β-arrestin-mediated signaling improves the efficacy of therapeutics

Β-arrestins (β-arrestin-1 and β-arrestin-2) were first identified as proteins that have the ability to desensitize g protein-coupled receptors (gpcrs). however,it has recently been found that β-arrestins can activate signaling pathways independent of g protein activation. the diversity of these signaling pathways has also been recognized. this leads to an appreciation of β-arrestin-biased agonists,which is a new class of drugs that selectively activate β-arrestin-mediated signaling without g protein activation. in this review,we will discuss the recent advance of β-arrestin-mediated signaling pathways,including a brief account of different biased agonists,their pharmacological applications,and novel β-arrestin research. © the japanese pharmacological society.