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In vivo imaging of mouse tumors by a lipidated cathepsin S substrate.
Angew. Chem.-Int. Edit. 53, 7669-7673 (2014)
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.
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Publication type
Article: Journal article
Document type
Scientific Article
Keywords
Fret ; Fluorescence Probes ; Homing ; Lipidation ; Tumor Diagnosis
Language
english
Publication Year
2014
HGF-reported in Year
0
ISSN (print) / ISBN
1433-7851
e-ISSN
1521-3773
Quellenangaben
Volume: 53,
Issue: 29,
Pages: 7669-7673
Publisher
Wiley
Publishing Place
Weinheim
Reviewing status
Peer reviewed
Institute(s)
Institute of Medicinal Chemistry (IMC)
POF-Topic(s)
30203 - Molecular Targets and Therapies
Research field(s)
Enabling and Novel Technologies
PSP Element(s)
G-506300-001
PubMed ID
24888522
Erfassungsdatum
2014-09-09