Compound class:
Peptide or derivative
Comment: This is a synthetic macrocyclic peptide that was designed to disrupt the protein-protein interaction between postsynaptic density protein-95 (PSD-95; gene symbol DLG4) and neuronal nitric oxide synthase (nNOS) [1], as a mechanism to disrupt the excitotoxic signaling and cell death that's induced (in acute ischaemia) by formation of the tri-protein complex of glutamate ionotropic receptor NMDA type subunit 2B (GRIN2B; GluN2B or NR2B), PSD-95 and nNOS. Structurally it mimics the β-hairpin motif of nNOS that forms the interaction with the PDZ2 domain of PSD-95.
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Bioactivity Comments |
Peptide 14 binds to PSD-95-PDZ2 with a Kd of 18.1 nM by isothermal titration calorimetry (ITC) [1]. |