G Protein Coupled Receptor Screening Assays Methods and Protocols 1st Edition by Duarte Miguel F Prazeres, Sofia Aires M Martins ISBN 1493923358 9781493923359

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Product details:

ISBN 10: 1493923358 

ISBN 13: 9781493923359

Author: Duarte Miguel F. Prazeres, Sofia Aires M. Martins

 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.

Table of contents:

1. Front Matter

2. Introduction

3. G Protein-Coupled Receptors: An Overview Of Signaling Mechanisms And Screening Assays

4. Time-Resolved FRET Strategy To Screen GPCR Ligand Library

5. Homogeneous Fluorescence Anisotropy-Based Assay For Characterization Of Ligand Binding Dynamics To GPCRs In Budded Baculoviruses

6. Construction Of Recombinant HEK293 Cell Lines For The Expression Of The Neurotensin Receptor NTSR1

7. cAMP Assay For GPCR Ligand Characterization: Application Of BacMam Expression System

8. Ca2+ Mobilization Assays In GPCR Drug Discovery

9. Using Constitutive Activity To Define Appropriate High-Throughput Screening Assays For Orphan G Protein-Coupled Receptors

10. Monitoring G Protein-Coupled Receptor Activation Using The Protein Fragment Complementation Technique Split TEV

11. Quantifying GPCR Internalization: A Focus On The Kisspeptin Receptor

12. GPCR Oligomerization Analysis By Means Of BRET And dFRAP

13. Use Of ImageJ To Recover Information From Individual Cells In A G Protein-Coupled Receptor Assay

14. Methods To Immobilize GPCR On The Surface Of SPR Sensors

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

16. Label-Free Biosensor Assays In GPCR Screening

17. Multidimensional GPCR Profiling And Screening Using Impedance-Based Label-Free And Real-Time Assay

18. Label-Free Functional Selectivity Assays

19. Measurement Of Surface-Mediated Ca2+ Transients On The Single-Cell Level In A Microfluidic Lab-On-A-Chip Environment

20. Cell-Based Assays And Animal Models For GPCR Drug Screening

21. Computer-Aided Design Of GPCR Ligands

22. Correction To: Using Constitutive Activity To Define Appropriate High-Throughput Screening Assays For Orphan G Protein-Coupled Receptors

23. Back Matter

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Tags: Duarte Miguel F Prazeres, Sofia Aires M Martins, G Protein, Coupled Receptor, Screening, Assays, Methods, Protocols