Inhibition of human and yeast 20S proteasome by analogues of trypsin inhibitor SFTI-1.

Dębowski, Dawid; Pikuła, Michał; Lubos, Marta; Langa, Paulina; Trzonkowski, Piotr; Lesner, Adam; Łęgowska, Anna; Rolka, Krzysztof · PLoS One · 2014

basic_science · Level V

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Abstract

Starting from the primary structure of sunflower trypsin inhibitor SFTI-1, we designed novel non-covalent inhibitors of human and yeast 20S proteasomes. Peptides with Arg residue in P1 position and two basic amino acid residues (Lys or/and Arg) in P2' and P3' positions strongly inhibited chymotrypsin-like and caspase-like activities, while trypsin-like activity was poorly modified. We found that some SFTI-1 analogues up-regulated exclusively the chymotrypsin-like activity of latent yeast 20S proteasome.

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