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Amiloride selectively inhibits the urokinase-type plasminogen activator

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Published in FEBS Letters. 1987, vol. 214, no. 1, p. 187-191
Abstract 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.
Keywords Amiloride/ pharmacologyAnimalsHumansKineticsPlasminogen Activators/ antagonists & inhibitorsPlasminogen InactivatorsProtease Inhibitors/metabolismSodium/metabolismTissue Plasminogen Activator/antagonists & inhibitorsUrokinase-Type Plasminogen Activator/ antagonists & inhibitors
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PMID: 3106085
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VASSALLI, Jean-Dominique, BELIN, Dominique. Amiloride selectively inhibits the urokinase-type plasminogen activator. In: FEBS Letters, 1987, vol. 214, n° 1, p. 187-191. https://archive-ouverte.unige.ch/unige:9067

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Deposited on : 2010-07-12

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