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Updated: Apr 25, 2026

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Published on: September 3, 2013
Peptidyl succinimidyl peptides as taspase 1 inhibitors
Johannes van den Boom1, Marija Mamić, Daniele Baccelliere
1Strukturelle Biochemie, Universität Duisburg-Essen, Zentrum für Medizinische Biotechnologie, Universitätsstrasse 2, 45117 Essen (Germany).
Abstract:
Taspase 1 is an N-terminal threonine protease implicated in leukemia and other cancers. Despite intensive efforts in recent years, only a limited number of Taspase 1 inhibitors are currently available, and they lack general applicability. Here we present a novel class of Taspase 1 inhibitors based on a peptidyl succinimidyl peptide motif. These inhibitors were obtained from the substrate cleavage sequence and mechanistic considerations involving the previously proposed asparaginase-type cleavage mechanism. We anticipate that this class of Taspase 1 inhibitor will find wide application in further biochemical and structural studies, for example for better investigating the molecular details of the unusual enzymatic cleavage mechanism of Taspase 1.
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