Mixed alkyl aryl phosphonate esters as quenched fluorescent activity-based probes for serine proteases
Author(s) -
Sevnur Serim,
Philipp Baer,
Steven H. L. Verhelst
Publication year - 2014
Publication title -
organic and biomolecular chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.923
H-Index - 146
eISSN - 1477-0539
pISSN - 1477-0520
DOI - 10.1039/c4ob02444c
Subject(s) - chemistry , phosphonate , aryl , alkyl , proteases , serine , fluorescence , organic chemistry , stereochemistry , enzyme , physics , quantum mechanics
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.
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