Targeted pH-dependent fluorescent activity-based cathepsin probes

Chem Commun (Camb). 2011 Sep 7;47(33):9363-5. doi: 10.1039/c1cc12947c. Epub 2011 Jul 18.

Abstract

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.

MeSH terms

  • Animals
  • Boron Compounds / chemistry*
  • Cathepsins / metabolism*
  • Dendritic Cells / metabolism
  • Fluorescent Dyes / chemistry*
  • Hydrogen-Ion Concentration
  • Leucine / analogs & derivatives
  • Leucine / chemistry
  • Mannose / chemistry
  • Mice
  • Microscopy, Fluorescence

Substances

  • 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene
  • Boron Compounds
  • DCG 04
  • Fluorescent Dyes
  • Cathepsins
  • Leucine
  • Mannose