Cell-permeable and plasma-stable peptidomimetic inhibitors of the postsynaptic density-95/N-methyl-D-aspartate receptor interaction

A Bach, JNN Eildal, N Stuhr-Hansen…

Index: Bach, Anders; Eildal, Jonas N. N.; Stuhr-Hansen, Nicolai; Deeskamp, Rasmus; Gottschalk, Marie; Pedersen, Soren W.; Kristensen, Anders S.; Stromgaard, Kristian Journal of Medicinal Chemistry, 2011 , vol. 54, # 5 p. 1333 - 1346

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Citation Number: 36

Abstract

The protein− protein interaction between the NMDA receptor and its intracellular scaffolding protein, PSD-95, is a potential target for treating ischemic brain diseases, neuropathic pain, and Alzheimer's disease. We have previously demonstrated that N-alkylated tetrapeptides are potent inhibitors of this interaction, and here, this template is exploited for the development of blood plasma-stable and cell-permeable inhibitors. Initially, we explored ...