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Title G protein-coupled receptors in drug discovery / edited by Wayne R. Leifert
Published New York : Humana Press, [2009]
©2009
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Description 1 online resource (xi, 376 pages) : illustrations
Series Methods in molecular biology, ; 552
Springer protocols
Methods in molecular biology (Clifton, N.J.) ; v. 552. 1064-3745
Springer protocols (Series)
Contents New insights into GPCR function: implications for HTS / Richard M. Eglen and Terry Reisine -- Screening technologies for G protein-coupled receptors: from HTS to uHTS / Maite de los Frailes and Emilio Diez -- GPCR signaling: understanding the pathway to successful drug discovery / Christine Williams and Stephen J. Hill -- An overview on GPCRs and drug discovery: structure-based drug design and structural biology on GPCRs / Kenneth Lundstrom -- Understanding the ligand-receptor-G protein ternary complex for GPCR drug discovery / Venkata R.P. Ratnala and Brian Kobilka -- Assay data quality assessment / Hanspeter Gubler -- Homology modeling of GPCRs / John Simms, Nathan E. Hall, Polo H.C. Lam, Laurence J. Miller, Arthur Christopoulos, Ruben Abagyan, and Patrick M. Sexton -- GPCR expression using baculovirus-infected Sf9 cells / Amanda L. Aloia, Richard V. Glatz, Edward J. McMurchie, and Wayne R. Leifert -- Radioligand binding assays: application of [(125)I]angiotensin II receptor binding / Wayne R. Leifert, Olgatina Bucco, Mahinda Y. Abeywardena, and Glen S. Patten -- [35S]GTPgammaS binding in G protein-coupled receptor assays / Tamara Cooper, Edward J. McMurchie, and Wayne R. Leifert -- 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 -- Use of the DiscoveRx Hit hunter cAMPII assay for direct measurement of cAMP in Gs and Gi GPCRs / Joe Bradley and David McLoughlin -- Use of aequorin for G protein-coupled receptor hit identification and compound profiling / Stephen J. Brough and Parita Shah -- BacMam: versatile gene delivery technology for GPCR assays / Elizabeth A. Davenport, Parvathi Nuthulaganti, and Robert S. Ames -- Yeast assays for G protein-coupled receptors / Simon J. Dowell and Andrew J. Brown -- GPCR microspot assays on solid substrates / Ye Fang and Joydeep Lahiri -- Resonant waveguide grating biosensor for whole-cell GPCR assays / Ye Fang, Ann M. Ferrie, and Elizabeth Tran -- FRET-based measurement of GPCR conformational changes / Sébastien Granier, Samuel Kim, Juan José Fung, Michael P. Bokoch, and Charles Parnot -- FLIPR assays of intracellular calcium in GPCR drug discovery / Kasper B. Hansen and Hans Bräuner-Osborne -- Use of fluorescence indicators in receptor ligands / Kaleeckal G. Harikumar and Laurence J. Miller -- Application of fluorescence resonance energy transfer techniques to establish ligand-receptor orientation / Kaleeckal G. Harikumar and Laurence J. Miller -- Detection of GPCR/beta-arrestin interactions in live cells using bioluminescence resonance energy transfer technology / Martina Kocan and Kevin D.G. Pfleger -- Using reporter gene technologies to detect changes in cAMP as a result of GPCR activation / Daniel J. Rodrigues and David McLoughlin -- 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 -- Xenopus oocyte electrophysiology in GPCR drug discovery / Kasper B. Hansen and Hans Bräuner-Osborne -- Immunoprecipitation and phosphorylation of G protein-coupled receptors / Walter G. Thomas
Summary 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
Bibliography Includes bibliographical references and index
Notes English
Print version record
Subject Drug development.
G proteins -- Receptors.
Receptors, G-Protein-Coupled.
Drug Discovery.
Genre/Form Laboratory Manual.
Form Electronic book
Author Leifert, Wayne R.
LC no. 2009921196
ISBN 1603273174 (Springer e-ISBN)
9781603273176 (Springer e-ISBN)
(hbk. ; alk. paper)
(hbk. ; alk. paper)