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Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)
S. Krajcovicova, R. Jorda, D. Hendrychova, V. Krystof, M. Soural
Language English Country Great Britain
Document type Journal Article, Research Support, Non-U.S. Gov't
Grant support
NV17-31834A
MZ0
CEP Register
PubMed
30601480
DOI
10.1039/c8cc08716d
Knihovny.cz E-resources
- MeSH
- Amides chemical synthesis MeSH
- Protein Kinase Inhibitors MeSH
- Ligands MeSH
- Urea chemical synthesis MeSH
- Proteolysis MeSH
- Resins, Synthetic MeSH
- Solid-Phase Synthesis Techniques methods MeSH
- Thalidomide * chemical synthesis MeSH
- Triazoles chemical synthesis MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
A preloaded resin consisting of a thalidomide moiety and an ethylene-oxy linker allows the simple and fast formation of PROTACs. The feasibility of the procedure was illustrated by conjugating different protein kinase inhibitors. The biological functionality of an ibrutinib-like conjugate was then confirmed by a cellular experiment.
References provided by Crossref.org
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