Recombinant Conus striatus Con-ikot-ikot
Potently and selectively blocks the desensitization of ionotropic glutamate AMPA receptor (GRIA1, GRIA2, GRIA3 and GRIA4). Can also open already desensitized GRIA1 receptors. Binds to a different site than does the drug cyclothiazide . The toxin acts like a straightjacket on the ligand-binding domain (LBD) "gating ring" of the receptor, restraining the domains via both intra- and interdimer cross-links such that agonist-induced closure of the LBD "clamshells" is transduced into an irislike expansion of the gating ring . Application of the toxin to hippocampal slices causes a large and rapid increase in resting AMPAR-mediated current leading to neuronal death .
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Reference:
CSB-EP316701DWI_1
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