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蛋白激酶C相互作用蛋白:从功能到药理学

PKC-interacting proteins: from function to pharmacology.

作者信息

Poole Alastair W, Pula Giordano, Hers Ingeborg, Crosby David, Jones Matthew L

机构信息

Department of Pharmacology, School of Medical Sciences, University Walk, Bristol BS8 1TD, UK.

出版信息

Trends Pharmacol Sci. 2004 Oct;25(10):528-35. doi: 10.1016/j.tips.2004.08.006.

Abstract

Protein kinase C (PKC) is a ubiquitously expressed family of kinases that have key roles in regulating multiple cellular activities. The activity of this family is controlled tightly by several molecular mechanisms, including interaction with binding-partner proteins. These PKC-interacting proteins (C-KIPs) confer specificity for individual PKC isoforms by regulating the activity and cellular localization of PKC isoforms and, subsequently, the ability of these isoforms to specifically regulate cellular functional events. Although many C-KIPs have been identified by genome and proteome-mining approaches, it is important to address the specificity and function of the interactions in greater detail because they might form novel drug targets. In this article, we review recent work on C-KIPs and the implications for pharmacological and therapeutic development.

摘要

蛋白激酶C(PKC)是一类广泛表达的激酶家族,在调节多种细胞活动中起关键作用。该家族的活性受到多种分子机制的严格控制,包括与结合伴侣蛋白的相互作用。这些与PKC相互作用的蛋白(C-KIPs)通过调节PKC亚型的活性和细胞定位,进而调节这些亚型特异性调节细胞功能事件的能力,赋予单个PKC亚型特异性。尽管通过基因组和蛋白质组挖掘方法已经鉴定出许多C-KIPs,但更详细地研究这些相互作用的特异性和功能很重要,因为它们可能形成新的药物靶点。在本文中,我们综述了关于C-KIPs的最新研究工作及其对药理学和治疗学发展的意义。

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