β-Arrestins (βarrs) are multifunctional intracellular proteins with an ability to directly interact with a large number of cellular partners including the G protein-coupled receptors (GPCRs). βarrs contribute to multiple aspects of GPCR signaling, trafficking and downregulation. Considering the central involvement of GPCR signaling in the onset and progression of diverse types of cancers, βarrs have also emerged as key players in the context of investigating cancer phenotypes, and as potential therapeutic targets. In this chapter, we first provide a brief account of structure and function of βarrs and then highlight recent discoveries unfolding novel functional attributes of βarrs in breast cancer. We also underscore the recent paradigms of modulating βarr functions in cellular context and potential therapeutic opportunities going forward.
Keywords: Allosteric modulators; Biased agonism; Breast cancer; Cellular signaling; Endocytosis; GPCRs; Protein-protein interaction; β-Arrestins.
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