(RP)-8-PCPT-CGMPS, A NOVEL CGMP-DEPENDENT PROTEIN-KINASE INHIBITOR

被引：128

作者：

BUTT, E ^{[1
]}

EIGENTHALER, M ^{[1
]}

GENIESER, HG ^{[1
]}

机构：

[1] INST BIOL LIFE SCI,D-28199 BREMEN,GERMANY

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION | 1994年 / 269卷 / 02期

关键词：

(RP)-8-PCPT-CGMPS; ((RP)-8-(PARA-CHLOROPHENYLTHIO)GUANOSINE-3'; 5'-CYCLIC MONOPHOSPHOROTHIOATE); (INHIBITOR); CGMP-DEPENDENT PROTEIN KINASE; PLATELET;

D O I：

10.1016/0922-4106(94)90095-7

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

In the present study, the inhibitory effect of the cGMP analog (Rp)-8-(para-chlorophenylthio)guanosine-3',5'-cyclic monophosphorothioate ((Rp)-8-pCPT-cGMPS) on the cGMP-dependent protein kinase-mediated protein phosphorylation in intact human platelets was investigated. In vitro phosphorylation experiments with the substrate kemptide demonstrated an inhibition of the cGMP-dependent protein kinase by (Rp)-8-pCPT-cGMPS with a K-i of 0.5 mu M. In intact human platelets, (Rp)-8-pCPT-cGMPS antagonized the activation of the cGMP-dependent protein kinase by 8-pCPT-cGMP without affecting cAMP-dependent protein kinase or cGMP-regulated phosphodiesterases. The data obtained suggest that (Rp)-8-pCPT-cGMPS may be a useful tool for studying the role of cGMP in vitro and in intact cells.

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收藏

页码：265 / 268

页数：4

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