Scientific article

Amiloride selectively inhibits the urokinase-type plasminogen activator

Published inFEBS letters, vol. 214, no. 1, p. 187-191
Publication date1987

The diuretic drug amiloride, an inhibitor of Na+ uptake, competitively inhibits the catalytic activity of the urokinase-type plasminogen activator (u-PA), with a Ki of 7 X 10(-6) M. Generation of plasmin, cleavage of peptide substrates, and interaction of u-PA with a specific macromolecular proteinase inhibitor are all prevented in the presence of the drug. In contrast, amiloride does not affect the activity of either tissue-type plasminogen activator, plasmin, plasma kallikrein or thrombin. The inhibition of u-PA by amiloride may be related to the previously reported inhibition of u-PA-type enzymes by Na+. Amiloride or related compounds could prove useful in selectively controlling u-PA-catalyzed extracellular proteolysis.

  • Amiloride/ pharmacology
  • Animals
  • Humans
  • Kinetics
  • Plasminogen Activators/ antagonists & inhibitors
  • Plasminogen Inactivators
  • Protease Inhibitors/metabolism
  • Sodium/metabolism
  • Tissue Plasminogen Activator/antagonists & inhibitors
  • Urokinase-Type Plasminogen Activator/ antagonists & inhibitors
Citation (ISO format)
VASSALLI, Jean-Dominique, BELIN, Dominique. Amiloride selectively inhibits the urokinase-type plasminogen activator. In: FEBS letters, 1987, vol. 214, n° 1, p. 187–191. doi: 10.1016/0014-5793(87)80039-x
Main files (1)
ISSN of the journal0014-5793

Technical informations

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