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肾素抑制剂

Renin inhibitors.

作者信息

Greenlee W J

机构信息

Merck Sharp and Dohme Research Laboratories, Merck and Co., Inc., Rahway, New Jersey 07065.

出版信息

Pharm Res. 1987 Oct;4(5):364-74. doi: 10.1023/a:1016422009662.

Abstract

Pharmacological intervention in the renin-angiotensin system (RAS) by inhibition of angiotensin-converting enzyme (ACE) is an effective therapy for the majority of hypertensive patients and a major advance in the treatment of hypertension and congestive heart failure. The success achieved with ACE inhibitors has increased interest in inhibitors of renin. Renin catalyzes the first and rate-limiting step of the RAS and, unlike ACE, has a high specificity for its endogenous protein substrate. A therapeutic agent that inhibits this specific reaction could have advantages over antihypertensive drugs with less specific modes of action. Although inhibitors of renin have been studied for over two decades, only recently has substantial progress been made toward potent, low molecular weight inhibitors likely to become useful therapeutic agents. Recent advances in the development of renin inhibitors, especially progress toward clinically useful inhibitors, is reviewed.

摘要

通过抑制血管紧张素转换酶(ACE)对肾素-血管紧张素系统(RAS)进行药理干预,对大多数高血压患者来说是一种有效的治疗方法,也是高血压和充血性心力衰竭治疗的一项重大进展。ACE抑制剂取得的成功增加了人们对肾素抑制剂的兴趣。肾素催化RAS的第一步也是限速步骤,与ACE不同,它对其内源性蛋白质底物具有高度特异性。一种抑制这种特定反应的治疗剂可能比作用方式较不特异的抗高血压药物具有优势。尽管对肾素抑制剂的研究已有二十多年,但直到最近才在可能成为有用治疗剂的强效、低分子量抑制剂方面取得了实质性进展。本文综述了肾素抑制剂开发的最新进展,特别是在临床有用抑制剂方面取得的进展。

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