title: Functional Regulation of Dopamine D₃ Receptor through Interaction with PICK1.
abstract: 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.
authors.affiliation: Pharmacology Laboratory, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea.
authors.forename: Mei
authors.initials: M
authors.lastname: Zheng
authors.affiliation: Pharmacology Laboratory, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea.
authors.forename: Xiaohan
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Pharmacology Laboratory, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea.
authors.forename: Chengchun
authors.initials: C
authors.lastname: Min
authors.affiliation: Medicinal Chemistry Laboratory, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea.
authors.forename: Bo-Gil
authors.initials: BG
authors.lastname: Choi
authors.affiliation: Physical Pharmacy Laboratory, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea.
authors.forename: In-Joon
authors.initials: IJ
authors.lastname: Oh
authors.affiliation: Pharmacology Laboratory, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea.
authors.forename: Kyeong-Man
authors.initials: KM
authors.lastname: Kim
keywords: Cell surface expression; Dopamine D₂ receptor; Dopamine D₃ receptor; Dopamine transporter; PICK1; Tolerance