G Protein-Coupled Receptors in Drug Discovery

Methods and Protocols

  • Marta Filizola

Part of the Methods in Molecular Biology book series (MIMB, volume 1335)

Table of contents

  1. Front Matter
    Pages i-xii
  2. James C. Errey, Andrew S. Doré, Andrei Zhukov, Fiona H. Marshall, Robert M. Cooke
    Pages 1-15
  3. Julia Wagner, Titiwat Sungkaworn, Katrin G. Heinze, Martin J. Lohse, Davide Calebiro
    Pages 53-66
  4. Minyoung Park, He Tian, Saranga Naganathan, Thomas P. Sakmar, Thomas Huber
    Pages 67-93
  5. Sara Marsango, María José Varela, Graeme Milligan
    Pages 95-105
  6. Ikuo Masuho, Kirill A. Martemyanov, Nevin A. Lambert
    Pages 107-113
  7. Kaleeckal G. Harikumar, Laurence J. Miller
    Pages 115-130
  8. Michelle L. Halls, Daniel P. Poole, Andrew M. Ellisdon, Cameron J. Nowell, Meritxell Canals
    Pages 131-161
  9. Terry Kenakin
    Pages 163-176
  10. Elizabeth K. M. Johnstone, Kevin D. G. Pfleger
    Pages 191-204
  11. Mario Rossi, Zhenzhong Cui, Ken-ichiro Nakajima, Jianxin Hu, Lu Zhu, Jürgen Wess
    Pages 205-221
  12. Robert L. Bertekap Jr., Neil T. Burford, Zhuyin Li, Andrew Alt
    Pages 223-240
  13. Gina F. Marrone, Susruta Majumdar, Gavril W. Pasternak
    Pages 241-249
  14. Thijs Beuming, Bart Lenselink, Daniele Pala, Fiona McRobb, Matt Repasky, Woody Sherman
    Pages 251-276
  15. Irina Kufareva, Tracy M. Handel, Ruben Abagyan
    Pages 295-311
  16. Andrés F. Marmolejo, José L. Medina-Franco, Marc Giulianotti, Karina Martinez-Mayorga
    Pages 313-324
  17. Back Matter
    Pages 325-327

About this book


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.


Allosteric modulators Biased agonists Drug design Drug targets GPCRs Oligomer-selective ligands Receptor structure and dynamics Therapeutic agents

Editors and affiliations

  • Marta Filizola
    • 1
  1. 1.Department of Structural and Chemical BiologyIcahn School of Medicine at Mount SinaiNew YorkUSA

Bibliographic information

  • DOI
  • Copyright Information Springer Science+Business Media New York 2015
  • Publisher Name Humana Press, New York, NY
  • eBook Packages Springer Protocols
  • Print ISBN 978-1-4939-2913-9
  • Online ISBN 978-1-4939-2914-6
  • Series Print ISSN 1064-3745
  • Series Online ISSN 1940-6029
  • Buy this book on publisher's site
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