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G Protein-Coupled Receptor Screening Assays

Methods and Protocols

  • Book
  • © 2015

Overview

Editors:
  1. Duarte Miguel F. Prazeres

    1. IBB – Institute for Biotechnology and Bioengineering, Lisbon, Portugal
      Department of Bioengineering, Instituto Superior Técnico Universidade de Lisboa, Lisbon, Portugal

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    You can also search for this editor in PubMed   Google Scholar

  2. Sofia Aires M. Martins

    1. IBB – Institute for Biotechnology and Bioengineering, Lisbon, Portugal

    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  • Includes cutting-edge methods and protocols
  • Provides step-by-step detail essential for reproducible results
  • Contains key notes and implementation advice
  • Includes supplementary material: sn.pub/extras

Part of the book series: Methods in Molecular Biology (MIMB, volume 1272)

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Table of contents (20 protocols)

  1. Front Matter

    Pages i-xii
    Download chapter PDF

  2. Introduction

    1. Front Matter

      Pages 1-1
      Download chapter PDF

    2. G protein-Coupled Receptors: An Overview of Signaling Mechanisms and Screening Assays

      • Duarte Miguel F. Prazeres, Sofia Aires M. Martins
      Pages 3-19

  3. GPCR Screening Assays

    1. Front Matter

      Pages 21-21
      Download chapter PDF

    2. Time-Resolved FRET Strategy to Screen GPCR Ligand Library

      • Nadia Oueslati, Candide Hounsou, Abderazak Belhocine, Thieric Rodriguez, Elodie Dupuis, Jurriaan M. Zwier et al.
      Pages 23-36

    3. Homogeneous Fluorescence Anisotropy-Based Assay for Characterization of Ligand Binding Dynamics to GPCRs in Budded Baculoviruses: The Case of Cy3B-NDP-α-MSH Binding to MC4 Receptors

      • Santa Veiksina, Sergei Kopanchuk, Olga Mazina, Reet Link, Anne Lille, Ago Rinken
      Pages 37-50

    4. Construction of Recombinant HEK293 Cell Lines for the Expression of the Neurotensin Receptor NTSR1

      • Su Xiao, Joseph Shiloach, Reinhard Grisshammer
      Pages 51-64

    5. cAMP Assay for GPCR Ligand Characterization: Application of BacMam Expression System

      • Olga Mazina, Anni Allikalt, Annika Heinloo, Reet Reinart-Okugbeni, Sergei Kopanchuk, Ago Rinken
      Pages 65-77

    6. Ca2+ Mobilization Assays in GPCR Drug Discovery

      • Grzegorz Woszczek, Elisabeth Fuerst
      Pages 79-89

    7. Using Constitutive Activity to Define Appropriate High-Throughput Screening Assays for Orphan G Protein-Coupled Receptors

      • Tony Ngo, James L. J. Coleman, Nicola J. Smith
      Pages 91-106

    8. Monitoring G Protein-Coupled Receptor Activation Using the Protein Fragment Complementation Technique Split TEV

      • Michael C. Wehr, Sabrina Galinski, Moritz J. Rossner
      Pages 107-118

    9. Quantifying GPCR Internalization: A Focus on the Kisspeptin Receptor

      • Macarena Pampillo, Andy V. Babwah
      Pages 119-132

    10. GPCR Oligomerization Analysis by Means of BRET and dFRAP

      • Francisco Ciruela, Víctor Fernández-Dueñas
      Pages 133-141

    11. Use of ImageJ to Recover Information from Individual Cells in a G Protein-Coupled Receptor Assay

      • João R. C. Trabuco, Sofia Aires M. Martins, Duarte Miguel F. Prazeres
      Pages 143-172

    12. Methods to Immobilize GPCR on the Surface of SPR Sensors

      • Laura Martínez-Muñoz, Rubén Barroso, Anabel Guedán Paredes, Mario Mellado, José Miguel Rodríguez-Frade
      Pages 173-188

    13. Olfactory Receptor Screening Assay Using Nanovesicle-Immobilized Carbon Nanotube Transistor

      • Jong Hyun Lim, Juhun Park, Seunghun Hong, Tai Hyun Park
      Pages 189-198

    14. Label-Free Biosensor Assays in GPCR Screening

      • Manuel Grundmann, Evi Kostenis
      Pages 199-213

    15. Multidimensional GPCR Profiling and Screening Using Impedance-Based Label-Free and Real-Time Assay

      • Ning Ke, Khanh Nguyen, Jeffery Irelan, Yama A. Abassi
      Pages 215-226

    16. Label-Free Functional Selectivity Assays

      • Ann M. Ferrie, Vasiliy Goral, Chaoming Wang, Ye Fang
      Pages 227-246

    17. Measurement of Surface-Mediated Ca2+ Transients on the Single-Cell Level in a Microfluidic Lab-on-a-Chip Environment

      • Michael Kirschbaum, Magnus S. Jaeger, Claus Duschl
      Pages 247-256
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Keywords

About this book

 This volume explores the considerable efforts that have been directed towards the development of G Protein-Coupled Receptors (GPCR) screening assays in order to disclose GPCR acting compounds, elucidate signaling mechanisms or evaluate compound’s efficacy. New discoveries in the field, along with the widely recognized need for better and safer pharmaceutical drugs constitute the main motivation for this book. Readers, both beginners and experienced researchers, will receive an updated overview of not only the established, but also the innovative technologies that promise to advance GPCR drug research. This book is organized into two major parts: the introductory part discusses the necessary foundations for the understanding of GPCR action and the rationale behind the design of the available screening assays; and part two provides detailed protocols for different screening approaches. Written in the highly successful Methods in Molecular Biology series format, the chapters include the kind of detailed description and implementation advice that is crucial for getting optimal results in the laboratory.

Practical and innovative, G Protein-Coupled Receptor Screening Assays: Methods and Protocols reaches out to everyone involved in the discovery of GPCR-active drugs, and provides a transversal overview of the different levels of GPCR signaling addressable in the different screening strategies and presents practical examples of how current assay technologies are contributing to new paradigms in GPCR drug research.

Editors and Affiliations

  • IBB – Institute for Biotechnology and Bioengineering, Lisbon, Portugal

    Duarte Miguel F. Prazeres, Sofia Aires M. Martins

  • Department of Bioengineering, Instituto Superior Técnico Universidade de Lisboa, Lisbon, Portugal

    Duarte Miguel F. Prazeres

Bibliographic Information

  • Book Title: G Protein-Coupled Receptor Screening Assays

  • Book Subtitle: Methods and Protocols

  • Editors: Duarte Miguel F. Prazeres, Sofia Aires M. Martins

  • Series Title: Methods in Molecular Biology

  • DOI: https://doi.org/10.1007/978-1-4939-2336-6

  • Publisher: Humana New York, NY

  • eBook Packages: Springer Protocols

  • Copyright Information: Springer Science+Business Media New York 2015

  • Hardcover ISBN: 978-1-4939-2335-9Published: 07 January 2015

  • Softcover ISBN: 978-1-4939-5580-0Published: 24 September 2016

  • eBook ISBN: 978-1-4939-2336-6Published: 06 January 2015

  • Series ISSN: 1064-3745

  • Series E-ISSN: 1940-6029

  • Edition Number: 1

  • Number of Pages: XII, 296

  • Number of Illustrations: 27 b/w illustrations, 51 illustrations in colour

  • Topics: Pharmacology/Toxicology, Proteomics

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