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G Protein-Coupled Receptors - 1st Edition - ISBN: 9780128035955, 9780128036129

G Protein-Coupled Receptors, Volume 132

1st Edition

Signaling, Trafficking and Regulation

Serial Volume Editor: Arun Shukla
Hardcover ISBN: 9780128035955
eBook ISBN: 9780128036129
Imprint: Academic Press
Published Date: 11th March 2016
Page Count: 502
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Table of Contents

  • Series Editors
  • <li>Preface</li> <li>Section I: Trafficking, Localization and Imaging of GPCRs<ul><li>Chapter 1. Localization and signaling of GPCRs in lipid rafts<ul><li>Introduction</li><li>1. Localization of GPCRs in Lipid Rafts</li><li>2. GPCR Signaling in Lipid Rafts</li></ul></li><li>Chapter 2. Imaging GPCRs trafficking and signaling with total internal reflection fluorescence microscopy in cultured neurons<ul><li>1. Image Acquisition</li><li>2. Image Analysis</li><li>3. Final Comments</li></ul></li><li>Chapter 3. Trafficking of ciliary G&#xA0;protein-coupled receptors<ul><li>Introduction</li><li>1. Rhodopsin as a Ciliary GPCR</li><li>2. Ciliary GPCRs in Other Neurons</li><li>3. Olfactory Sensory Neuron Ciliary GPCRs</li><li>4. Dynamic Trafficking of Ciliary GPCRs</li><li>Conclusions and Future Directions</li></ul></li><li>Chapter 4. Single-molecule resolution of G protein-coupled receptor (GPCR) complexes<ul><li>Introduction</li><li>1. Imaging Methodologies to Study Single GPCR Molecules</li><li>2. Methods for Photoactivated Dye-Localization Microscopy</li><li>Conclusions and Perspectives</li></ul></li><li>Chapter 5. Quantification of the mRNA expression of G protein-coupled receptors in human adipose tissue<ul><li>Introduction</li><li>1. Materials</li><li>2. Methods</li><li>Notes</li></ul></li></ul></li> <li>Section II: Signaling and Regulation of GPCRs<ul><li>Chapter 6. Studying the regulation of&#xA0;endosomal cAMP production in GPCR signaling<ul><li>Introduction</li><li>1. Materials</li><li>2. Experimental Procedures</li><li>3. Discussion</li></ul></li><li>Chapter 7. Olfactory receptor signaling<ul><li>Introduction</li><li>1. Specificity</li><li>2. Dimerization</li><li>3. Perception</li><li>4. Olfactory Transduction</li><li>5. Mechanisms of Odorant Adaptation</li><li>6. Perspectives</li></ul></li><li>Chapter 8. Assessing Smoothened-mediated Hedgehog signaling in zebrafish<ul><li>Introduction</li><li>1. Analysis of Smoothened-mediated Hh Signaling in Zebrafish</li><li>Summary</li></ul></li><li>Chapter 9. GPCRs and actin&#x2013;cytoskeleton dynamics<ul><li>Introduction</li><li>1. GPCRs and G Proteins</li><li>2. Actin&#x2013;cytoskeleton Dynamics</li><li>3. GPCR/G Protein Signaling and Actin Polymerization</li><li>4. Cellular Processes Controlled by Actin&#x2013;cytoskeleton Rearrangements Induced&#xA0;by&#xA0;GPCRs</li><li>5. The Cross Talk of GPCR Signaling with the Homeostatic Hippo and TGF-&#x3B2; Signaling Pathways</li><li>6. Protocols to Evaluate Actin&#x2013;cytoskeleton Rearrangements</li><li>7. Method to Evaluate the Actin&#x2013;Cytoskeleton Dynamics Modulated by GPCR Signaling in&#xA0;Hepatic Cells</li><li>8. Protocols for IF Assays</li><li>Conclusions</li></ul></li></ul></li> <li>Section III: Cellular Assays for GPCRs<ul><li>Chapter 10. GPCR-radioligand binding assays<ul><li>1. Types of Binding Assays</li><li>2. Components of Binding Assays&#x2014;Considerations for GPCR Binding Assay Design</li><li>Abbreviations</li></ul></li><li>Chapter 11. Tracking GPCR biosynthesis and degradation using a nonradioactive pulse chase methodology<ul><li>Introduction</li><li>1. Materials Required</li><li>2. Basic Methodology</li><li>3. General Workflow of Experiments</li><li>4. Results</li><li>5. Discussion</li></ul></li><li>Chapter 12. Tango assay for ligand-induced GPCR&#x2013;&#x3B2;-arrestin2 interaction: Application in drug discovery<ul><li>1. Background and Rationale</li><li>2. Various &#x3B2;-Arrestin Recruitment Assays</li><li>3. Principle of Tango Assay</li><li>4. Reagents and Methods</li><li>5. Data Analysis</li><li>6. Results and Data Interpretation</li><li>7. Summary and Future Perspectives</li></ul></li><li>Chapter 13. Resonance Energy Transfer-Based Approaches to Study GPCRs<ul><li>Introduction</li><li>1. RET Approaches</li><li>2. Ligand Binding</li><li>3. Ligand-Induced Conformational Changes</li><li>4. GPCR&#x2013;G Protein Interaction</li><li>5. Second Messenger Production</li><li>6. &#x3B2;-Arrestin Recruitment</li><li>7. Receptor Internalization</li><li>8. Receptor Oligomerization</li><li>9. Summary and Outlook</li></ul></li><li>Chapter 14. Quantitative analysis of G-protein-coupled receptor internalization using DnaE intein-based assay<ul><li>Introduction</li><li>1. Materials and Methods</li><li>2. Discussion</li><li>Summary</li></ul></li><li>Chapter 15. Cellular and subcellular context determine outputs from signaling biosensors<ul><li>Introduction and Rationale</li><li>1. Materials and Instrumentation Required</li><li>2. Basic Methodology</li><li>3. Experimental Strategies</li><li>4. Discussion</li></ul></li></ul></li> <li>Section IV: Structural and Computational Investigation of GPCRs<ul><li>Chapter 16. Protease-activated receptors (PARs) in&#xA0;cancer: Novel biased signaling and targets for&#xA0;therapy<ul><li>Introduction</li><li>1. Novel Signaling of PARs Endowing Critical PH-Domain-Binding Motifs</li><li>2. PARs and Human Placenta</li><li>3. Future Directions</li></ul></li><li>Chapter 17. Computational methods for studying G protein-coupled receptors (GPCRs)<ul><li>Introduction</li><li>1. Prediction of Receptor Structure</li><li>2. Studies of Ligand&#x2013;Receptor Interactions</li><li>3. Biased Signaling</li><li>4. Allosterism</li><li>5. Dimerization</li></ul></li><li>Chapter 18. Comparing Class A&#xA0;GPCRs to bitter taste receptors: Structural motifs, ligand interactions and agonist-to-antagonist ratios<ul><li>Introduction</li><li>1. Sequence Is Less Conserved Than Structure: Sequence Alignments and GPCR Signature Motifs</li><li>2. Ligand&#x2013;Receptor Interactions in TAS2Rs Compared&#xA0;to Class A GPCRs</li><li>Conclusion and Outlook</li></ul></li><li>Chapter 19. What can simulations tell us about GPCRs: Integrating the scales<ul><li>Introduction</li><li>1. Multiscale Simulations: Accuracy, Advantages, and Limitations</li><li>2. Analyzing the Dynamics of GPCR&#x2013;Ligand Interactions</li><li>3. Can Current Simulation Techniques Allow Us to Study GPCR Activation?</li><li>4. The Dynamic Interplay between the Membrane and Receptors</li><li>5. GPCR Organization in the Cell Membrane</li><li>Conclusions</li></ul></li><li>Volumes in Series</li><li>Index</li></ul></li>


G-Protein-Coupled Receptors: Signaling, Trafficking, and Regulation, a new volume in the Methods in Cell Biology series continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers research methods in G-Protein-Coupled Receptors, and includes sections on such topics signaling, trafficking and regulation.

Key Features

  • Covers the increasingly appreciated cell biology field of G-protein-coupled receptors
  • Includes both established and new technologies
  • Contributed by experts in the field
  • Covers topics such as signaling, trafficking, and regulation


Researchers and students in cell, molecular and developmental biology


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© Academic Press 2016
11th March 2016
Academic Press
Hardcover ISBN:
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About the Serial Volume Editor

Arun Shukla

Arun Shukla

Dr. Arun K. Shukla obtained his M.Sc. (Master in Science) from the Center for Biotechnology at the Jawaharlal Nehru University in New Delhi, India. Dr. Shukla did his Ph.D. from the Department of Molecular Membrane Biology at the Max Planck Institute of Biophysics in Frankfurt, Germany. His Ph.D. research work was focused on structural studies of G Protein-Coupled Receptors (GPCRs).

Dr. Shukla subsequently carried out his post-doctoral work in the Department of Medicine at the Duke University in North Carolina, USA. During his post-doctoral research work, Dr. Shukla focused on understanding the biophysical and structural basis of ß-arrestin mediated regulation of GPCRs and non-canonical GPCR signaling. Dr. Shukla has served as an Assistant Professor in the Department of Medicine at the Duke University in Durham, North Carolina, USA.

Dr. Shukla is currently an Assistant Professor in Department of Biological Sciences and Bioengineering at the Indian Institute of Technology, Kanpur, India. Dr. Shukla is also an Intermediate Fellow of the Wellcome Trust-DBT India Alliance. The research program in Dr. Shukla’s laboratory is focused on understanding the molecular mechanism of activation, signaling and regulation of G Protein-Coupled Receptors.

Affiliations and Expertise

Indian Institute of Technology, Kanpur, India