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Amiloride selectively inhibits the urokinase‐type plasminogen activator

Year: 1987

Type: article

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.

Source: FEBS Letters

DOI: 10.1016/0014-5793(87)80039-x

Authors: Jean-Dominique Vassalli, Dominique Belin

Institution: University of Geneva

Language: English

Topic: Protease and Inhibitor Mechanisms

Subfield: Cancer Research

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funders: Sir Jules Thorn Charitable Trust, Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung