Functional Regulation of Dopamine D₃ Receptor through Interaction with PICK1.
10.4062/biomolther.2016.015
- Author:
Mei ZHENG
1
;
Xiaohan ZHANG
;
Chengchun MIN
;
Bo Gil CHOI
;
In Joon OH
;
Kyeong Man KIM
Author Information
1. Pharmacology Laboratory, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea. kmkim@jnu.ac.kr
- Publication Type:Original Article
- Keywords:
Dopamine D₂ receptor;
Dopamine D₃ receptor;
Dopamine transporter;
PICK1;
Cell surface expression;
Tolerance
- MeSH:
Autoreceptors;
Dopamine Plasma Membrane Transport Proteins;
Dopamine*;
Dopaminergic Neurons;
Endocytosis;
Hand
- From:Biomolecules & Therapeutics
2016;24(5):475-481
- CountryRepublic of Korea
- Language:English
-
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.
