title: Mixed alkyl aryl phosphonate esters as quenched fluorescent activity-based probes for serine proteases.
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.
authors.affiliation: Lehrstuhl für Chemie der Biopolymere, Technische Universität München, Weihenstephaner Berg 3, 85354 Freising, Germany. steven.verhelst@isas.de.
authors.forename: Sevnur
authors.initials: S
authors.lastname: Serim
authors.forename: Philipp
authors.initials: P
authors.lastname: Baer
authors.forename: Steven H L
authors.initials: SH
authors.lastname: Verhelst
mesh_terms: D004789:Enzyme Activation; D057075:Enzyme Assays / Q000379:methods; D004952:Esters / Q000737:chemistry*; D005456:Fluorescent Dyes / Q000032:analysis / Q000737:chemistry*; D008856:Microscopy, Fluorescence; D015394:Molecular Structure; D063065:Organophosphonates / Q000737:chemistry*; D057057:Serine Proteases / Q000032:analysis / Q000378:metabolism*
chemical_list: D004952:Esters; D005456:Fluorescent Dyes; D063065:Organophosphonates; D057057:Serine Proteases