G protein-biased agonists of the μ-opioid receptor (MOPr) have been proposed as an improved
class of opioid analgesics. Recent studies have been unable to reproduce the original …

The functional role of heteromers of G-protein-coupled receptors is a matter of debate. In the
present study, we demonstrate that heteromerization of adenosine A 1 receptors (A 1 Rs) …

There is evidence for strong functional antagonistic interactions between adenosine A 2A
receptors (A 2A Rs) and dopamine D 2 receptors (D 2 Rs). Although a close physical …

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. …

G protein‐coupled chemokine receptors and their peptidergic ligands are interesting
therapeutic targets due to their involvement in various immune‐related diseases, including …

The existence of A 2A -D 2 heteromeric complexes is based on coimmunoprecipitation studies
and on fluorescence resonance energy transfer and bioluminescence resonance energy …

Antagonistic and reciprocal interactions are known to exist between adenosine and dopamine
receptors in the striatum. In the present study, double immunofluorescence experiments …

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 …

Following inducible expression in HEK293 cells, the human orexin-1 receptor was targeted
to the cell surface but became internalized following exposure to the peptide agonist orexin A…