The adenosine class of heterotrimeric guanine nucleotide–binding protein (G protein)–coupled
receptors (GPCRs) mediates the important role of extracellular adenosine in many …

The design of G-protein-coupled receptor (GPCR) allosteric modulators, an active area of
modern pharmaceutical research, has proved challenging because neither the binding modes …

Biased agonism describes the ability of ligands to stabilize different conformations of a
GPCR linked to distinct functional outcomes and offers the prospect of designing pathway-specific …

It is now acknowledged that G protein–coupled receptors, the largest class of drug targets,
adopt multiple active states that can be preferentially stabilized by orthosteric ligands or …

The recent progress in crystallography of G-protein coupled receptors opens an unprecedented
venue for structure-based GPCR drug discovery. To test efficiency of the structure-based …

Biased agonism at G protein–coupled receptors describes the phenomenon whereby some
drugs can activate some downstream signaling activities to the relative exclusion of others. …

Atypical antipsychotic drugs (APDs) have been hypothesized to show reduced extrapyramidal
side effects (EPS) due to their rapid dissociation from the dopamine D 2 receptor. However…

Although classical approaches to G-protein-coupled receptor (GPCR) drug design have
targeted the orthosteric binding site, potentially all GPCRs possess druggable allosteric sites. In …

G-protein-coupled receptors (GPCRs) are one of the most tractable classes of drug targets.
These dynamic proteins can adopt multiple active states that are linked to distinct functional …

SB269652 is to our knowledge the first drug-like allosteric modulator of the dopamine D 2
receptor (D 2 R), but it contains structural features associated with orthosteric D 2 R …