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KMID : 0606920160240050475
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Biomolecules & Therapeutics
2016 Volume.24 No. 5 p.475 ~ p.481
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Functional Regulation of Dopamine D3 Receptor through Interaction with PICK1
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Zheng Mei
Zhang Xiaohan
Min Chengchun
Choi Bo-Gil
Oh In-Joon
Kim Kyeong-Man
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Abstract
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PICK1, a PDZ domain-containing protein, is known to increase the reuptake activities of dopamine transporters by increasing their expressions on the cell surface. Here, we report a direct and functional interaction between PICK1 and dopamine D3 receptors (D3R), which act as autoreceptors to negatively regulate dopaminergic neurons. PICK1 colocalized with both dopamine D2 receptor (D2R) and D3R in clusters but exerted different functional influences on them. The cell surface expression, agonist affinity, endocytosis, and signaling of D2R were unaffected by the coexpression of PICK1. On the other hand, the surface expression and tolerance of D3R were inhibited by the coexpression of PICK1. These findings show that PICK1 exerts multiple effects on D3R functions.
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KEYWORD
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Dopamine D2 receptor, Dopamine D3 receptor, Dopamine transporter, PICK1, Cell surface expression, Tolerance
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