Synthesis and activity of amides of tripeptides as potential urokinase inhibitors.
Eleven peptides of the general formula H-d-Ser-Ala-Arg-NH-X, where X = (CH2)n-NH2, n = 2-9, (CH2)m-OH, m = 2-4, were obtained and tested for their effect on the amidolytic activities of urokinase, thrombin, trypsin, plasmin, t-PA, and kallikrein. H-D-Ser-Ala-Arg-NH-(CH2)5-NH2 inhibited urokinase with a Ki value of 6.3 microM.
Markowska
Agnieszka
A
Department of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland. agnieszka.markowska@umwb.edu.pl
Bruzgo
Irena
I
Midura-Nowaczek
Krystyna
K
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D014568:Urokinase-Type Plasminogen Activator / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D009842:Oligopeptides; D014568:Urokinase-Type Plasminogen Activator