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蛋白激酶:平滑肌中大电导钙激活钾通道的调节者

Protein kinases: tuners of the BKCa channel in smooth muscle.

作者信息

Schubert R, Nelson M T

机构信息

Institute of Physiology, University of Rostock, PSF 100888, D-18055, Rostock, Germany.

出版信息

Trends Pharmacol Sci. 2001 Oct;22(10):505-12. doi: 10.1016/s0165-6147(00)01775-2.

Abstract

Large-conductance, Ca(2+)-activated K(+) (BK(Ca)) channels in smooth muscle cells are unique because they integrate changes in both intracellular Ca(2+) and membrane potential. Protein kinases such as cAMP-dependent protein kinase, cGMP-dependent protein kinase and protein kinase C can affect tissue function by 'tuning' the apparent Ca(2+)- and/or voltage-sensitivity of the BK(Ca) channel to physiological changes in both Ca(2+) concentrations and membrane potential. However, despite the central importance of kinase-mediated modulation of BK(Ca) channels in different smooth muscle tissues, many key issues, including the sites and mechanisms of actions of protein kinases, remain unresolved. In this article, the role of protein kinases in the regulation of BK(Ca) channels is discussed.

摘要

平滑肌细胞中的大电导钙激活钾(BK(Ca))通道独具特色,因为它们整合了细胞内钙离子和膜电位的变化。诸如环磷酸腺苷依赖性蛋白激酶、环磷酸鸟苷依赖性蛋白激酶和蛋白激酶C等蛋白激酶,可通过“调节”BK(Ca)通道对钙离子浓度和膜电位生理变化的表观钙敏感性和/或电压敏感性,来影响组织功能。然而,尽管激酶介导的BK(Ca)通道调节在不同平滑肌组织中至关重要,但许多关键问题,包括蛋白激酶的作用位点和作用机制,仍未得到解决。本文将讨论蛋白激酶在BK(Ca)通道调节中的作用。

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