G protein-coupled receptors (GPCRs) are a family of cell-surface proteins that play critical
roles in regulating a variety of pathophysiological processes and thus are targeted by almost …

G protein–coupled receptors engage both G proteins and β-arrestins, and their coupling can
be biased by ligands and mutations. Here, to resolve structural elements and mechanisms …

G protein‐coupled receptors (GPCRs) are membrane‐bound proteins that are ubiquitously
expressed in many cell types and take part in mediating multiple signaling pathways …

G protein–coupled receptors (GPCRs) are important therapeutic targets that exhibit
functional selectivity (biased signaling), in which different ligands or receptor variants elicit …

While the dynamics of the intracellular surface in agonist-stimulated GPCRs is well studied,
the impact of GPCR dynamics on G-protein selectivity remains unclear. Here, we combine …

The M2 muscarinic acetylcholine receptor (M2R) is a prototypical GPCR that plays important
roles in regulating heart rate and CNS functions. Crystal structures provide snapshots of the …

Here, we report the design and use of G protein-coupled receptor-based biosensors to
monitor ligand-mediated conformational changes in receptors in intact cells. These …

The high affinity dopamine D4 receptor ligand APH199 and derivatives thereof exhibit bias
toward the Gi signaling pathway over β-arrestin recruitment compared to quinpirole. Based …

1, 4-Disubstituted aromatic piperazines are privileged structural motifs recognized by
aminergic G protein-coupled receptors. Connection of a lipophilic moiety to the …

The histamine H1 receptor (H1R) is a G protein-coupled receptor (GPCR) and plays a key
role in allergic reactions upon activation by histamine which is locally released from mast …