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Cysteine protease inhibitors containing small rings
1Department of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, D-97074 Wuerzburg, Germany. schirmei@pharmazie.uni-wuerzburg.de
Mini Reviews in Medicinal Chemistry
|July 23, 2003
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.