A Chromogenic and Fluorogenic Peptide Substrate for the Highly Sensitive Detection of Proteases in Biological Matrices

The synthesis and application of a novel type of chromogenic and fluorogenic substrate for protease detection is described. The outstanding performance of the tripeptide substrates is exemplified by specific fluorescence detection of thrombin and factor Xa at only 500 fM concentration. The substrate...

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Veröffentlicht in:Journal of medicinal chemistry 2016-08, Vol.59 (16), p.7576-7583
Hauptverfasser: Arian, Dumitru, Harenberg, Job, Krämer, Roland
Format: Artikel
Sprache:eng
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Zusammenfassung:The synthesis and application of a novel type of chromogenic and fluorogenic substrate for protease detection is described. The outstanding performance of the tripeptide substrates is exemplified by specific fluorescence detection of thrombin and factor Xa at only 500 fM concentration. The substrate is also applicable to the sensitive detection of the thrombin inhibitor dabigatran in human plasma and whole blood samples, highlighting its potential for a point-of-care test for instant monitoring the blood levels of this blockbuster anticoagulant drug in specific clinical situations.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.6b00652