GABA θ1 receptor: inhibition by protein kinase C activators

Tadashi Kusama; Manabu Sakurai; Yasuo Kizawa; George R. Uhl; Hajime Murakami

doi:10.1016/0922-4106(95)90086-1

GABA θ1 receptor: inhibition by protein kinase C activators

Tadashi Kusama, Manabu Sakurai, Yasuo Kizawa, George R. Uhl, Hajime Murakami

School of Medicine

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

Abstract

The effects of protein kinase C (PKC) activators on γ-aminobutyric acid (GABA) θ₁ receptor function were studied in θ₁-expressingXenopus oocytes. The PKC activator phorbol 12-myristate 13-acetate (PMA) but not the inactive analog phorbol 12-mono-myristate inhibited the GABA-gated chloride currents. Mezerein, a non-phorbol ester type PKC activator, also inhibited the θ₁ responses, but 8-chlorophenylthio-cyclic AMP, a protein kinase A activator, had no effect. The effect of PMA was significantly reduced by a PKC inhibitor, staurosporine. These results suggest that GABA θ₁ receptor function can be regulated by PKC-mediated phosphorylation events.

Original language	English (US)
Pages (from-to)	431-434
Number of pages	4
Journal	European Journal of Pharmacology: Molecular Pharmacology
Volume	291
Issue number	3
DOIs	https://doi.org/10.1016/0922-4106(95)90086-1
State	Published - Nov 30 1995

Keywords

Down-regulation
GABA θ receptor
Phorbol ester
Protein kinase C
Staurosporine
Xenopus oocyte

ASJC Scopus subject areas

Pharmacology

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10.1016/0922-4106(95)90086-1

Cite this

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title = "GABA θ1 receptor: inhibition by protein kinase C activators",

abstract = "The effects of protein kinase C (PKC) activators on γ-aminobutyric acid (GABA) θ1 receptor function were studied in θ1-expressingXenopus oocytes. The PKC activator phorbol 12-myristate 13-acetate (PMA) but not the inactive analog phorbol 12-mono-myristate inhibited the GABA-gated chloride currents. Mezerein, a non-phorbol ester type PKC activator, also inhibited the θ1 responses, but 8-chlorophenylthio-cyclic AMP, a protein kinase A activator, had no effect. The effect of PMA was significantly reduced by a PKC inhibitor, staurosporine. These results suggest that GABA θ1 receptor function can be regulated by PKC-mediated phosphorylation events.",

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author = "Tadashi Kusama and Manabu Sakurai and Yasuo Kizawa and Uhl, {George R.} and Hajime Murakami",

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T2 - inhibition by protein kinase C activators

AU - Kusama, Tadashi

AU - Sakurai, Manabu

AU - Kizawa, Yasuo

AU - Uhl, George R.

AU - Murakami, Hajime

PY - 1995/11/30

Y1 - 1995/11/30

N2 - The effects of protein kinase C (PKC) activators on γ-aminobutyric acid (GABA) θ1 receptor function were studied in θ1-expressingXenopus oocytes. The PKC activator phorbol 12-myristate 13-acetate (PMA) but not the inactive analog phorbol 12-mono-myristate inhibited the GABA-gated chloride currents. Mezerein, a non-phorbol ester type PKC activator, also inhibited the θ1 responses, but 8-chlorophenylthio-cyclic AMP, a protein kinase A activator, had no effect. The effect of PMA was significantly reduced by a PKC inhibitor, staurosporine. These results suggest that GABA θ1 receptor function can be regulated by PKC-mediated phosphorylation events.

AB - The effects of protein kinase C (PKC) activators on γ-aminobutyric acid (GABA) θ1 receptor function were studied in θ1-expressingXenopus oocytes. The PKC activator phorbol 12-myristate 13-acetate (PMA) but not the inactive analog phorbol 12-mono-myristate inhibited the GABA-gated chloride currents. Mezerein, a non-phorbol ester type PKC activator, also inhibited the θ1 responses, but 8-chlorophenylthio-cyclic AMP, a protein kinase A activator, had no effect. The effect of PMA was significantly reduced by a PKC inhibitor, staurosporine. These results suggest that GABA θ1 receptor function can be regulated by PKC-mediated phosphorylation events.

KW - Down-regulation

KW - GABA θ receptor

KW - Phorbol ester

KW - Protein kinase C

KW - Staurosporine

KW - Xenopus oocyte

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ER -

GABA θ1 receptor: inhibition by protein kinase C activators

Abstract

Keywords

ASJC Scopus subject areas

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