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抑制 Rho-激酶在动脉高血压中的潜在益处。

Potential benefits of rho-kinase inhibition in arterial hypertension.

机构信息

Department of Physiology, University of Greifswald, Greifswalder Str. 11c, 17495, Greifswald, Karlsburg, Germany,

出版信息

Curr Hypertens Rep. 2013 Oct;15(5):506-13. doi: 10.1007/s11906-013-0373-0.

Abstract

Arterial hypertension is a major health problem, accounting for 12 % of the global death rate. A large proportion of patients treated for high blood pressure do not reach target blood pressure values. The question arises if new antihypertensive drugs could improve present hypertension treatment. Rho-kinases (ROCKs) are ubiquitously expressed serine/threonine kinases and involved in a variety of cell functions. They contribute to the pathogenesis of human and experimental hypertension. Pharmacological ROCK inhibition has been shown to effectively lower blood pressure in patients and experimental animals. Progress has been made towards the understanding on how non-selective ROCK inhibitors lower arterial pressure and efforts are currently undertaken to develop ROCK inhibitors to improve their specificity and isoenzyme selectivity. If introduction of ROCK inhibitors for the treatment of high blood pressure can significantly advance currently available options of antihypertensive pharmacotherapy awaits further experimental and clinical research.

摘要

动脉高血压是一个主要的健康问题,占全球死亡率的 12%。很大一部分接受高血压治疗的患者未达到目标血压值。那么问题来了,新的降压药物是否可以改善目前的高血压治疗。Rho 激酶(ROCKs)是普遍表达的丝氨酸/苏氨酸激酶,参与多种细胞功能。它们与人类和实验性高血压的发病机制有关。已经证明,药理学 ROCK 抑制可以有效降低患者和实验动物的血压。在了解非选择性 ROCK 抑制剂如何降低动脉压方面已经取得了进展,目前正在努力开发 ROCK 抑制剂以提高其特异性和同工酶选择性。如果 ROCK 抑制剂的引入可以显著改善目前可用的抗高血压药物治疗的选择,那么这有待进一步的实验和临床研究。

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