G protein-coupled receptors (GPCRs) remain a major domain of pharmaceutical discovery.
The identification of GPCR lead compounds and their optimization are now structure-based …

Although a plurality of drugs target G-protein-coupled receptors (GPCRs), most have
emerged from classical medicinal chemistry and pharmacology programs and resemble one …

G-protein–coupled receptors (GPCRs) still offer enormous scope for new therapeutic targets.
Currently marketed agents are dominated by those with activity at aminergic receptors and …

Highlights•A wealth of GPCR ligand binding site data is available from structures and
mutants.•Integrating structural and mutant data is a tool to design mutagenesis …

G-protein-coupled receptors (GPCRs) comprise the largest single class of cell-surface
receptors, and have a history of being excellent therapeutic targets for a number of diseases …

The critical involvement of GPCRs (G-protein-coupled receptors) in nearly all physiological
processes, and the presence of these receptors at the interface between the extracellular …

Many central biological events rely on protein–ligand interactions. The identification and
characterization of protein-binding sites for ligands are crucial for the understanding of …

G protein‐coupled receptors (GPCRs) transmit extracellular signals into the intracellular
space, and play key roles in the physiological regulation of virtually every cell and tissue …

G protein-coupled receptors (GPCRs) are the most intensively studied drug targets, mostly
due to their substantial involvement in human pathophysiology and their pharmacological …

G-protein-coupled receptors (GPCRs) represent the most important class of drug targets
both in terms of therapeutic benefit and pharmaceutical sales. The majority of current GPCR …