G Protein-Coupled Receptors in Drug Discovery : Methods and Protocols / edited by Marta Filizola.

Format:

Book

Contributor:

Filizola, Marta, editor.

SpringerLink (Online service)

Series:

Methods in molecular biology 1064-3745 ; 1335.

Springer Protocols (Springer-12345)

Methods in Molecular Biology, 1064-3745 ; 1335

Language:

English

Subjects (All):

Medicine.

Pharmacology.

Proteomics.

Biomedicine.

Pharmacology/Toxicology.

Local Subjects:

Biomedicine.

Pharmacology/Toxicology.

Proteomics.

Physical Description:

1 online resource (XII, 327 pages) : 71 illustrations, 50 illustrations in color.

Edition:

Second edition 2015.

Contained In:

Springer eBooks

Place of Publication:

New York, NY : Springer New York : Imprint: Humana Press, 2015.

System Details:

text file PDF

Summary:

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.

Contents:

Purification of Stabilized GPCRs for Structural and Biophysical Analyses

Purification and Crystallization of a Thermostabilized Agonist-Bound Conformation of the Human Adenosine A2A Receptor

2D Projection Analysis of GPCR Complexes by Negative Stain Electron Microscopy

Nuts and Bolts of CF3 and CH3 NMR Towards the Understanding of Conformational Exchange of GPCRs

Single-Molecule Fluorescence Microscopy for the Analysis of Fast Receptor Dynamics

Quantitative Multi-Color Detection Strategies for Bioorthogonally-Labeled GPCRs

Approaches to Characterize and Quantify Oligomerization of GPCRs

Monitoring G Protein Activation in Cells with BRET

Use of Fluorescence Indicators in Receptor Ligands

Detection and Quantification of Intracellular Signalling Using FRET-Based Biosensors and High Content Imaging

The Measurement of Receptor Signaling Bias

Approaches to Assess Functional Selectivity in GPCRs: Evaluating G Protein Signaling in an Endogenous Environment

Bioluminescence Resonance Energy Transfer Approaches to Discover Bias in GPCR Signaling

Virus-Mediated Expression of DREADDs for In Vivo Metabolic Studies

High-Throughput Screening for Allosteric Modulators of GPCRs

Radioligand Binding Assay for an Exon 11-Associated Mu Opioid Receptor Target

Docking and Virtual Screening Strategies for GPCR Drug Discovery

The Dynamic Process of Drug-GPCR Binding at either Orthosteric or Allosteric Sites Evaluated by Metadynamics

Experiment-Guided Molecular Modeling of Protein-Protein Complexes Involving GPCRs

Interaction Fingerprints and Their Applications to Identify Hot Spots.

Other Format:

Printed edition:

ISBN:

9781493929146

Access Restriction:

Restricted for use by site license.