Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor
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- Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor
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PSD-95 PDZ domains are biologically important and promising drug targets. Here, we discover a triazole-based peptidomimetic, 10, by ‘click chemistry’. Compound 10 inhibits the PDZ2/GluN2B interaction with affinity similar to tripeptide SAV and better than current small-molecules. Thus, 10 represents a new class of PSD-95 PDZ inhibitors.
Originalsprog | Engelsk |
---|---|
Tidsskrift | MedChemComm |
Vol/bind | 7 |
Udgave nummer | 3 |
Sider (fra-til) | 531-536 |
Antal sider | 6 |
ISSN | 2040-2503 |
DOI | |
Status | Udgivet - 2016 |
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ID: 154053805