The recombinant GABA transporter GAT1 is downregulated upon activation of protein kinase C

FEBS Letters

Sato, Kohji¹  Betz, Heinrich¹  Schloss, Patrick¹ 

[1] Abteilung Neurochemie, Max-Planck-Institut für Hirnforschung, Deutschordenstrasse 46, D-60528 Frankfurt, Germany

关键词: GABA uptake;    Neurotransmitter transporter;    Protein kinase C;    Rat;    GABA;    γ-aminobutyric acid;    GAT;    GABA transporter;    H7;    1-(5-isoquinolinylsulphonyl)-2-methylpiperazine;    HEK cell;    human embryonic kidney cell;    PMA;    phorbol 12-myristate 13-acetate;    PKC;    protein kinase C;    SERT;    serotonin transporter;    TPA;    12-0-tetradecanoylphorbol-13-acetate;    PDD;    4α-phorbol-12;    13-dide-canoate;   

DOI  :  10.1016/0014-5793(95)01191-G

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Treatment of human embryonic kidney 293 cells expressing the rat γ-aminobutyric acid (GABA) transporter 1 (GAT1) with the protein kinase C (PKC) activator phorbol 12-myristate 13-acetate (PMA) was found to decrease the velocity of specific [³H]GABA uptake. This downregulation varied with extracellular GABA concentration and was blocked by the PKC inhibitors 1-(5-isoquinolinylsulphonyl)-2-methylpiperazine (H7) and staurosporine. An about 50% reduction of uptake velocity by PMA treatment was observed at GABA concentrations > 1 μM, whereas only a minor effect was seen at low substrate concentrations. These data indicate that GAT1 activity is downregulated by PKC activation.

【 授权许可】

Unknown