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Rho激酶抑制剂的研究进展

Rresearch progress on the Rho kinase inhibitors

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【作者】 李航张明杰王东华孙婧譞何新益

【Author】 LI Hang;ZHANG Ming-jie;WANG Dong-hua;SUN Jing-xuan;HE Xin-yi;School of food science and Bioengineering, Tianjin agricultural university;Institute of Science, Tianjin university;Institute of pharmaceutical Science and Technology, Tianjin university;

【通讯作者】 何新益;

【机构】 天津农学院食品科学与生物工程学院天津大学理学院天津大学药物科学与技术学院

【摘要】 Rho激酶抑制剂是治疗心脑血管疾病的重要靶点,也是当前国内外研究的热点。本文对国内外关于Rho激酶结构组成、Rho激酶参与心脏衰竭发病机制、代谢综合征发病机制、参与MLC的磷酸化调控发病机制的研究工作进行了总结与分析。重点介绍了四大类的Rho激酶抑制剂,分别为异喹啉类、4-氨基吡啶类、吲唑类、酰胺和脲类,其代表物有Fasudil和Y-27632等化合物,并简述了Rho激酶抑制剂对神经细胞具有的修复作用。研究高效Rho激酶抑制剂,并深入研究其作用机理,对治疗心脑血管疾病具有重要的科学意义与应用价值,也是治疗心脑血管疾病新的发展方向。

【Abstract】 Rho kinase inhibitor is an important target in the treatment of cardiovascular and cerebrovascular diseases, and it is also a hot research topic at home and abroad.In this paper, domestic and foreign studies on Rho kinase′s structure, Rho kinase′s involvement in the heart failure, the pathogenesis of metabolic syndrome, and MLC phosphorylation were summarized and analyzed.Four kinds of Rho kinase inhibitors, namely isoquinoline, 4-aminopyridine inhibitors, indazole inhibitors, amides and ureas, were mainly introduced.The representative compounds were Fasudil and Y-27632 compounds, and the repair effect of Rho kinase inhibitors on nerve cells was briefly described.Further research on Rho kinase inhibitors had important scientific significance and application value for the treatment of cardiovascular and cerebrovascular diseases, and was also a new development direction for the treatment of cardiovascular and cerebrovascular diseases.

【关键词】 Rho激酶抑制剂法舒地尔Y-27632细胞突触
【Key words】 Rho kinase inhibitorFasudilY-27632cell synapse
【基金】 天津农学院科学研究与发展基金项目(20190107)资助;国家自然基金项目(31701569)资助
  • 【文献出处】 化学研究与应用 ,Chemical Research and Application , 编辑部邮箱 ,2021年02期
  • 【分类号】TQ464.8
  • 【被引频次】7
  • 【下载频次】366
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