Expanding neuropeptide signalling by multiplying receptor functional states and sub-cellular locations

Neuropeptide signalling is primarily based on activation of G protein-coupled receptors (GPCRs), the largest family of membrane receptors. GPCRs are involved in multiple physiological processes and are important drug targets for many human diseases. In this at a glance review, we focus on the recent advances in GPCR signalling related to the different structural and functional features of complexes involved in G protein- and arrestin-mediated signalling, receptor dimerization and oligomerization, modulation and transactivation of other signalling proteins and receptor compartimentalization. Our goal is to highlight the astonishingly complex and diverse network of signal transduction events that could arise from the activation of neuropeptide receptors.