Tadashi Kusama , Manabu Sakurai , Yasuo Kizawa , George R. Uhl , Hajime Murakami
{"title":"GABA θ1受体:受到蛋白激酶C激活剂的抑制","authors":"Tadashi Kusama , Manabu Sakurai , Yasuo Kizawa , George R. Uhl , Hajime Murakami","doi":"10.1016/0922-4106(95)90086-1","DOIUrl":null,"url":null,"abstract":"<div><p>The effects of protein kinase C (PKC) activators on γ-aminobutyric acid (GABA) <em>θ</em><sub>1</sub> receptor function were studied in <em>θ</em><sub>1</sub>-expressing<em>Xenopus</em> 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 θ<sub>1</sub> 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 <em>θ</em><sub>1</sub> receptor function can be regulated by PKC-mediated phosphorylation events.</p></div>","PeriodicalId":100502,"journal":{"name":"European Journal of Pharmacology: Molecular Pharmacology","volume":"291 3","pages":"Pages 431-434"},"PeriodicalIF":0.0000,"publicationDate":"1995-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0922-4106(95)90086-1","citationCount":"23","resultStr":"{\"title\":\"GABA θ1 receptor: inhibition by protein kinase C activators\",\"authors\":\"Tadashi Kusama , Manabu Sakurai , Yasuo Kizawa , George R. Uhl , Hajime Murakami\",\"doi\":\"10.1016/0922-4106(95)90086-1\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The effects of protein kinase C (PKC) activators on γ-aminobutyric acid (GABA) <em>θ</em><sub>1</sub> receptor function were studied in <em>θ</em><sub>1</sub>-expressing<em>Xenopus</em> 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 θ<sub>1</sub> 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 <em>θ</em><sub>1</sub> receptor function can be regulated by PKC-mediated phosphorylation events.</p></div>\",\"PeriodicalId\":100502,\"journal\":{\"name\":\"European Journal of Pharmacology: Molecular Pharmacology\",\"volume\":\"291 3\",\"pages\":\"Pages 431-434\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1995-11-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0922-4106(95)90086-1\",\"citationCount\":\"23\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Pharmacology: Molecular Pharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/0922410695900861\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Pharmacology: Molecular Pharmacology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/0922410695900861","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
GABA θ1 receptor: inhibition by protein kinase C activators
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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