title: A Chromogenic and Fluorogenic Peptide Substrate for the Highly Sensitive Detection of Proteases in Biological Matrices.
abstract: 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.
authors.affiliation: Anorganisch-Chemisches Institut, Universität Heidelberg , Im Neuenheimer Feld 270, 69120 Heidelberg, Germany.
authors.forename: Dumitru
authors.initials: D
authors.lastname: Arian
authors.affiliation: Medical Faculty Mannheim, Universität Heidelberg , Maybachstrasse 14, 68169 Mannheim, Germany.
authors.forename: Job
authors.initials: J
authors.lastname: Harenberg
authors.affiliation: Anorganisch-Chemisches Institut, Universität Heidelberg , Im Neuenheimer Feld 270, 69120 Heidelberg, Germany.
authors.forename: Roland
authors.initials: R
authors.lastname: Krämer
mesh_terms: D000069604:Dabigatran / Q000097:blood / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D015951:Factor Xa / Q000032:analysis* / Q000378:metabolism; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000032:analysis* / Q000037:antagonists & inhibitors / Q000378:metabolism
chemical_list: D010455:Peptides; D013917:Thrombin; D015951:Factor Xa; D000069604:Dabigatran