Protein-Coupled Receptors

  • Physiological Relevance of Constitutive Activity of GPCRs
  • Constitutive Activity of GPCRs and Pathophysiology of Disease
  • Physiological Relevance of Inverse Agonists
  • Inverse Agonists as Drugs

Methodological Approaches

  • Analysis of Constitutive GPCR Activity in Membranes and Intact Cells
  • Measurement of Constitutive Activity of GPCRs in Intact Cells

Constitutive Activity of b-Adrenoceptors: Analysis in Membrane Systems

  • Analysis of βAR/Gs Protein Coupling in Membranes
  • Development of the Concept that βARs are Constitutively Active
  • Probing Models of GPCR Activation with β2ARwt and β2ARCAM with Inverse Agonists
  • Probing Models of GPCR Activation with β2ARwt and β2ARCAM and with Partial and Full Agonists
  • Probing Models of GPCR Activation with β2ARwt and Purine Nucleotides
  • Constitutive Activity of the β2AR Coupled to Various G?s Proteins
  • Probing Models of GPCR Activation with β2AR Coupled to Various Classes of G proteins
  • Comparison of the Constitutive Activities of the β1AR and the β2AR

Constitutive Activity of ?-Adrenoceptors: Analysis by Physiological Methods

  • Constitutive Activity and Inverse Agonism: Definition and Detection
  • β1-Adrenoceptors
  • β2-Adrenoceptors
  • Homo- and Heterodimerization of β1- and β2ARs

Constitutive Activity at the a1-Adrenoceptors: Past and Future Implications

  • Theoretical and Experimental Approaches for Study of Constitutive GPCR Activity
  • Constitutively Activating Mutations of the a1AR Subtypes
  • A Putative Model of Receptor Activation for the a1BAR
  • Constitutive Activity of Wild-type a1ARs and Inverse Agonism
  • Receptor Regulation and Constitutive Activity of the a1ARs

Constitutive Activity of Muscarinic Acetylcholine Receptors: Implications for Receptor Activation and Physiological Relevance

  • Constitutive Activity – Native Systems
  • Constitutive Activity – Recombinant Systems
  • Constitutive Activation by G Proteins
  • Structure–Function Analysis of Receptor Activation
  • Structure–Function Model for Activation

Constitutively Active Histamine Receptors

  • The Histamine Receptors
  • Assay Systems for Detection of Constitutive Activity of Histamine Receptors

Constitutively Active Serotonin Receptors

  • 5-HT1A Receptor (5-HT1AR)
  • 5-HT1B and 5-HT1D Receptors (5-HT1BR and 5-HT1DR)
  • 5-HT2A Receptor (5-HT2AR)
  • 5-HT2C Receptor (5-HT2CR)

Virally Encoded Constitutively Active Chemokine Receptors

  • The Human Cytomegalovirus-encoded Chemokine Receptor Homologue pUS28
  • The Human Kaposi’s Sarcoma Virus-encoded Chemokine Receptor KSHV-GPCR


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G Protein-Coupled Receptors as Drug Targets
Analysis of Activation and Constitutive Activity
edited by Roland Seifert

2006 • 304 pages • $214.00 + shipping
Texas residents please add 6.75 % sales tax

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