Journal
CHEMPLUSCHEM
Volume 80, Issue 6, Pages 928-937Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cplu.201500004
Keywords
activity-based protein profiling; drug delivery; fluorescent probes; mannose receptors; oligomannose
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Funding
- Netherlands Organization for Scientific Research (NWO-CW)
- European Research Council
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Three fluorescent cathepsin inhibitor glycoconjugates have been designed, synthesized, and evaluated in terms of their cell internalization and cathepsin inhibitory properties. The conjugates are composed of a peptide epoxysuccinate, capable of covalent and irreversible binding to cysteine proteases, coupled to a fluorescent BODIPY dye and functionalized with a mono-, tri-, or heptamannoside. Mannose-receptor-dependent uptake of the probes in live dendritic cells is shown to depend on the type of carbohydrate attached. Where uptake of the monomannoside is poor and mannose-receptor-independent, the intracellular labeling of cathepsins by the probes equipped with a tri- or heptamannoside conjugate appeared concentration- and mannose-receptor-dependent.
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