G Protein-Coupled Receptors in Drug Discovery

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

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