Click here to close Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly. We suggest using a current version of Chrome, FireFox, or Safari.
XB-ART-15223
Nat Biotechnol 1998 Mar 01;163:286-91. doi: 10.1038/nbt0398-286.
Show Gene links Show Anatomy links

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

Ferrer-Montiel AV , Merino JM , Blondelle SE , Perez-Payà E , Houghten RA , Montal M .


???displayArticle.abstract???
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.

???displayArticle.pubmedLink??? 9528011
???displayArticle.link??? Nat Biotechnol
???displayArticle.grants??? [+]

Species referenced: Xenopus
Genes referenced: grin1 grin2a