G Protein-Coupled Receptors in Drug Discovery

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.