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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Selected peptides targeted to the NMDA receptor channel protect neurons from excitotoxic death.

Excitotoxic neuronal death, associated with neurodegeneration and stroke, is triggered primarily by massive Ca2+ influx arising from overactivation of glutamate receptor channels of the N-methyl-D-aspartate (NMDA) subtype. To search for channel blockers, synthetic combinatorial libraries were assayed for block of agonist-evoked currents by the human NR1- NR2A NMDA receptor subunits expressed in amphibian oocytes. A set of arginine-rich hexapeptides selectively blocked the NMDA receptor channel with IC50 approximately 100 nM, a potency similar to clinically tolerated blockers such as memantine, and only marginally blocked on non-NMDA glutamate receptors. These peptides prevent neuronal cell death elicited by an excitotoxic insult on hippocampal cultures.[1]

References

  1. Selected peptides targeted to the NMDA receptor channel protect neurons from excitotoxic death. Ferrer-Montiel, A.V., Merino, J.M., Blondelle, S.E., Perez-Payà, E., Houghten, R.A., Montal, M. Nat. Biotechnol. (1998) [Pubmed]
 
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