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KMID : 0606920160240050517
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Biomolecules & Therapeutics
2016 Volume.24 No. 5 p.517 ~ p.522
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Roles of Dopamine D2 Receptor Subregions in Interactions with β-Arrestin2
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Zhang Xiaohan
Choi Bo-Gil
Kim Kyeong-Man
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Abstract
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β-Arrestins are one of the protein families that interact with G protein-coupled receptors (GPCRs). The roles of β-arrestins are multifaceted, as they mediate different processes including receptor desensitization, endocytosis, and G protein-independent signaling. Thus, determining the GPCR regions involved in the interactions with β-arrestins would be a preliminary step in understanding the molecular mechanisms involved in the selective direction of each function. In the current study, we determined the roles of the N-terminus, intracellular loops, and C-terminal tail of a representative GPCR in the interaction with β-arrestin2. For this, we employed dopamine D2 and D3 receptors (D2R and D3R, respectively), since they display distinct agonist-induced interactions with β-arrestins. Our results showed that the second and third intracellular loops of D2R are involved in the agonist-induced translocation of β-arrestins toward plasma membranes. In contrast, the N- and C-termini of D2R exerted negative effects on the basal interaction with β-arrestins.
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KEYWORD
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β-Arrestin, G protein-coupled receptors, Dopamine D2 receptor, Dopamine D3 receptor
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