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MORE ABOUT THIS BOOK
Main description:
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.
Contents:
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
Sebastien Granier, Samuel Kim, Juan Jose Fung, Michael P. Bokoch, and Charles Parnot
19. FLIPR (R) Assays of Intracellular Calcium in GPCR Drug Discovery
Kasper B. Hansen and Hans Brauner-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 Brauner-Osborne
26. Immunoprecipitation and Phosphorylation of G-Protein Coupled Receptors
Walter G. Thomas
PRODUCT DETAILS
Publisher: Springer (Humana Press Inc.)
Publication date: June, 2009
Pages: 388
Weight: 934g
Availability: Available
Subcategories: Pharmacology
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