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

作者：Bach Anders^*; Pedersen Thomas B; Stromgaard Kristian

来源：Medchemcomm, 2016, 7(3): 531-536.

DOI：10.1039/c5md00445d

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.

• 出版日期2016