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Amiloride selectively inhibits the urokinase‐type plasminogen activator
Author(s) -
Vassalli Jean-Dominique,
Belin Dominique
Publication year - 1987
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(87)80039-x
Subject(s) - amiloride , plasminogen activator , urokinase , chemistry , activator (genetics) , pharmacology , biochemistry , endocrinology , medicine , receptor , sodium , organic chemistry
The diuretic drug amiloride, an inhibitor of Na + uptake, competitively inhibits the catalytic activity of the urokinase‐type plasminogen activator (u‐PA), with a K i of 7 × 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.