The activation of G protein-coupled receptors (GPCRs) is triggered by ligand binding to their
orthosteric sites, which induces ligand-specific conformational changes. Agonists and …

The human genome encodes 850 G protein-coupled receptors (GPCRs), half of which are
considered potential drug targets. GPCRs transduce extracellular stimuli into a plethora of …

Arrestins interact with G protein–coupled receptors (GPCRs) to stop G protein activation and
to initiate key signaling pathways. Recent structural studies shed light on the molecular …

Oxytocin (OT) and vasopressin (AVP) are conserved peptide signaling hormones that are
critical for diverse processes including osmotic homeostasis, reproduction, lactation and …

Cannabis activates the cannabinoid receptor 1 (CB1), which elicits analgesic and emotion
regulation benefits, along with adverse effects, via G i and β-arrestin signaling pathways …

The M2 muscarinic receptor (M2R) is a prototypical G-protein-coupled receptor (GPCR) that
serves as a model system for understanding GPCR regulation by both orthosteric and …

The small cyclic neuropeptide hormone oxytocin (OT) and its cognate receptor play a central
role in the regulation of social behaviour and sexual reproduction. Here we report the single …

Cryogenic electron microscopy (cryo-EM) has revolutionized the field of structural biology,
particularly in solving the structures of large protein complexes or cellular machineries that …

The type 2 bradykinin receptor (B2R) is a G protein-coupled receptor (GPCR) in the
cardiovascular system, and the dysfunction of B2R leads to inflammation, hereditary …

Genetic variations in the genes encoding G protein-coupled receptors (GPCRs) can disrupt
receptor structure and function, which can result in human genetic diseases. Disease …