G protein-coupled receptors in drug discovery: methods and protocols / edited by Marta Filizola.

First edition edited by Wayne R. Leifert.

Includes bibliographical references and index.

Purification of stabilized GPCRs for structural and biophysical analyses / James C. Errey [and others] -- Purification and crystallization of a thermostabilized agonist-bound conformation of the human adenosine A2A receptor / Christopher G. Tate and Guillaume Lebon -- 2D projection analysis of GPCR complexes by negative stain electron microscopy / Alys Peisley and Georgios Skiniotis -- Nuts and bolts of CF3 and CH3 NMR towards the understanding of conformational exchange of GPCRs / R. Scott Prosser and Tae Hun Kim -- Single-molecule fluorescence microscopy for the analysis of fast receptor dynamics / Julia Wagner [and others] -- Quantitative multi-color detection strategies for bioorthogonally labeled GPCRs / Minyoung Park [and others] -- Approaches to characterize and quantify oligomerization of GPCRs / Sara Marsango, María José Varela, and Graeme Milligan -- Monitoring G protein activation in cells with BRET / Ikuo Masuho, Kirill A. Martemyanov, and Nevin A. Lambert -- Use of fluorescence indicators in receptor ligands / Kaleeckal G. Harikumar and Laurence J. Miller -- Detection and quantification of intracellular signaling using FRET-based biosensors and high content imaging / Michelle L. Halls [and others] -- Measurement of receptor signaling bias / Terry Kenakin -- Approaches to assess functional selectivity in GPCRs : evaluating G protein signaling in an endogenous environment / Laura M. Bohn, Lei Zhou, and Jo-Hao Ho -- Bioluminescence resonance energy transfer approaches to discover bias in GPCR signaling / Elizabeth K.M. Johnstone and Kevin D.G. Pfleger -- Virus-mediated expression of DREADDs for in vivo metabolic studies / Mario Rossi [and others] -- High-throughput screening for allosteric modulators of GPCRs / Robert L. Bertekap Jr. [and others] -- Radioligand binding assay for an exon 11-associated mu opioid receptor target / Gina F. Marrone, Susruta Majumdar, and Gavril W. Pasternak -- Docking and virtual screening strategies for GPCR drug discovery / Thijs Beuming [and others] -- Dynamic process of drug-GPCR binding at either orthosteric or allosteric sites evaluated by metadynamics / Sebastian Schneider, Davide Provasi, and Marta Filizola -- Experiment-guided molecular modeling of protein-protein complexes involving GPCRs / Irina Kufareva, Tracy M. Handel, and Ruben Abagyan -- Interaction fingerprints and their applications to identify hot spots / Andrés F. Marmolejo [and others].

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.--