Synthesis and activity of amides of tripeptides as potential urokinase inhibitors

J Enzyme Inhib Med Chem. 2010 Feb;25(1):139-42. doi: 10.3109/14756360903049042.

Abstract

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.

MeSH terms

  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / pharmacology*
  • Urokinase-Type Plasminogen Activator / antagonists & inhibitors*

Substances

  • Enzyme Inhibitors
  • Oligopeptides
  • Urokinase-Type Plasminogen Activator