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G Protein-Coupled Receptors in Drug Discovery

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Cover of 'G Protein-Coupled Receptors in Drug Discovery'

Table of Contents

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    Book Overview
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    Chapter 1 Purification of Stabilized GPCRs for Structural and Biophysical Analyses
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    Chapter 2 Purification and Crystallization of a Thermostabilized Agonist-Bound Conformation of the Human Adenosine A 2A Receptor
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    Chapter 3 2D Projection Analysis of GPCR Complexes by Negative Stain Electron Microscopy
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    Chapter 4 Nuts and Bolts of CF 3 and CH 3 NMR Toward the Understanding of Conformational Exchange of GPCRs
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    Chapter 5 Single-Molecule Fluorescence Microscopy for the Analysis of Fast Receptor Dynamics
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    Chapter 6 Quantitative Multi-color Detection Strategies for Bioorthogonally Labeled GPCRs
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    Chapter 7 Approaches to Characterize and Quantify Oligomerization of GPCRs
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    Chapter 8 Monitoring G Protein Activation in Cells with BRET
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    Chapter 9 Use of Fluorescence Indicators in Receptor Ligands
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    Chapter 10 Detection and Quantification of Intracellular Signaling Using FRET-Based Biosensors and High Content Imaging
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    Chapter 11 The Measurement of Receptor Signaling Bias
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    Chapter 12 Approaches to Assess Functional Selectivity in GPCRs: Evaluating G Protein Signaling in an Endogenous Environment
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    Chapter 13 Bioluminescence Resonance Energy Transfer Approaches to Discover Bias in GPCR Signaling
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    Chapter 14 Virus-Mediated Expression of DREADDs for In Vivo Metabolic Studies
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    Chapter 15 High-Throughput Screening for Allosteric Modulators of GPCRs
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    Chapter 16 Radioligand Binding Assay for an Exon 11-Associated Mu Opioid Receptor Target
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    Chapter 17 Docking and Virtual Screening Strategies for GPCR Drug Discovery
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    Chapter 18 The Dynamic Process of Drug–GPCR Binding at Either Orthosteric or Allosteric Sites Evaluated by Metadynamics
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    Chapter 19 Experiment-Guided Molecular Modeling of Protein–Protein Complexes Involving GPCRs
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    Chapter 20 Interaction Fingerprints and Their Applications to Identify Hot Spots
Attention for Chapter 5: Single-Molecule Fluorescence Microscopy for the Analysis of Fast Receptor Dynamics
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Chapter title
Single-Molecule Fluorescence Microscopy for the Analysis of Fast Receptor Dynamics
Chapter number 5
Book title
G Protein-Coupled Receptors in Drug Discovery
Published in
Methods in molecular biology, January 2015
DOI 10.1007/978-1-4939-2914-6_5
Pubmed ID
Book ISBNs
978-1-4939-2913-9, 978-1-4939-2914-6
Authors

Julia Wagner, Titiwat Sungkaworn, Katrin G. Heinze, Martin J. Lohse, Davide Calebiro, Wagner, Julia, Sungkaworn, Titiwat, Heinze, Katrin G., Lohse, Martin J., Calebiro, Davide

Abstract

Assessing the dynamics of individual membrane proteins in living cells is a powerful approach to investigate their assembly, mobility, and function. Here, we describe how to image single G protein-coupled receptors (GPCRs), both in the active and inactive state. This is achieved by combining labeling of GPCRs with bright organic fluorophores and fluorescent imaging by total internal reflection fluorescence microscopy. Using this method, individual tracks of single molecules can be analyzed in parallel with high spatial precision and with frame rates up to 50/s.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 20 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 20 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 4 20%
Researcher 3 15%
Student > Bachelor 2 10%
Student > Master 2 10%
Professor 1 5%
Other 2 10%
Unknown 6 30%
Readers by discipline Count As %
Biochemistry, Genetics and Molecular Biology 6 30%
Agricultural and Biological Sciences 3 15%
Pharmacology, Toxicology and Pharmaceutical Science 2 10%
Medicine and Dentistry 1 5%
Neuroscience 1 5%
Other 1 5%
Unknown 6 30%