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汽巴 - 嘉基杰出研究奖。肾上腺素能受体功能的磷酸化调节。

Ciba-Geigy award for outstanding research. Regulation of adrenergic receptor function by phosphorylation.

作者信息

Lefkowitz R J, Caron M G

出版信息

J Mol Cell Cardiol. 1986 Sep;18(9):885-95. doi: 10.1016/s0022-2828(86)80003-7.

Abstract

The various subtypes of adrenergic receptors represent distinct structural entities which are coupled in different ways to two major transmembrane signalling systems, the adenylate cyclase and phosphatidyl-inositol pathways. Recent evidence suggests that the functional linkage of both beta and alpha 1-adrenergic receptors to their respective effector systems is regulated by covalent modification of the receptors by phosphorylation-dephosphorylation reactions. Receptor phosphorylation appears to lead to desensitization of the biological response to receptor stimulation. Several kinases including protein kinase A, protein kinase C and a cAMP independent kinase appear to participate in these reactions.

摘要

肾上腺素能受体的各种亚型代表不同的结构实体,它们以不同方式与两种主要的跨膜信号系统(腺苷酸环化酶和磷脂酰肌醇途径)偶联。最近的证据表明,β和α1肾上腺素能受体与其各自效应系统的功能联系是通过磷酸化-去磷酸化反应对受体进行共价修饰来调节的。受体磷酸化似乎导致对受体刺激的生物学反应脱敏。包括蛋白激酶A、蛋白激酶C和一种不依赖cAMP的激酶在内的几种激酶似乎参与了这些反应。

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