Title | G Protein-Coupled Receptors in Drug Discovery [electronic resource] : Methods and Protocols / edited by Marta Filizola |
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Imprint | New York, NY : Springer New York : Imprint: Humana Press, 2015 |
Edition | 2nd ed. 2015 |
Connect to | http://dx.doi.org/10.1007/978-1-4939-2914-6 |
Descript | XII, 327 p. 71 illus., 50 illus. in color. online resource |
Purification 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