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020 _a9781493929146
024 7 _a10.1007/978-1-4939-2914-6
_2doi
040 _aES-MaUEC
_bspa
_cES-MaUEC
_dES-MaUEC
050 4 _aQP552 .G16
_b2015 EB
245 0 0 _aG Protein-Coupled Receptors in Drug Discovery
_b: Methods and Protocols
_cedited by Marta Filizola.
250 _a2nd edition 2015
264 1 _aNew York, NY
_bSpringer International Publishing
_c2015
300 _a1 recurso en línea (XII, 327 páginas)
_b71 ilustraciones, 50 ilustraciones a color
336 _atexto
_btxt
_2rdacontent
337 _aelectrónico
_bc
_2rdamedia
338 _arecurso electrónico
_bcr
_2rdacarrier
347 _aarchivo de texto
_bPDF
490 0 _aMethods in Molecular Biology
_x1940-6029
_v1335
505 0 _aPurification of Stabilized GPCRs for Structural and Biophysical Analyses -- Purification and Crystallization of a Thermostabilized Agonist-Bound Conformation of the Human Adenosine A2A Receptor -- 2D Projection Analysis of GPCR Complexes by Negative Stain Electron Microscopy -- Nuts and Bolts of CF3 and CH3 NMR Towards the Understanding of Conformational Exchange of GPCRs -- Single-Molecule Fluorescence Microscopy for the Analysis of Fast Receptor Dynamics -- Quantitative Multi-Color Detection Strategies for Bioorthogonally-Labeled GPCRs -- Approaches to Characterize and Quantify Oligomerization of GPCRs -- Monitoring G Protein Activation in Cells with BRET -- Use of Fluorescence Indicators in Receptor Ligands -- Detection and Quantification of Intracellular Signalling Using FRET-Based Biosensors and High Content Imaging -- The Measurement of Receptor Signaling Bias -- Approaches to Assess Functional Selectivity in GPCRs: Evaluating G Protein Signaling in an Endogenous Environment -- Bioluminescence Resonance Energy Transfer Approaches to Discover Bias in GPCR Signaling -- Virus-Mediated Expression of DREADDs for In Vivo Metabolic Studies -- High-Throughput Screening for Allosteric Modulators of GPCRs -- Radioligand Binding Assay for an Exon 11-Associated Mu Opioid Receptor Target -- Docking and Virtual Screening Strategies for GPCR Drug Discovery -- The Dynamic Process of Drug-GPCR Binding at either Orthosteric or Allosteric Sites Evaluated by Metadynamics -- Experiment-Guided Molecular Modeling of Protein-Protein Complexes Involving GPCRs -- Interaction Fingerprints and Their Applications to Identify Hot Spots.
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.
988 _aSpringer_Protocols_2015
650 7 _2embne
_9147588
_aProteínas G
776 0 8 _iPrinted edition:
_z9781493929139
776 0 8 _iPrinted edition:
_z9781493929153
776 0 8 _iPrinted edition:
_z9781493949670
856 4 0 _uhttps://go.openathens.net/redirector/universidadeuropea.es?url=https://doi.org/10.1007/978-1-4939-2914-6
_zAcceso a este recurso digital (usuarios Universidad Europea de Madrid)
942 _2lcc
_cLE
998 _b12/2023
_dz
_ean
_zSI