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The role of KATP channels in cerebral ischemic stroke and diabetes.
Acta Pharmacologica Sinica ( IF 8.2 ) Pub Date : 2018-May-01 , DOI: 10.1038/aps.2018.10
Vivian Szeto , Nai-hong Chen , Hong-shuo Sun , Zhong-ping Feng

ATP-sensitive potassium (KATP) channels are ubiquitously expressed on the plasma membrane of cells in multiple organs, including the heart, pancreas and brain. KATP channels play important roles in controlling and regulating cellular functions in response to metabolic state, which are inhibited by ATP and activated by Mg-ADP, allowing the cell to couple cellular metabolic state (ATP/ADP ratio) to electrical activity of the cell membrane. KATP channels mediate insulin secretion in pancreatic islet beta cells, and controlling vascular tone. Under pathophysiological conditions, KATP channels play cytoprotective role in cardiac myocytes and neurons during ischemia and/or hypoxia. KATP channel is a hetero-octameric complex, consisting of four pore-forming Kir6.x and four regulatory sulfonylurea receptor SURx subunits. These subunits are differentially expressed in various cell types, thus determining the sensitivity of the cells to specific channel modifiers. Sulfonylurea class of antidiabetic drugs blocks KATP channels, which are neuroprotective in stroke, can be one of the high stoke risk factors for diabetic patients. In this review, we discussed the potential effects of KATP channel blockers when used under pathological conditions related to diabetics and cerebral ischemic stroke.

中文翻译:

KATP通道在脑缺血性中风和糖尿病中的作用。

ATP敏感钾(K ATP)通道在心脏,胰腺和大脑等多个器官的细胞质膜上普遍表达。K ATP通道在响应代谢状态时控制和调节细胞功能中起重要作用,这些功能被ATP抑制并被Mg-ADP激活,从而使细胞将细胞的代谢状态(ATP / ADP比)与细胞的电活动耦合膜。K ATP通道介导胰岛β细胞中的胰岛素分泌,并控制血管张力。在病理生理条件下,K ATP通道在缺血和/或缺氧期间对心肌细胞和神经元起细胞保护作用。钾ATP通道是一个杂八聚体复合物,由四个成孔的Kir6.x和四个调节性磺酰脲受体SURx亚基组成。这些亚基在各种细胞类型中差异表达,因此决定了细胞对特定通道修饰物的敏感性。磺脲类抗糖尿病药会阻断中风的神经保护性K ATP通道,可能是糖尿病患者中风的高风险因素之一。在这篇综述中,我们讨论了在与糖尿病和脑缺血性卒中相关的病理条件下使用时,K ATP通道阻滞剂的潜在作用。
更新日期:2018-04-19
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