title: Inhibition of human and yeast 20S proteasome by analogues of trypsin inhibitor SFTI-1.
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.
authors.affiliation: Department of Bioorganic Chemistry, Faculty of Chemistry, University of Gdansk, Gdansk, Poland.
authors.forename: Dawid
authors.initials: D
authors.lastname: Dębowski
authors.affiliation: Department of Clinical Immunology and Transplantology, Medical University of Gdansk, Gdansk, Poland.
authors.forename: Michał
authors.initials: M
authors.lastname: Pikuła
authors.affiliation: Department of Bioorganic Chemistry, Faculty of Chemistry, University of Gdansk, Gdansk, Poland.
authors.forename: Marta
authors.initials: M
authors.lastname: Lubos
authors.affiliation: Department of Clinical Immunology and Transplantology, Medical University of Gdansk, Gdansk, Poland.
authors.forename: Paulina
authors.initials: P
authors.lastname: Langa
authors.affiliation: Department of Clinical Immunology and Transplantology, Medical University of Gdansk, Gdansk, Poland.
authors.forename: Piotr
authors.initials: P
authors.lastname: Trzonkowski
authors.affiliation: Department of Bioorganic Chemistry, Faculty of Chemistry, University of Gdansk, Gdansk, Poland.
authors.forename: Adam
authors.initials: A
authors.lastname: Lesner
authors.affiliation: Department of Bioorganic Chemistry, Faculty of Chemistry, University of Gdansk, Gdansk, Poland.
authors.forename: Anna
authors.initials: A
authors.lastname: Łęgowska
authors.affiliation: Department of Bioorganic Chemistry, Faculty of Chemistry, University of Gdansk, Gdansk, Poland.
authors.forename: Krzysztof
authors.initials: K
authors.lastname: Rolka
mesh_terms: D020169:Caspases / Q000378:metabolism; D002918:Chymotrypsin / Q000378:metabolism; D006801:Humans; D010455:Peptides / Q000378:metabolism; D010456:Peptides, Cyclic / Q000378:metabolism*; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism*; D014357:Trypsin / Q000378:metabolism; D014361:Trypsin Inhibitors / Q000378:metabolism*; D015003:Yeasts / Q000378:metabolism*
chemical_list: D010455:Peptides; D010456:Peptides, Cyclic; C448501:SFTI-1 peptide, sunflower; D014361:Trypsin Inhibitors; D002918:Chymotrypsin; D014357:Trypsin; D020169:Caspases; D046988:Proteasome Endopeptidase Complex