Details
| Original language | English |
|---|---|
| Pages (from-to) | 7669-7673 |
| Number of pages | 5 |
| Journal | Angewandte Chemie - International Edition |
| Volume | 53 |
| Issue number | 29 |
| Early online date | 30 May 2014 |
| Publication status | Published - 14 Jul 2014 |
| Externally published | Yes |
Abstract
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.
Keywords
- fluorescence probes, FRET, homing, lipidation, tumor diagnosis
ASJC Scopus subject areas
- Chemical Engineering(all)
- Catalysis
- Chemistry(all)
- General Chemistry
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In: Angewandte Chemie - International Edition, Vol. 53, No. 29, 14.07.2014, p. 7669-7673.
Research output: Contribution to journal › Article › Research › peer review
}
TY - JOUR
T1 - In Vivo Imaging of Mouse Tumors by a Lipidated Cathepsin Substrate
AU - Hu, Hai Yu
AU - Vats, Divya
AU - Vizovisek, Matej
AU - Kramer, Lovro
AU - Germanier, Catherine
AU - Wendt, K. Ulrich
AU - Rudin, Markus
AU - Turk, Boris
AU - Plettenburg, Oliver
AU - Schultz, Carsten
PY - 2014/7/14
Y1 - 2014/7/14
N2 - 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.
AB - 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.
KW - fluorescence probes
KW - FRET
KW - homing
KW - lipidation
KW - tumor diagnosis
UR - http://www.scopus.com/inward/record.url?scp=84904438282&partnerID=8YFLogxK
U2 - 10.1002/anie.201310979
DO - 10.1002/anie.201310979
M3 - Article
C2 - 24888522
AN - SCOPUS:84904438282
VL - 53
SP - 7669
EP - 7673
JO - Angewandte Chemie - International Edition
JF - Angewandte Chemie - International Edition
SN - 1433-7851
IS - 29
ER -