Peptide blocking the TRPM2- PKCγ interaction for stroke

A peptide that blocks the interaction between the neuronal cation channel TRPM2 and the neuron-specific kinase PKCγ could help treat stroke by preventing TRPM2-enhanced potentiation of extra-synaptic NMDA receptor activity, which is known to cause ischemic neuronal death and worsen excitotoxicity and ischemic injury, but has been difficult to target selectively.

Studies in a human embryonic kidney cell line showed PKCγ and TRPM2 promote each other's activity via direct physical interaction involving the N-terminus of TRPM2, and a membrane-permeable peptide mimicking that TRPM2 N-terminal region prevented the interaction between the two proteins. ...