Over the years, β-arrestins have emerged as multifunctional molecular scaffolding proteins regulating almost every imaginable G protein-coupled receptor (GPCR) function. Originally discovered as GPCR-desensitizing molecules, they have been shown to also serve as important regulators of GPCR signaling, sequestration, and vesicular trafficking. This broad functional role implicates β-arrestins as key regulatory proteins for cellular function. Hence, this chapter summarizes the current understanding of the β-arrestin family's unique ability to control the kinetics as well as the extent of GPCR activity at the level of desensitization, sequestration, and subsequent intracellular trafficking.
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