G Protein-Coupled Receptors in Drug Discovery

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In this authoritative volume, experts in the field provide a range of classic and cutting-edge laboratory protocols developed for GPCR research. This volume serves to aid all those who wish to further the vital research in their GPCR drug discovery programs.
The G protein-coupled receptors (GPCRs) and associated peripheral G proteins underpin a multitude of physiological processes. The GPCRs represent one of the largest superfamilies in the human genome and are a significant target for bioactive and drug discovery programs. It is estimated that greater than 50% of all drugs, including those in development, currently target GPCRs. Many of the characterized GPCRs have known ligands; however, approximately 20% of GPCRs are described as orphan GPCRs, apparent GPCRs that share the generic high-level structure charact- istic of GPCRs but whose endogenous ligand is not known. Therefore, it is expected that the field of GPCR drug discovery and development will greatly expand in the coming years with emphasis on new generations of drugs against GPCRs with unique therapeuticuseswhichmayincludedrugssuchasallostericregulators,inverseagonists, and identification of orphan GPCR ligands. AswelearnmoreaboutthemolecularsignalingcascadesfollowingGPCRactivation, we acquire a better appreciation of the complexity of cell signaling and as a result, also acquire a vast array ofnew molecularmethods toinvestigate these andother processes. Thegeneralaimofthisbookistoprovideresearcherswitharangeofprotocolsthatmay be useful in their GPCR drug discovery programs. It is also the basis for the devel- ment of future assays in this field. Therefore, the range of topics covered and the appropriate methodological approaches in GPCR drug discovery are reflected in this book. Itisinterestingtonotethatfuturedirectionsindrugdiscoverywillrequireinput and collaboration from a plethora of fields of research. As such, this book will likely be of interest to scientists involved in such fields as molecular biology, pharmacology, biochemistry, cellular signaling, and bio-nanotechnology.
Contains several comprehensive reviews of GPCR screening technologies by authoritative leaders Provides an easily accessible reference volume for cell-based GPCR screening written by leading researchers in the field Covers a wide range of assay formats and systems Emphasizes technologies applicable to high throughput screening and research-based, high information content assays Presents a diverse approach to experimental design, covering model biological systems, screening modalities, detection technologies, and approaches to data analysis Comprehensive guide to developing, running, and analyzing cell-based assays in high-throughput screening Includes supplementary material: sn.pub/extras
Klappentext
The G protein-coupled receptors (GPCRs), known to be one of the largest superfamilies in the human genome, underpin a multitude of physiological processes and represent a significant target for bioactive and drug discovery programs. In G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols, experts in the field provide a range of classic and cutting-edge laboratory protocols developed for GPCR research, as well as several current review articles relevant to the area of high throughput GPCR screening, with discussion on GPCR structure and GPCR signalling. Written in the highly successful Methods in Molecular Biology™ series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and notes on troubleshooting and avoiding known pitfalls. Authoritative and easy to use, G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols serves to aid all those who wish to further the vital research in their GPCR drug discovery programs.
Inhalt
1. New Insights into GPCR Function: Implications for HTS Richard M. Eglen and Terry Reisine 2. Screening Technologies for G-protein Coupled Receptors: From HTS to uHTS Maite de los Frailes and Emilio Diez 3. GPCR Signaling: Understanding the Pathway to Successful Drug Discovery Christine Williams and Stephen J. Hill 4. An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRs Kenneth Lundstrom 5. Understanding the Ligand-Receptor-G-Protein Ternary Complex for GPCR Drug Discovery Venkata R.P. Ratnala and Brian Kobilka 6. Assay Data Quality Assessment Hanspeter Gubler 7. Homology Modeling of GPCRs John Simms, Nathan E. Hall, Polo H.C. Lam, Laurence J. Miller, Arthur Christopoulos, Ruben Abagyan, and Patrick M. Sexton 8. GPCR Expression Using Baculovirus-Infected Sf9 Cells Amanda L. Aloia, Richard V. Glatz, Edward J. McMurchie, and Wayne R. Leifert 9. Radioligand Binding Assays: Application of [125I]Angiotensin II Receptor Binding Wayne R. Leifert, Olgatina Bucco, Mahinda Y. Abeywardena, and Glen S. Patten 10. [35S]GTPg S Binding in G-Protein Coupled Receptor Assays Tamara Cooper, Edward J. McMurchie, and Wayne R. Leifert 11. A Time-Resolved Fluorescent Lanthanide (Eu)-GTP Binding Assay for Chemokine Receptors as Targets in Drug Discovery Jean Labrecque, Rebecca S.Y. Wong, and Simon P. Fricker 12. Use of the DiscoveRx Hithunter cAMPII Assay for Direct Measurement of cAMP in Gs and Gi GPCRs Joe Bradley and David McLoughlin 13. Use of Aequorin for G-protein Coupled Receptor Hit Identification and Compound Profiling Stephen J. Brough and Parita Shah 14. BacMam: Versatile Gene Delivery Technology for GPCR Assays Elizabeth A. Davenport, Parvathi Nuthulaganti, and Robert S. Ames 15. Yeast Assays for G-Protein Coupled Receptors Simon J. Dowell and Andrew J. Brown 16. GPCR Microspot Assays on Solid Substrates Ye Fang and Joydeep Lahiri 17. Resonant Waveguide Grating Biosensor for Whole Cell GPCR Assays Ye Fang, Ann M. Ferrie, and Elizabeth Tran 18. FRET-Based Measurement of GPCR Conformational Changes Sébastien Granier, Samuel Kim, Juan José Fung, Michael P. Bokoch, and Charles Parnot 19. FLIPR® Assays of Intracellular Calcium in GPCR Drug Discovery Kasper B. Hansen and Hans Bräuner-Osborne 20. Use of Fluorescence Indicators in Receptor Ligands Kaleeckal G. Harikumar and Laurence J. Miller 21. Application of Fluorescence Resonance Energy Transfer Techniques to Establish Ligand-Receptor Orientation Kaleeckal G. Harikumar and Laurence J. Miller 22. Detection of GPCR/ß-Arrestin Interactions in Live Cells Using Bioluminescence Resonance Energy Transfer (BRET) Technology Martina Kocan and Kevin D.G. Pfleger 23. Using Reporter Gene Technologies to Detect Changes in cAMP as a Result of GPCR Activation Daniel J. Rodrigues and David McLoughlin 24. A Quantum Dot Labeled Ligand-Receptor Binding Assay for G-Protein Coupled Receptors Contained in Minimally Purified Membrane Nanopatches Jody L. Swift, Melanie C. Burger, and David T. Cramb 25. Xenopus Oocyte Electrophysiology in GPCR Drug Discovery Kasper B. Hansen and Hans Bräuner-Osborne 26. Immunoprecipitation and Phosphorylation of G-Protein Coupled Receptors Walter G. Thomas