Therapeutic Potential of Targeting ß-Arrestin
ß-arrestins are multifunctional proteins that modulate heptahelical 7 transmembrane receptors, also known as G protein-coupled receptors (GPCRs), a superfamily of receptors that regulate most physiological processes.
Richard A. Bond +3 more
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Programmed cell death (apoptosis) is a coordinated set of events eventually leading to the massive activation of specialized proteases (caspases) that cleave numerous substrates, orchestrating fairly uniform biochemical changes than culminate in cellular suicide. Apoptosis can be triggered by a variety of stimuli, from external signals or growth factor
Seunghyi, Kook +2 more
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The α-arrestin ARRDC3 mediates ALIX ubiquitination and G protein-coupled receptor lysosomal sorting. [PDF]
The sorting of G protein-coupled receptors (GPCRs) to lysosomes is critical for proper signaling and cellular responses. We previously showed that the adaptor protein ALIX regulates lysosomal degradation of protease-activated receptor-1 (PAR1), a GPCR ...
Dores, Michael R +4 more
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Mammalian α arrestins link activated seven transmembrane receptors to Nedd4 family e3 ubiquitin ligases and interact with β arrestins. [PDF]
The complement of fungal cell surface proteins is widely regulated by ubiquitination of membrane proteins, which results in their endocytosis and vacuolar degradation.
Fortune F Shea +4 more
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Insulin Action under Arrestin [PDF]
Insulin signaling is key to the etiology of metabolic syndrome. Recent work (Luan et al., 2009) uncovers a role for beta-arrestin, previously known to control GPCR desensitization, in insulin signaling. In mouse models, beta-arrestin-2 controls whole-body insulin action by regulating assembly of a complex containing insulin receptor, c-Src, and Akt.
Stöckli, Jacqueline, James, David E.
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Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser. [PDF]
G-protein-coupled receptors (GPCRs) signal primarily through G proteins or arrestins. Arrestin binding to GPCRs blocks G protein interaction and redirects signalling to numerous G-protein-independent pathways.
Barty, Anton +71 more
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Distinct cellular and subcellular distributions of G protein-coupled receptor kinase and arrestin isoforms in the striatum. [PDF]
G protein-coupled receptor kinases (GRKs) and arrestins mediate desensitization of G protein-coupled receptors (GPCR). Arrestins also mediate G protein-independent signaling via GPCRs.
Evgeny Bychkov +4 more
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β‐arrestin‐biased ACKR3 Promotes Gαi:β‐arrestin Complex Formation
Atypical chemokine receptor 3 (ACKR3)—previously known as CXC‐chemokine receptor 7 (CXCR7)—is involved in a wide range of physiological processes including angiogenesis, neuronal development, and tumorigenesis. As a β‐arrestin biased G protein‐coupled receptor (GPCR), ACKR3 recruits β‐arrestin, but lacks G protein activity.
Taylor Kohlmann +2 more
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G protein-coupled receptor kinase-2 (GRK-2) regulates serotonin metabolism through the monoamine oxidase AMX-2 in Caenorhabditis elegans. [PDF]
G protein-coupled receptors (GPCRs) regulate many animal behaviors. GPCR signaling is mediated by agonist-promoted interactions of GPCRs with heterotrimeric G proteins, GPCR kinases (GRKs), and arrestins.
Aryal, Dipendra K. +5 more
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The vasopressin type 2 receptor (V2R) is an essential G protein-coupled receptor (GPCR) in renal regulation of water homeostasis. Upon stimulation, the V2R activates Gαs and Gαq/11, which is followed by robust recruitment of β-arrestins and receptor ...
Carole Daly +6 more
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