Cover Picture: Fluorogenic Peptide-Based Substrates for Monitoring Thrombin Activity (ChemMedChem 4/2012)

Authors

  • Dr. Sander S. van Berkel,

    1. Radboud University Nijmegen, Institute for Molecules and Materials, Heyendaalseweg 135, 6525 AJ Nijmegen (The Netherlands)
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  • Bas van der Lee,

    1. Radboud University Nijmegen, Institute for Molecules and Materials, Heyendaalseweg 135, 6525 AJ Nijmegen (The Netherlands)
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  • Dr. Floris L. van Delft,

    1. Radboud University Nijmegen, Institute for Molecules and Materials, Heyendaalseweg 135, 6525 AJ Nijmegen (The Netherlands)
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  • Dr. Rob Wagenvoord,

    1. Synapse BV, University of Maastricht, Cardiovascular Research Institute Maastricht, P.O. Box 616, 6200 MD Maastricht (The Netherlands)
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  • Prof. Dr. H. Coenraad Hemker,

    1. Synapse BV, University of Maastricht, Cardiovascular Research Institute Maastricht, P.O. Box 616, 6200 MD Maastricht (The Netherlands)
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  • Prof. Dr. Floris P. J. T. Rutjes

    Corresponding author
    1. Radboud University Nijmegen, Institute for Molecules and Materials, Heyendaalseweg 135, 6525 AJ Nijmegen (The Netherlands)
    • Radboud University Nijmegen, Institute for Molecules and Materials, Heyendaalseweg 135, 6525 AJ Nijmegen (The Netherlands)
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Abstract

original image

The cover picture shows thrombin-specific substrates bound in the active site of thrombin. In the background, the intact fluorogenic conjugate (shown in yellow) of thrombin-specific tripeptide H-Gly-Gly-Arg and 7-amino-4-methylcoumarin (AMC) bound to thrombin is displayed. Prior to thrombin-mediate hydrolysis, this substrate displays only weak fluorescence. Upon cleavage of the Arg[BOND]AMC bond, strongly fluorescent AMC (shown in bright blue) is liberated. Quantification of the increase in fluorescence over time provides a direct measure for the amount of thrombin present in plasma. Moreover, from these data, the specific thrombin activity can be calculated, which is a direct measure of the coagulability of a clotting sample. These substrates have potential application in microfluidic devices for point-of-care tests, allowing the rapid diagnosis of blood or plasma samples. For more details, see the Full Paper by Floris P. J. T. Rutjes et al. on p. 606 ff.

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