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Issue 20, 2017
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Highly selective and rapidly activatable fluorogenic Thrombin sensors and application in human lung tissue

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Abstract

A library of FRET-based peptides were prepared and studied as Thrombin substrates. This identified probes that showed selective activation by Thrombin, low fluorescent background signals, stability to Factor Xa, matrix metalloproteases, and primary human inflammatory cell lysates and supernatant. These were selected for further optimization, creating a second generation of fluorogenic probes with improved solubility and Plasmin resistance. The optimised probe allowed the detection of Thrombin activity in ex vivo fibrotic human tissue.

Graphical abstract: Highly selective and rapidly activatable fluorogenic Thrombin sensors and application in human lung tissue

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Publication details

The article was received on 17 Mar 2017, accepted on 26 Apr 2017 and first published on 28 Apr 2017


Article type: Paper
DOI: 10.1039/C7OB00663B
Citation: Org. Biomol. Chem., 2017,15, 4344-4350
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    Highly selective and rapidly activatable fluorogenic Thrombin sensors and application in human lung tissue

    A. Megia-Fernandez, B. Mills, C. Michels, S. V. Chankeshwara, K. Dhaliwal and M. Bradley, Org. Biomol. Chem., 2017, 15, 4344
    DOI: 10.1039/C7OB00663B

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