Amiloride selectively inhibits the urokinase‐type plasminogen activator

FEBS Letters

Vassalli, Jean-Dominique¹  Belin, Dominique² 

[1] Institut d'Histologie et d'Embryologie, Centre Médical Universitaire, 1 rue Michel Servet, 1211 Geneva 4, Switzerland;Département de Pathologie, Centre Médical Universitaire, 1 rue Michel Servet, 1211 Geneva 4, Switzerland

关键词: Plasminogen activator;    Urokinase;    Plasminogen;    Amiloride;    Protease inhibitor;    Na+;   

DOI  :  10.1016/0014-5793(87)80039-X

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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.

【 授权许可】

Unknown