Small Molecule Analogs of a Neuroprotective Peptide
One out of every 20 deaths in the United States is caused by stroke. If administered quickly, surgery or clot-dissolving agents can improve the odds of survival. Recently, researchers at the University of Pittsburgh developed a peptide that acts a potent neuroprotectant, preserving living brain cells until other treatment can be accessed.
Description
After identifying an anchoring chemotype by studying the interaction site utilized by the neuroprotective peptide, 26 million commercially available compounds were virtually selected for testing. Of these, five were non-toxic to cortical neurons in culture, and one conferred neuroprotective benefits against glutamate uptake inhibition apoptotic excitotoxic injury. This compound was also shown to prevent an increase in K+ currents in neurons undergoing apoptosis without influencing baseline K+ currents or NMDA-induced Ca2+ responses. Crucially, this small molecule displaced syntaxin from binding to the original neuroprotective peptides, validating its potential to serve as an analog to the original peptide.Applications
· Neuroprotectant during stroke, prolonging the window of opportunity for effective treatment· Prototype for future neuroprotective studies