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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Cysteine Protease Inhibitors Containing Small Rings

Author(s): T. Schirmeister and A. Klockow

Volume 3, Issue 6, 2003

Page: [585 - 596] Pages: 12

DOI: 10.2174/1389557033487935

Price: $65

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, ß-lactam and ß-lactone rings as electrophilic fragments.

Keywords: cysteine protease inhibitors, epoxysuccinyl peptides, peptidomimetic inhibitors, epoxide, aziridine, thiirane, cyclopropane


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