DEFINITION
β-arrestins (β-arrestin-1 / ARRB1 and β-arrestin-2 / ARRB2) are cytoplasmic adaptor proteins that bind GPCRs after receptor phosphorylation by G-protein-coupled receptor kinases (GRKs). They uncouple the receptor from heterotrimeric G-proteins (desensitisation), scaffold clathrin-mediated endocytosis (internalisation) and act as signalling hubs in their own right.
At GLP-1R and related class B receptors, β-arrestin recruitment is an important component of the overall signalling response and a central variable in biased-agonism research.
WHY IT MATTERS
β-arrestin biology is central to understanding receptor desensitisation, internalisation and biased signalling at GLP-1R.
RELATED
Compounds