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G Protein Coupled Receptors in Drug Discovery Methods and Protocols 2nd Edition by Marta Filizola ISBN 1493929135 9781493929139

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G Protein Coupled Receptors in Drug Discovery Methods and Protocols 2nd ed. 2015 Edition Marta Filizola Digital Instant Download

Author(s): Marta Filizola
ISBN(s): 9781493929139, 1493929135
Edition: 2nd ed. 2015
File Details: PDF, 11.29 MB
Year: 2015
Language: english
SKU: EB-5201232 Category: Tag:

G Protein Coupled Receptors in Drug Discovery Methods and Protocols 2nd Edition by Marta Filizola – Ebook PDF Instant Download/Delivery: 1493929135, 9781493929139

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Product details:

ISBN 10: 1493929135 

ISBN 13: 9781493929139

Author:  Marta Filizola 

This detailed volume provides an overview of recent techniques employed in the field of G protein-coupled receptors (GPCRs) to screen for new drugs and to derive information about their receptor structure, dynamics, and function for the purpose of developing improved therapeutics. Owing to remarkable recent advances in the structural, biophysical and biochemical analyses of these receptors, as well as a growing body of evidence hinting at the possible relevance of allosteric modulators, biased agonists and oligomer-selective ligands as improved therapeutic agents, drug discovery for GPCRs has recently taken a completely new direction. For this book, expert contributors have shared their protocols and views on the impact of these methodologies on modern drug discovery. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols and tips on troubleshooting and avoiding known pitfalls.

Practical and fully updated, G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols, Second Edition serves as an ideal guide for a diverse audience from structural and molecular biologists to pharmacologists and drug designers who wish to explore this extensive class of key drug targets.

Table of contents:

Chapter 1: Purification of Stabilized GPCRs for Structural and Biophysical Analyses
Chapter 2: Purification and Crystallization of a Thermostabilized Agonist-Bound Conformation of the Human Adenosine A2A Receptor
Chapter 3: 2D Projection Analysis of GPCR Complexes by Negative Stain Electron Microscopy
Chapter 4: Nuts and Bolts of CF3 and CH3 NMR Toward the Understanding of Conformational Exchange of GPCRs
Chapter 5: Single-Molecule Fluorescence Microscopy for the Analysis of Fast Receptor Dynamics
Chapter 6: Quantitative Multi-color Detection Strategies for Bioorthogonally Labeled GPCRs
Chapter 7: Approaches to Characterize and Quantify Oligomerization of GPCRs
Chapter 8: Monitoring G Protein Activation in Cells with BRET
Chapter 9: Use of Fluorescence Indicators in Receptor Ligands
Chapter 10: Detection and Quantification of Intracellular Signaling Using FRET-Based Biosensors and High Content Imaging
Chapter 11: The Measurement of Receptor Signaling Bias
Chapter 12: Approaches to Assess Functional Selectivity in GPCRs: Evaluating G Protein Signaling in an Endogenous Environment
Chapter 13: Bioluminescence Resonance Energy Transfer Approaches to Discover Bias in GPCR Signaling
Chapter 14: Virus-Mediated Expression of DREADDs for In Vivo Metabolic Studies
Chapter 15: High-Throughput Screening for Allosteric Modulators of GPCRs
Chapter 16: Radioligand Binding Assay for an Exon 11-Associated Mu Opioid Receptor Target
Chapter 17: Docking and Virtual Screening Strategies for GPCR Drug Discovery
Chapter 18: The Dynamic Process of Drug–GPCR Binding at Either Orthosteric or Allosteric Sites Evaluated by Metadynamics
Chapter 19: Experiment-Guided Molecular Modeling of Protein–Protein Complexes Involving GPCRs: Interaction Fingerprints and Their Applications to Identify Hot Spots

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Tags: Marta Filizola, G, Protein, Coupled, Receptors, Drug, Discovery, Methods, Protocols