Organic & Biomolecular Chemistry 2015-02-28

Mixed alkyl aryl phosphonate esters as quenched fluorescent activity-based probes for serine proteases.

Sevnur Serim, Philipp Baer, Steven H L Verhelst

Index: Org. Biomol. Chem. 13(8) , 2293-9, (2015)

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Abstract

Activity-based probes (ABPs) are powerful tools for the analysis of active enzyme species in whole proteomes, cells or animals. Quenched fluorescent ABPs (qABPs) can be applied for real time imaging, allowing the visualization of dynamic enzyme activation by fluorescent microscopy. Unfortunately, qABPs are only available for a few enzymes. We here describe the design and synthesis of qABPs for serine proteases based on a phosphonate ester scaffold.