Targeted pH-dependent fluorescent activity-based cathepsin probes

摘要

Bifunctional, pH-activatable BODIPY dyes were developed and incorporated in mannose cluster-containing activity-based probes for cysteine proteases. Mannose receptor-dependent uptake of the probes in dendritic cells, followed by trafficking to acidic cellular compartments resulted in fluorescence as seen by live-cell imaging, and subsequent cathepsin inhibition. Fluorescent dyes are applied in many different areas of chemical biology. Among these dyes, boron-dipyrromethene (BODIPY) derivatives are frequently used due to their excellent photochemical properties and relative stability under physiological conditions.