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Hu, H.Y.* ; Vats, D.* ; Vizovisek, M.* ; Krämer, L.* ; Germanier, C.* ; Wendt, K.U.* ; Rudin, M.* ; Turk, B.* ; Plettenburg, O.* ; Schultz, C.*

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

Angew. Chem.-Int. Edit. 53, 7669-7673 (2014)
DOI PMC
Open Access Green as soon as Postprint is submitted to ZB.
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 Article Number: , Supplement: ,
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