蛋白激酶C对内向整流钾离子通道的调节机制

Modulation mechanism of PKC upon inwardly rectifying potassium channels

内向整流钾离子(Kir)通道是在很多组织中广泛分布的一种钾离子通道,在维持钾离子平衡电位、调节细胞兴奋性和胰岛素分泌等方面发挥着重要的作用。Kir通道是众多调节因素作用的靶点,这些因素包括:K+、Mg2+、pH、ATP、G蛋白偶联受体(GPCR),磷脂酰肌醇4,5二磷酸(PIP2)、蛋白激酶A(PKA)、蛋白激酶C(PKC)、花生四烯酸(AA)等。由于很多细胞外信号是通过PKC信号转导通路来调控Kir通道的,多年来为了更好地界定PKC在调控Kir通道功能中所扮演的角色及机制,人们进行了大量而深入的研究。本文对PKC调节Kir通道机制的研究进展及目前提出的一些新观点进行综述。

Inwardly rectifying potassium （Kir） channels are widely distributed in many tissues and play important roles in physiological processes such as maintaining K＋ homeostasis,regulating cell excitability and insulin secretion.The activity of Kir channels is regulated by a number of modulators,such as K＋,Mg2＋,pH,ATP,GPCR,PIP2,PKA,PKC,AA（arachidonic acid）,etc.Study of the regulating mechanisms of Kir channel is a key step in understanding the physiology and physiopathology of these channels.Because many extra molecular signals regulate Kir channels via PKC pathway,much effort has been made over the past decade to understand role of PKC in regulating Kir channels.This paper summarizes the molecular basis of PKC modulation of Kir channels and the recent progression on the area.