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Amiloride selectively inhibits the urokinase‐type plasminogen activator
Open accessAbstract
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.
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Citations
Cited by
Cell-Associated Plasminogen Activation: Regulation and Physiological Functions
Saksela, O., & Rifkin, D. B. (1988) · Annual Review of Cell Biology · doi:10.1146/annurev.cb.04.110188.000521 · Cited by 818
Montesano, R., Pepper, M. S., Möhle-Steinlein, U., Risau, W., Wagner, E. F., & Orci, L. (1990) · Cell · doi:10.1016/0092-8674(90)90009-4 · Cited by 454
The plasminogen activator system: biology and regulation
Irigoyen, J. P., Muñoz-Cánoves, P., Montero, L., Koziczak, M., & Nagamine, Y. (1999) · Cellular and Molecular Life Sciences · doi:10.1007/pl00000615 · Cited by 368
Extracellular proteolysis in the adult murine brain.
Sappino, A. P., Madani, R., Huarte, J., Belin, D., Kiss, J. Z., Wohlwend, A., & Vassalli, J. D. (1993) · Journal of Clinical Investigation · doi:10.1172/jci116637 · Cited by 356
Self-citationThe urokinase plasminogen activator system: a target for anti-cancer therapy
Ulisse, S., Baldini, E., Sorrenti, S., & D'Armiento, M. (2009) · Current Cancer Drug Targets · doi:10.2174/156800909787314002 · Cited by 312
Metadata
- Authors
- Vassalli, J.-D., & Belin, D.
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 1987-04-06
- Volume
- 214
- Issue
- 1
- Pages
- 187-191
- ISSN
- 0014-5793 (ISSN-L)
- 1873-3468
- OpenAlex
- W2061417741
- Cited by
- 380
- References
- 0
- FWCI
- 5.06
- Type
- journal article
- Language
- en
- Open access
- green
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- Vassalli, J.-D., & Belin, D. (1987). Amiloride selectively inhibits the urokinase‐type plasminogen activator. FEBS Letters. https://doi.org/10.1016/0014-5793(87)80039-x
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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