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The recombinant GABA transporter GAT1 is downregulated upon activation of protein kinase C
Author(s) -
Sato Kohji,
Betz Heinrich,
Schloss Patrick
Publication year - 1995
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(95)01191-g
Subject(s) - staurosporine , protein kinase c , gaba transporter , activator (genetics) , transporter , chemistry , phorbol , extracellular , downregulation and upregulation , gamma aminobutyric acid , biochemistry , kinase , receptor , gene
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 [ 3 H]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 μ M, whereas only a minor effect was seen at low substrate concentrations. These data indicate that GAT1 activity is downregulated by PKC activation.