G protein-coupled receptors in drug discovery : methods and protocols
著者
書誌事項
G protein-coupled receptors in drug discovery : methods and protocols
（Methods in molecular biology / John M. Walker, series editor, 1335）（Springer protocols）
Humana Press, c2015
2nd ed
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注記
Includes bibliographical references and index
内容説明・目次
内容説明
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.
目次
1. Purification of Stabilized GPCRs for Structural and Biophysical Analyses
James C. Errey, Andrew S. Dore, Andrei Zhukov, Fiona H. Marshall, and Robert M. Cooke
2. Purification and Crystallization of a Thermostabilized Agonist-Bound Conformation of the Human Adenosine A2A Receptor
Christopher G. Tate and Guillaume Lebon
3. 2D Projection Analysis of GPCR Complexes by Negative Stain Electron Microscopy
Alys Peisley and Georgios Skiniotis
4. Nuts and Bolts of CF3 and CH3 NMR Towards the Understanding of Conformational Exchange of GPCRs
R. Scott Prosser and Tae Hun Kim
5. Single-Molecule Fluorescence Microscopy for the Analysis of Fast Receptor Dynamics
Julia Wagner, Titiwat Sungkaworn, Katrin G. Heinze, Martin J. Lohse, and Davide Calebiro
6. Quantitative Multi-Color Detection Strategies for Bioorthogonally-Labeled GPCRs
Minyoung Park, He Tian, Saranga Naganathan, Thomas P. Sakmar, and Thomas Huber
7. Approaches to Characterize and Quantify Oligomerization of GPCRs
Sara Marsango, Maria Jose Varela Liste, and Graeme Milligan
8. Monitoring G Protein Activation in Cells with BRET
Ikuo Masuho, Kirill A. Martemyanov, and Nevin A. Lambert
9. Use of Fluorescence Indicators in Receptor Ligands
Kaleeckal G. Harikumar and Laurence J. Miller
10. Detection and Quantification of Intracellular Signalling Using FRET-Based Biosensors and High Content Imaging
Michelle L. Halls, Daniel P. Poole, Andrew M. Ellisdon, Cameron J. Nowell, and Meritxell Canals
11. The Measurement of Receptor Signaling
Bias
Terry Kenakin
12. Approaches to Assess Functional Selectivity in GPCRs: Evaluating G Protein Signaling in an Endogenous Environment
Laura M. Bohn, Lei Zhou, and Jo-Hao Ho
13. Bioluminescence Resonance Energy Transfer Approaches to Discover Bias in GPCR Signaling
Elizabeth K.M. Johnstone and Kevin D.G. Pfleger
14. Virus-Mediated Expression of DREADDs for In Vivo Metabolic Studies
Mario Rossi, Zhenzhong Cui, Ken-ichiro Nakajima, Jianxin Hu, Lu Zhu, and Jurgen Wess
15. High-Throughput Screening for Allosteric Modulators of GPCRs
Robert L. Bertekap, Jr., Neil T. Burford, Zhuyin Li, and Andrew Alt
16. Radioligand Binding Assay for an Exon 11-Associated Mu Opioid Receptor Target
Gina F. Marrone, Susruta Majumdar, and Gavril W. Pasternak
17. Docking and Virtual Screening Strategies for GPCR Drug Discovery
Thijs Beuming, Bart Lenselink, Daniele Pala, Fiona McRobb, Matt Repasky, and Woody Sherman
18. The Dynamic Process of Drug-GPCR Binding at either Orthosteric or Allosteric Sites Evaluated by Metadynamics
Sebastian Schneider, Davide Provasi, and Marta Filizola
19. Experiment-Guided Molecular Modeling of Protein-Protein Complexes Involving GPCRs
Irina Kufareva, Tracy M. Handel, and Ruben Abagyan
20. Interaction Fingerprints and Their Applications to Identify Hot Spots
Andres F. Marmolejo, Jose L. Medina-Franco, Marc Giulianotti, and Karina Martinez-Mayorga
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