对人肾素具有强效和特异性抑制作用的修饰肽。

Modified peptides which display potent and specific inhibition of human renin.

作者信息

Luly J R, Plattner J J, Stein H, Yi N, Soderquist J, Marcotte P A, Kleinert H D, Perun T J

出版信息

Biochem Biophys Res Commun. 1987 Feb 27;143(1):44-51. doi: 10.1016/0006-291x(87)90627-9.

Abstract

A new class of angiotensinogen analogues which contain heteroatom-methylene and retro-inverso amide bond replacements was synthesized and evaluated for renin inhibition. Selected compounds in the series were specific for renin over other aspartic proteinases, and the most potent inhibitor demonstrated hypotensive activity in a salt depleted monkey.

摘要

合成了一类新型的血管紧张素原类似物，其含有杂原子亚甲基和反向酰胺键替代物，并对其进行了肾素抑制活性评估。该系列中选定的化合物对肾素具有相对于其他天冬氨酸蛋白酶的特异性，并且最有效的抑制剂在缺盐的猴子中表现出降压活性。