Peptidyl succinimidyl peptides as taspase 1 inhibitors.

Johannes van den Boom, Marija Mamić, Daniele Baccelliere, Susanne Zweerink, Farnusch Kaschani, Shirley Knauer, Peter Bayer, Markus Kaiser

Chembiochem : a European journal of chemical biology 2014 Oct 13

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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. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Citation

Johannes van den Boom, Marija Mamić, Daniele Baccelliere, Susanne Zweerink, Farnusch Kaschani, Shirley Knauer, Peter Bayer, Markus Kaiser. Peptidyl succinimidyl peptides as taspase 1 inhibitors. Chembiochem : a European journal of chemical biology. 2014 Oct 13;15(15):2233-7