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Updated: Oct 2, 2026

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog
Published on: November 5, 2014
4-amidinobenzylamine-based inhibitors of urokinase
Sebastian Künzel1, Andrea Schweinitz, Siegmund Reissmann
1Institut fur Biochemie und Biophysik, Universitat Jena, Philosophenweg 12, D-07743, Jena, Germany.
Abstract:
A series of 4-amidinobenzylamine-based peptidomimetic inhibitors of urokinase was synthesized. The most potent one, benzylsulfonyl-D-Ser-Ala-4-amidinobenzylamide 16, inhibits uPA with a K(i) of 7.7 nM but is less selective than 10 with a Gly as P2 residue. Hydroxyamidine and carbonate prodrugs were prepared, which are rapidly converted into the active inhibitors in rats after subcutaneous application.
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