Ratiometric activatable cell-penetrating peptides provide rapid in vivo readout of thrombin activation

Angew Chem Int Ed Engl. 2013 Jan 2;52(1):325-30. doi: 10.1002/anie.201205721. Epub 2012 Oct 18.


In real time: thrombin activation in vivo can be imaged in real time with ratiometric activatable cell penetrating peptides (RACPPs). RACPPs are designed to combine 1) dual-emission ratioing, 2) far red to infrared wavelengths for in vivo mammalian imaging, and 3) cleavage-dependent spatial localization. The most advanced RACPP uses norleucine (Nle)-TPRSFL as a linker that increases sensitivity to thrombin by about 90-fold.

Publication types

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

MeSH terms

  • Animals
  • Cell-Penetrating Peptides / metabolism*
  • Fluorescence
  • Fluorescence Resonance Energy Transfer / methods
  • Mice
  • Mice, Transgenic
  • Thrombin / metabolism*


  • Cell-Penetrating Peptides
  • Thrombin