G Protein-Coupled Receptors in Drug Discovery (Methods in Molecular Biology (552))

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__TM 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. New insights into GPCR function: implications for HTS -- R.M. Eglen and T. Reisine Screening technologies for G protein-coupled receptors: from HTS to uHTS -- M. De los Frailes and E. Diez GPCR signaling: understanding the pathway to successful drug discovery -- C. Williams and S.J. Hill An overview on GPCRs and drug discovery: structure-based drug design and structural biology on GPCRs -- K. Lundstrom Understanding the ligand-receptor-G protein ternary complex for GPCR drug discovery -- V.R. Ratnala and B. Kobilka Assay data quality assessment -- H. Gubler Homology modeling of GPCRs -- J. Simms ... [et al.] GPCR expression using baculovirus-infected Sf9 cells -- A.L. Aloia ... [et al.] Radioligand binding assays: application of [(125)I]angiotensin II receptor binding -- W.R. Leifert ... [et al.] [35S]GTPgammaS binding in G protein-coupled receptor assays -- T. Cooper, E.J. McMurchie and W.R. Leifert A time-resolved fluorescent lanthanide (Eu)-GTP binding assay for chemokine receptors as targets in drug discovery -- J. Labrecque, R.S. Wong and S.P. Fricker Use of the DiscoveRx Hit hunter cAMPII assay for direct measurement of cAMP in Gs and Gi GPCRs -- J. Bradley and D. McLoughlin Use of aequorin for G protein-coupled receptor hit identification and compound profiling -- S.J. Brough and P. Shah BacMam: versatile gene delivery technology for GPCR assays -- E.A. Davenport, P. Nuthulaganti and R.S. Ames Yeast assays for G protein-coupled receptors -- S.J. Dowell and A.J. Brown GPCR microspot assays on solid substrates -- Y. Fang and J. Lahiri Resonant waveguide grating biosensor for whole-cell GPCR assays -- Y. Fang, A.M. Ferrie and E. Tran FRET-based measurement of GPCR conformational changes -- S. Granier ... [et al.] FLIPR assays of intracellular calcium in GPCR drug discovery -- K.B. Hansen and H. Brauner-Osborne Use of fluorescence indicators in receptor ligands -- K.G. Harikumar and L.J. Miller Application of fluorescence resonance energy transfer techniques to establish ligand-receptor orientation -- K.G. Harikumar and L.J. Miller Detection of GPCR/beta-arrestin interactions in live cells using bioluminescence resonance energy transfer technology -- M. Kocan and K.D. Pfleger Using reporter gene technologies to detect changes in cAMP as a result of GPCR activation -- D.J. Rodrigues and D. McLoughlin A quantum dot-labeled ligand-receptor binding assay for G protein-coupled receptors contained in minimally purified membrane nanopatches -- J.L. Swift, M.C. Burger and D.T. Cramb Xenopus oocyte electrophysiology in GPCR drug discovery -- K.B. Hansen and H. Brauner-Osborne Immunoprecipitation and phosphorylation of G protein-coupled receptors -- W.G. Thomas. 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 TM 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. Front Matter....Pages i-xi Back Matter....Pages 1-13 ....Pages 15-37