New therapeutics that antagonize endothelin: Promises and frustrations

被引：126

作者：

Remuzzi, G

Perico, N

Benigni, A

机构：

[1] Mario Negri Inst Pharmacol Res, I-24125 Bergamo, Italy

[2] Osped Riuniti Bergamo, Dept Med & Transplantat, I-24128 Bergamo, Italy

来源：

NATURE REVIEWS DRUG DISCOVERY | 2002年 / 1卷 / 12期

关键词：

D O I：

10.1038/nrd962

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

The discovery of endothelin - a highly potent endogenous vasoconstrictor - in 1988 has led to considerable efforts to develop antagonists of endothelin receptors that could have therapeutic potential in disorders including hypertension, heart failure and renal diseases. However, in general, the results of trials in humans have not mirrored the highly promising effects in animal disease models. Here, we discuss preclinical and clinical results with endothelin antagonists, and consider possible approaches to fully realizing the potential of endothelin antagonism.

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收藏

页码：986 / 1001

页数：16

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