含小环的半胱氨酸蛋白酶抑制剂。

Cysteine protease inhibitors containing small rings.

作者信息

Schirmeister T, Klockow A

机构信息

Department of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, D-97074 Wuerzburg, Germany.

出版信息

Mini Rev Med Chem. 2003 Sep;3(6):585-96. doi: 10.2174/1389557033487935.

DOI:10.2174/1389557033487935

PMID:12871161

Abstract

Since the discovery of E-64 in 1978 as potent cysteine protease inhibitor a variety of inhibitors containing small rings as electrophilic building blocks responsible for enzyme inhibition have been developed. In this review we summarize new aspects concerning epoxysuccinyl peptides derived from E-64 and discuss inhibition potency, selectivity and mechanisms of peptidic and peptidomimetic inhibitors containing epoxide, aziridine, thiirane, cyclopropane, beta-lactam and beta-lactone rings as electrophilic fragments.

摘要

自1978年发现E-64作为强效半胱氨酸蛋白酶抑制剂以来，已经开发出了多种含有小环作为负责酶抑制的亲电结构单元的抑制剂。在这篇综述中，我们总结了源自E-64的环氧琥珀酰肽的新方面，并讨论了含有环氧、氮丙啶、硫杂环丙烷、环丙烷、β-内酰胺和β-内酯环作为亲电片段的肽类和拟肽类抑制剂的抑制效力、选择性和作用机制。