Idris Iskandar, Gray Samuel, Donnelly Richard
Division of Vascular Medicine, School of Medical and Surgical Sciences, University of Nottingham, Derbyshire Royal Infirmary, United Kingdom.
Ann N Y Acad Sci. 2002 Jun;967:176-82.
Protein kinase C (PKC) is a family of multifunctional isozymes that plays an important role in the regulation of intracellular insulin signal transduction in various insulin-sensitive tissues. This article highlights current understanding on the mechanism of PKC-induced insulin resistance in skeletal muscle, a major target site for insulin-mediated glucose disposal. Initial, apparently contradictory findings on the role of PKC on insulin action can be explained on the basis that certain PKC isoforms (e.g., -zeta and -lambda) have been identified as downstream targets of PI3-kinase activation, while DAG-sensitive PKCs (e.g., -theta; and -epsilon) have negative regulatory effects on insulin signaling. Hence, pharmacological therapies targeting specific PKC isoforms could enhance insulin action and improve glycemic control in patients with impaired glucose tolerance and overt diabetes.
蛋白激酶C(PKC)是一类多功能同工酶,在各种胰岛素敏感组织中细胞内胰岛素信号转导的调节中发挥重要作用。本文重点介绍了目前对PKC诱导骨骼肌胰岛素抵抗机制的理解,骨骼肌是胰岛素介导的葡萄糖代谢的主要靶位点。关于PKC对胰岛素作用的作用最初看似矛盾的发现可以基于以下事实来解释:某些PKC同工型(例如ζ和λ)已被确定为PI3激酶激活的下游靶点,而二酰甘油敏感的PKC(例如θ和ε)对胰岛素信号传导具有负调节作用。因此,针对特定PKC同工型的药物治疗可以增强胰岛素作用,并改善糖耐量受损和显性糖尿病患者的血糖控制。