G protein–coupled receptors (GPCRs) constitute the largest family of membrane proteins in
the human genome and are important therapeutic targets. During the last decade, the …

The two β-arrestins, β-arrestin-1 and-2 (systematic names: arrestin-2 and-3, respectively),
are multifunctional intracellular proteins that regulate the activity of a very large number of …

Summary Serotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential
targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the …

Phosphorylation of G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs)
desensitizes G-protein signalling and promotes arrestin signalling, which is also modulated …

Abstract The β1-adrenoceptor (β1AR) is a G-protein-coupled receptor (GPCR) that couples
to the heterotrimeric G protein Gs. G-protein-mediated signalling is terminated by …

Over one-third of current drugs target G-protein-coupled receptors (GPCRs). Leveraging the
phenomenon of biased signaling, where different ligands that bind to the same GPCR …

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 …

Abstract β-arrestins mediate regulatory processes for over 800 different G protein-coupled
receptors (GPCRs) by adopting specific conformations that result from the geometry of the …

Arrestins have pivotal roles in regulating G protein-coupled receptor (GPCR) signalling by
desensitizing G protein activation and mediating receptor internalization,. It has been …

Agonist-induced GPCR phosphorylation is a key determinant for the binding and activation
of β-arrestins (βarrs). However, it is not entirely clear how different GPCRs harboring …