Biomol Ther.  2016 Sep;24(5):475-481. 10.4062/biomolther.2016.015.

Functional Regulation of Dopamine D₃ Receptor through Interaction with PICK1

Affiliations
  • 1Pharmacology Laboratory, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea. kmkim@jnu.ac.kr
  • 2Medicinal Chemistry Laboratory, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea.
  • 3Physical Pharmacy Laboratory, College of Pharmacy, Chonnam National University, Gwangju 61186, Republic of Korea.

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.

Keyword

Dopamine D₂ receptor; Dopamine D₃ receptor; Dopamine transporter; PICK1; Cell surface expression; Tolerance
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