PHORBOL-ESTER-INDUCED PHOSPHORYLATION OF THE BETA-2-ADRENERGIC RECEPTOR DECREASES ITS COUPLING TO GS

被引：55

作者：

BOUVIER, M ^{[1
]}

GUILBAULT, N ^{[1
]}

BONIN, H ^{[1
]}

机构：

[1] UNIV MONTREAL,RECH SYST NERVEUX AUTONOME GRP,MONTREAL H3C 3J7,QUEBEC,CANADA

来源：

FEBS LETTERS | 1991年 / 279卷 / 02期

关键词：

BETA-2-ADRENERGIC RECEPTOR; PHOSPHORYLATION; PROTEIN KINASE-C; ADENYLYL CYCLASE; DESENSITIZATION; PHORBOL-ESTER; RECEPTOR UNCOUPLING;

D O I：

10.1016/0014-5793(91)80159-Z

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：

Phorbol-esters have been shown to modulate the beta-adrenergic-stimulated adenylyl cyclase in a number of cell lines. Here, using site directed mutagenesis, we investigate the role of the beta-2-adrenergic receptor phosphorylation by protein kinase C in this regulatory process. Mutation of the serine-261, -262, -344 and -345 of the beta-2-adrenergic receptor prevented the phorbol-ester-induced phosphorylation of the receptor. This mutation also abolished the phorbol-ester-induced decrease in high-affinity agonist binding and potency of the beta-2-adrenergic receptor. We suggest that protein kinase C mediated phosphorylation of the receptor promotes its functional uncoupling.

引用

页码：243 / 248

页数：6

共 39 条

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