Reviews the structural basis of ligand binding and allosteric mechanisms Presents concrete examples of structure-based drug discovery Illustrates GPCR biased signaling in physiological contexts

Zusammenfassung

Inhalt
Structures of Non-rhodopsin GPCRs Elucidated Through X-Ray Crystallography.- NMR Spectroscopy for the Characterization of GPCR Energy Landscapes.- Structure and Activation Mechanism of GPCRs.- Structure-Based Discovery of GPCR Ligands from Crystal Structures and Homology Models.- Integration on Ligand and Structure Based Approaches in GPCRs.- Biased Agonist Pharmacochaperones: Small Molecules in the Toolbox for Selectively Modulating GPCR Activity.- Endosomal PTH Receptor Signaling Through cAMP and Its Consequence for Human Medicine.- Structure and Function Studies of GPCRs by Site-Specific Incorporation of Unnatural Amino Acids.- Fluorescent-Based Strategies to Investigate G Protein-Coupled Receptors: Evolution of the Techniques to a Better Understanding.- Modulation of Metabotropic Glutamate Receptors by Orthosteric, Allosteric, and Light-Operated Ligands.