蛋白激酶C(protein kinase C,PKC)是一个多基因家族,包含多种同工酶,分布广泛且功能复杂,在许多信号转导通路发挥重要作用。磷脂酰肌醇(4,5)二磷酸(PIP2)是分布在细胞膜中的磷脂类信号分子,在细胞中的分布和含量处于动态变化中。PIP2的水解后生成DAG和IP3。DAG可以直接激活PKC,而IP3通过调节细胞内钙离子的浓度从而改变钙依赖型PKCs的活性。同时,PKC通过激活PI4K或PIP5K可以调节细胞膜PIP2水平。PKCs使离子通道蛋白发生磷酸化,改变通道蛋白与PIP2的亲和力,从而影响PIP2对离子通道的调节。该文对PKCs和PIP2在细胞信号转导过程中相互调节的相关研究进展进行综述。
Protein kinase C(PKC) comprises a multigene family of related serine/threonine kinases that sit at the crossroads of many signal transduction pathways,playing an important role with complex functions.Phosphatidylinositol 4,5-bisphosphate(PIP2) is a key signaling molecule in cell membrane;it is not only the precursor of soluble inositol phosphate(IP3) and diacylglycerol(DAG),it can also act as a second messenger itself.Phospholipase C(PLC) hydrolyzes PIP2 to generate membrane-bound DAG,which activates PKC,and IP3,which mobilizes intracellular calcium to regulate the activity of PKC.The activation of PKC increases the activity of PI4 kinase or PIP5 kinase to enhance the synthesis of PIP2.This review deals with the mutual regulation between PKCs and PIP2 and current progress in related research.