ACTIVATION OF PROTEIN-KINASE-C RESULTS IN DOWN-MODULATION OF DIFFERENT RECOMBINANT GABA(A)-CHANNELS

被引：56

作者：

SIGEL, E ^{[1
]}

BAUR, R ^{[1
]}

MALHERBE, P ^{[1
]}

机构：

[1] HOFFMANN LA ROCHE AG,PHARMACEUT RES DEPT,CH-4051 BASEL,SWITZERLAND

来源：

FEBS LETTERS | 1991年 / 291卷 / 01期

关键词：

XENOPUS OOCYTE; GAMMA-AMINOBUTYRATE RECEPTOR; ION CHANNEL; EXPRESSION; PHORBOL ESTER; PROTEIN KINASE-C;

D O I：

10.1016/0014-5793(91)81124-Q

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Different combinations of cloned rat brain subunits of the GABA(A) receptor were expressed in Xenopus oocytes. The effect of the phorbol ester PMA, an activator of protein kinase C, on the expressed GABA-gated ion current was determined. Ion currents were diminished by beta-PMA, but not by the control substance alpha-PMA, irrespective of the subunit combination studied. The mechanism of current decrease was investigated in more detail for the subunit combination alpha-5-beta-2-gamma-2. The reversal potential of the current remained unaffected, while the maximal current amplitude was decreased and the apparent K(a) for GABA-dependent channel gating was shifted to higher concentrations.

引用

页码：150 / 152

页数：3

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