Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors, Volume 115

• Contributors
• Preface
• Chapter One. Approaches for Probing Allosteric Interactions at 7 Transmembrane Spanning Receptors
• 1 Introduction
• 2 General Considerations for Assays Designed to Identify and Characterize Allosteric Modulators
• 3 General Workflow Used in Identifying and Characterizing Allosteric Modulators
• 4 Data Analysis: General Features for Allosteric Interactions
• 5 Kinetic Assays to Measure Allosteric Interactions at 7TMRs
• 6 Label-Free Technology
• 7 Endpoint Assays
• 8 Radioligand Binding Assays for Allosteric Interactions
• 9 Competitive or Not Competitive
• 10 Conclusions and Future Directions
• References
• Chapter Two. Pharmacology of Metabotropic Glutamate Receptor Allosteric Modulators
• Abbreviations
• 1 Introduction
• 2 Physiology and Pharmacology of mGlus
• 3 Allosteric Modulation of mGlus
• 4 Location of Allosteric Sites
• 5 Therapeutic Indications for Allosteric Modulators
• 6 Concluding Remarks
• References
• Chapter Three. Mining the Potential of Label-Free Biosensors for Seven-Transmembrane Receptor Drug Discovery
• 1 Introduction
• 2 Promises of Label-Free Screening
• 3 Challenges of Label-Free Screening
• 4 The Value Proposition of Label-Free to Drug Discovery
• 5 Concluding Remarks
• References
• Chapter Four. G Protein-Coupled Receptors in Cancer
• 1 General Introduction
• 2 Biochemical Interactions
• 3 Drug Design
• References
• Chapter Five. GPCRs in Stem Cell Function
• Abbreviations
• 1 Introduction
• 2 Types of Stem Cells
• 3 GPCRs in Embryonic Stem Cells
• 4 GPCRs in Induced Pluripotent Stem Cells
• 5 GPCRs in Adult Stem Cells
• 6 GPCRs in Cancer Stem Cells
• 7 Summary
• References
• Chapter Six. Application of Receptor Theory to Allosteric Modulation of Receptors
• 1 Introduction
• 2 The Allosteric Two-State Model
• 3 Operational Models of Receptor Activation with Constitutive Activity
• 4 Further Exploration of the cTCM
• 5 Summary
• References
• Chapter Seven. What Ligand-Gated Ion Channels Can Tell Us About the Allosteric Regulation of G Protein-Coupled Receptors
• 1 Introduction
• 2 Drug-Induced Conformational Changes in Receptor Activity
• 3 Ligand-Gated Ion Channels
• 4 G Protein-Coupled Receptors
• 5 Conclusions
• References
• Chapter Eight. Modeling Cooperativity Effects in Dimeric G Protein-Coupled Receptors
• 1 Introduction
• 2 Modeling Cooperativity Effects in Monomeric GPCRs: The Allosteric Two-State Model
• 3 Modeling Cooperativity Effects in Dimeric GPCRs
• 4 Conclusions
• References
• Chapter Nine. Chemokine Receptor Oligomerization and Allostery
• 1 Introduction
• 2 Background: Chemokine Structure and Interactions with Receptors
• 3 Evidence for Hetero- and Homo-Oligomerization of Chemokine Receptors
• 4 Functional Effects of Chemokine Receptor Hetero-Oligomerization on Ligand Binding
• 5 Effects of Chemokine Hetero- and Homo-Oligomerization on Signaling
• 6 Heterodimerization of Chemokine Receptors with Nonchemokine Receptors
• 7 Other Sources of Allostery in Chemokine Receptor Signaling: Chemokine Oligomerization
• 8 Conclusions and Future Perspectives
• References
• Chapter Ten. Fine-Tuning of GPCR Signals by Intracellular G Protein Modulators
• 1 Introduction: Heterotrimeric G Proteins and Their Binding Partners
• 2 Organization of G Protein-Mediated Signals
• 3 RGS Proteins
• 4 GPSM Proteins
• 5 Nonreceptor GEFs
• 6 Interactions Between G Protein Modulatory Domains
• 7 Conclusions
• References
• Index

In this thematic volume of Progress in Molecular Biology and Translational Science, researchers reflect on recent developments and research surrounding G protein-coupled receptors. The chapters cover a large breadth of research, including GPCR role in stem cell function and pharmacology.

Authors explore in-depth research techniques and applications of GPCR usage, covering theory, laboratory approaches, and unique qualities that make GPCRs a crucial tool in microbiological and cancer research.

• Contributions from leading authorities
• Informs and updates on all the latest developments in the field

Researchers of G-protein receptors, molecular biology, and translational science