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020			_a9781493929139
020			_a1493929135
020			_z9781493929146
020			_a1493929143
035			_a(OCoLC)ocn908374534
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060	0	0	_aW1 _bME9616J v.1335 2016
060	1	0	_aQU 25
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130	0		_aG protein-coupled receptors in drug discovery (Filizola)
245	1	0	_aG protein-coupled receptors in drug discovery: methods and protocols / _cedited by Marta Filizola.
250			_aSecond edition.
260			_aNew York _bHumana Press _c2015
300			_axii, 327 pages : _billustrations (many color) ; _c26 cm.
490	1		_aMethods in molecular biology, _x1064-3745 ; _v1335
490	1		_aSpringer protocols, _x1949-2448
500			_aFirst edition edited by Wayne R. Leifert.
504			_aIncludes bibliographical references and index.
505	0	0	_tPurification of stabilized GPCRs for structural and biophysical analyses / _rJames C. Errey [and others] -- _tPurification and crystallization of a thermostabilized agonist-bound conformation of the human adenosine A2A receptor / _rChristopher G. Tate and Guillaume Lebon -- _t2D projection analysis of GPCR complexes by negative stain electron microscopy / _rAlys Peisley and Georgios Skiniotis -- _tNuts and bolts of CF3 and CH3 NMR towards the understanding of conformational exchange of GPCRs / _rR. Scott Prosser and Tae Hun Kim -- _tSingle-molecule fluorescence microscopy for the analysis of fast receptor dynamics / _rJulia Wagner [and others] -- _tQuantitative multi-color detection strategies for bioorthogonally labeled GPCRs / _rMinyoung Park [and others] -- _tApproaches to characterize and quantify oligomerization of GPCRs / _rSara Marsango, María José Varela, and Graeme Milligan -- _tMonitoring G protein activation in cells with BRET / _rIkuo Masuho, Kirill A. Martemyanov, and Nevin A. Lambert -- _tUse of fluorescence indicators in receptor ligands / _rKaleeckal G. Harikumar and Laurence J. Miller -- _tDetection and quantification of intracellular signaling using FRET-based biosensors and high content imaging / _rMichelle L. Halls [and others] -- _tMeasurement of receptor signaling bias / _rTerry Kenakin -- _tApproaches to assess functional selectivity in GPCRs : evaluating G protein signaling in an endogenous environment / _rLaura M. Bohn, Lei Zhou, and Jo-Hao Ho -- _tBioluminescence resonance energy transfer approaches to discover bias in GPCR signaling / _rElizabeth K.M. Johnstone and Kevin D.G. Pfleger -- _tVirus-mediated expression of DREADDs for in vivo metabolic studies / _rMario Rossi [and others] -- _tHigh-throughput screening for allosteric modulators of GPCRs / _rRobert L. Bertekap Jr. [and others] -- _tRadioligand binding assay for an exon 11-associated mu opioid receptor target / _rGina F. Marrone, Susruta Majumdar, and Gavril W. Pasternak -- _tDocking and virtual screening strategies for GPCR drug discovery / _rThijs Beuming [and others] -- _tDynamic process of drug-GPCR binding at either orthosteric or allosteric sites evaluated by metadynamics / _rSebastian Schneider, Davide Provasi, and Marta Filizola -- _tExperiment-guided molecular modeling of protein-protein complexes involving GPCRs / _rIrina Kufareva, Tracy M. Handel, and Ruben Abagyan -- _tInteraction fingerprints and their applications to identify hot spots / _rAndrés F. Marmolejo [and others].
520			_aThis detailed volume provides an overview of recent techniques employed in the field of G protein-coupled receptors (GPCRs) to screen for new drugs and to derive information about their receptor structure, dynamics, and function for the purpose of developing improved therapeutics. Owing to remarkable recent advances in the structural, biophysical, and biochemical analyses of these receptors, as well as a growing body of evidence hinting at the possible relevance of allosteric modulators, biased agonists, and oligomer-selective ligands as improved therapeutic agents, drug discovery for GPCRs has recently taken a completely new direction. For this book, expert contributors have shared their protocols and views on the impact of these methodologies on modern drug discovery. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Practical and fully updated, G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols, Second Edition serves as an ideal guide for a diverse audience from structural and molecular biologists to pharmacologists and drug designers who wish to explore this extensive class of key drug targets.--
650		0	_aG proteins _xReceptors.
650		0	_aDrug development. _913259
650	1	2	_aReceptors, G-Protein-Coupled.
650	2	2	_aDrug Discovery.
650		7	_aDrug development. _2fast _913259
650		7	_aG proteins _xReceptors. _2fast
655		2	_aLaboratory Manuals.
700	1		_aFilizola, Marta, _eeditor.
830		0	_aMethods in molecular biology (Clifton, N.J.) ; _vv. 1335.
830		0	_aSpringer protocols (Series) _98945
906			_a7 _bcbc _cpccadap _d2 _encip _f20 _gy-gencatlg
942			_2ddc _cBK
999			_c6996 _d6996