In vivo imaging of mouse tumors by a lipidated cathepsin S substrate

Hai Yu Hu, Divya Vats, Matej Vizovisek, Lovro Kramer, Catherine Germanier, K. Ulrich Wendt, Markus Rudin, Boris Turk, Oliver Plettenburg, Carsten Schultz

Research output: Contribution to journalArticlepeer-review

54 Scopus citations


The synthesis and evaluation of two cathepsin S-specific probes is described. For long-term retention of the probe at the target site and a high signal-to-noise ratio, we introduced a lipidation approach via the simple attachment of palmitoic acid to the reporter. After cathepsin S-specific cleavage in cultured cells and in a grafted tumor mouse model, fluorescence increased owing to dequenching and we observed an intracellular accumulation of the fluorescence in the target tissue. The lipidated probe provided a prolonged and strongly fluorescent signal in tumors when compared to the very similar non-lipidated probe, demonstrating that non-invasive tumor identification is feasable. The homing principle by probe lipidation might also work for selective administration of cytotoxic compounds to specifically reduce tumor mass.

Original languageEnglish (US)
Pages (from-to)7669-7673
Number of pages5
JournalAngewandte Chemie - International Edition
Issue number29
StatePublished - Jul 14 2014
Externally publishedYes


  • FRET
  • fluorescence probes
  • homing
  • lipidation
  • tumor diagnosis

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)


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