Enzyme-Activated Fluorogenic Probes for Live-Cell and in Vivo Imaging

ACS Chem Biol. 2018 Jul 20;13(7):1810-1823. doi: 10.1021/acschembio.8b00371. Epub 2018 Jul 6.


Fluorogenic probes, small-molecule sensors that unmask brilliant fluorescence upon exposure to specific stimuli, are powerful tools for chemical biology. Those probes that respond to enzymatic catalysis illuminate the complex dynamics of biological processes at a level of spatiotemporal detail and sensitivity unmatched by other techniques. Here, we review recent advances in enzyme-activated fluorogenic probes for biological imaging. We organize our survey by enzyme classification, with emphasis on fluorophore masking strategies, modes of enzymatic activation, and the breadth of current and future applications. Key challenges such as probe selectivity and spectroscopic requirements are described alongside therapeutic, diagnostic, and theranostic opportunities.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Enzymes / metabolism*
  • Fluorescence
  • Fluorescent Dyes / chemistry*
  • Fluorescent Dyes / metabolism*
  • Humans
  • Optical Imaging / methods*


  • Enzymes
  • Fluorescent Dyes