caa a22 4500 445326328 CHVBK 20180317142722.0 cr unu---uuuuu 170323e20110301xx s 000 0 eng 10.1007/s10989-011-9239-y doi (NATIONALLICENCE)springer-10.1007/s10989-011-9239-y Tripeptides with C-Terminal Arginine as Potential Inhibitors of Urokinase [Elektronische Daten] [Agnieszka Markowska, Irena Bruzgo, Wojciech Miltyk, Krystyna Midura-Nowaczek] We synthesized and tested ten peptides with the molecular structure being H-d-Ser-AA-Arg-OH for their effect on the amidolytic activities against urokinase, thrombin, trypsin, plasmin, tissue plasminogen activator and kallikrein. The inserted amino acid in each peptide was either leucine, norleucine, izoleucine, valine, norvaline, α-metyloalanine, α-aminobutanoic acid, homoleucine, tert-leucine or neoglycine. H-d-Ser-NVal-Arg-OH (compound 4) was the most active inhibitor of urokinase plasminogen activator with a Ki value of 0.85μM. Compound 4 showed cytotoxic effect against MDA-MB-231 and DLD cell lines, respectively, with IC50 values of 25 and 19μM. Synthesised compounds did not have activity against MCF-7 cancer cells. These peptides were nontoxic against pig's erythrocytes in vitro. Springer Science+Business Media, LLC, 2011 Urokinase inhibitor nationallicence Anti-amidolytic activity nationallicence Low molecular weight peptides nationallicence Markowska Agnieszka Department of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland aut Bruzgo Irena Department of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland aut Miltyk Wojciech Laboratory of Drug Analysis, Medical University of Bialystok, Bialystok, Poland aut Midura-Nowaczek Krystyna Department of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland aut International Journal of Peptide Research and Therapeutics Springer Netherlands 17/1(2011-03-01), 47-52 1573-3149 17:1<47 2011 17 10989 https://doi.org/10.1007/s10989-011-9239-y text/html Onlinezugriff via DOI 1 brief-communication jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s10989-011-9239-y text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Markowska Agnieszka Department of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland aut NATIONALLICENCE 700 1- Bruzgo Irena Department of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland aut NATIONALLICENCE 700 1- Miltyk Wojciech Laboratory of Drug Analysis, Medical University of Bialystok, Bialystok, Poland aut NATIONALLICENCE 700 1- Midura-Nowaczek Krystyna Department of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland aut NATIONALLICENCE 773 0- International Journal of Peptide Research and Therapeutics Springer Netherlands 17/1(2011-03-01), 47-52 1573-3149 17:1<47 2011 17 10989 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer