Cysteine protease inhibitors containing small rings.
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.
Schirmeister
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Department of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, D-97074 Wuerzburg, Germany. schirmei@pharmazie.uni-wuerzburg.de
Klockow
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D001388:Aziridines / Q000737:chemistry / Q000494:pharmacology; D003521:Cyclopropanes / Q000737:chemistry / Q000494:pharmacology; D003546:Cysteine Endopeptidases / Q000187:drug effects; D015853:Cysteine Proteinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D004852:Epoxy Compounds / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007769:Lactams / Q000737:chemistry / Q000494:pharmacology; D007783:Lactones / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000737:chemistry / Q000494:pharmacology
D001388:Aziridines; D003521:Cyclopropanes; D015853:Cysteine Proteinase Inhibitors; D004852:Epoxy Compounds; D007769:Lactams; D007783:Lactones; D013440:Sulfides; D003546:Cysteine Endopeptidases