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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Hauptverfasser: Arian, Dumitru (VerfasserIn) , Harenberg, Job (VerfasserIn) , Krämer, Roland (VerfasserIn)
Dokumenttyp: Article (Journal)
Sprache:Englisch
Veröffentlicht: July 27, 2016
In: Journal of medicinal chemistry
Year: 2016, Jahrgang: 59, Heft: 16, Pages: 7576-7583
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.6b00652
Online-Zugang:Verlag, Volltext: https://doi.org/10.1021/acs.jmedchem.6b00652
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Verfasserangaben:Dumitru Arian, Job Harenberg, and Roland Krämer
Beschreibung
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.
Beschreibung:Gesehen am 23.08.2019
Beschreibung:Online Resource
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.6b00652