Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor

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Anders Bach, Thomas B. Pedersen, Kristian Strømgaard

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.

Original languageEnglish
JournalMedChemComm
Volume7
Issue number3
Pages (from-to)531-536
Number of pages6
ISSN2040-2503
DOIs
Publication statusPublished - 2016

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