A Coumarin- Labeled Vinyl Sulfone as Tripeptidomimetic Activity- Based Probe for Cysteine Cathepsins

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F14%3A00429455" target="_blank" >RIV/61388963:_____/14:00429455 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1002/cbic.201300806" target="_blank" >http://dx.doi.org/10.1002/cbic.201300806</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/cbic.201300806" target="_blank" >10.1002/cbic.201300806</a>

Result language
angličtina
Original language name
A Coumarin- Labeled Vinyl Sulfone as Tripeptidomimetic Activity- Based Probe for Cysteine Cathepsins
Original language description
A coumarin-tetrahydroquinoline hydride 8 was synthesized as a chemical tool for fluorescent labeling. The rigidified tricyclic coumarin structure was chosen for its suitable fluorescence properties. The connection of 8 with a vinyl sulfone building blockwas accomplished by convergent synthesis thereby leading to the coumarin-based, tripeptidomimetic activity-based probe 10, containing a Gly-Phe-Gly motif. Probe 10 was evaluated as inactivator of the therapeutically relevant human cysteine cathepsins S,L, K, and B: it showed particularly strong inactivation of cathepsin S. The detection of recombinant and native cathepsin S was demonstrated by applying 10 to in-gel fluorescence imaging.
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CE - Biochemistry
OECD FORD branch
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Project
<a href="/en/project/GAP302%2F11%2F1481" target="_blank" >GAP302/11/1481: Serine proteases of human parasite Schistosoma mansoni and their function in host-parasite interactions</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2014
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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