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目的综述钠氢交换蛋白1(NHE-1)磷酸化激酶p90核糖体S6激酶(RSK)及其抑制剂的最新研究进展。方法结合近期国内外的文献,综合介绍了RSK的结构、介导NHE-1活性的关系以及RSK抑制剂的研究现状和发展趋势。结果与结论NHE-1是一类分布广泛的膜蛋白,具有调节细胞内的pH值和细胞容量的功能,在心脑血管疾病的发生和发展中起着重要的作用。RSK是NHE-1的重要调节蛋白,针对RSK设计的抑制剂,可间接地抑制NHE-1磷酸化激活而发挥心脑血管治疗的作用。为针对NHE-1药物的研发提供了新的方向。
OBJECTIVE: To summarize recent progress in the study of p65 ribosomal S6 kinase (RSK) and its inhibitors of sodium-hydrogen exchange protein 1 (NHE-1) phosphorylation kinase. Methods Based on the recent literatures at home and abroad, the relationship between the structure of RSK and the activity of NHE-1 and the research status and development trend of RSK inhibitors were introduced. RESULTS AND CONCLUSION NHE-1 is a kind of widely distributed membrane protein with the function of regulating intracellular pH value and cell volume, which plays an important role in the occurrence and development of cardiovascular and cerebrovascular diseases. RSK is an important regulator of NHE-1, an inhibitor of RSK design, which can indirectly inhibit the activation of phosphorylation of NHE-1 to exert the effect of cardiovascular therapy. It provides a new direction for the research and development of NHE-1 drugs.