Polyamine-like actions of peptides derived from conantokin-G, an N-methyl-D-aspartate (NMDA) antagonist.

摘要: Conantokins-T and -G are highly conserved polypeptides derived from Conus venoms. The N-methyl-D-aspartate (NMDA) antagonist properties of these compounds have been attributed to a potent noncompetitive inhibition polyamine responses. Substitution the gamma-carboxyglutamate residues as well modification N C termini conantokin-G abolished responses at NMDA receptor complex. However, several modified closely mimicked neurochemical profile polyamines One derivatives, Tyr0-conantokin-G, was found be most compound exhibiting polyamine-like actions complex described date, approximately 7-fold more than spermine. Circular dichroism studies demonstrate significant alpha-helical content in (27% aqueous medium). this alpha-helicity is not sufficient for action parent peptide neither necessary nor behavior analogs. derivatives report should useful probes examining role both recognition site operation