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Fluorogenic Substrates for In Situ Monitoring of Caspase-3 Activity in Live Cells

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Original languageEnglish
Article number0153209
Number of pages11
JournalPLoS ONE
Volume11
Issue number5
DOIs
Publication statusPublished - 11 May 2016

Abstract

The in situ detection of caspase-3 activity has applications in the imaging and monitoring of multiple pathologies, notably cancer. A series of cell penetrating FRET-based fluorogenic substrates were designed and synthesised for the detection of caspase-3 in live cells. A variety of modifications of the classical caspase-3 and caspase-7 substrate sequence Asp-Glu-Val-Asp were carried out in order to increase caspase-3 affinity and eliminate caspase-7 cross-reactivity. To allow cellular uptake and good solubility, the substrates were conjugated to a cationic peptoid. The most selective fluorogenic substrate 27, FAM-Ahx-Asp-Leu-Pro-Asp-Lys(MR)-Ahx, conjugated to the cell penetrating peptoid at the C-terminus, was able to detect and quantify caspase-3 activity in apoptotic cells without cross-reactivity by caspase-7.

    Research areas

  • ACTIVITY-BASED PROBES, UNNATURAL AMINO-ACIDS, PENETRATING PEPTIDES, APOPTOTIC PATHWAYS, CANCER, SPECIFICITY, CLEAVAGE, INHIBITORS, DISCOVERY, PROTEASES

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