beta-Arrestin-Mediated Signaling Improves the Efficacy of Therapeutics

beta-Arrestins (beta-arrestin-1 and beta-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 beta-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 beta-arrestin-biased agonists, which is a new class of drugs that selectively activate beta-arrestin-mediated signaling without G protein activation. In this review, we will discuss the recent advance of beta-arrestin-mediated signaling pathways, including a brief account of different biased agonists, their pharmacological applications, and novel beta-arrestin research.