【摘 要】
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In finding a new treatment for a number of neurological disorders and diseases, such as epilepsy, stroke and amyotrophic lateral sclerosis (ALS), one of the potential therapeutic strategies is to deve
【机 构】
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Department of Chemistry, and the Center for Neuroscience Research, State University of New York (SUN
【出 处】
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中国神经科学学会第九届全国学术会议暨第五届会员代表大会
论文部分内容阅读
In finding a new treatment for a number of neurological disorders and diseases, such as epilepsy, stroke and amyotrophic lateral sclerosis (ALS), one of the potential therapeutic strategies is to develop inhibitors for the α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors, a receptor subtype in the glutamate ion channel receptor family.This is because excessive activity of AMPA receptors leads to abnormal calcium influx into neurons, which in turn leads to cell death.In developing AMPA receptor inhibitors that are both potent and water soluble, we have used systematic evolution of ligands by exponential enrichment (SELEX) and have successfully identified three classes of aptamers with nanomolar affinity against AMPA receptors.In the class of competitive aptamers, we found one aptamer with an IC50 value of 30 nM, rivaling any other exiting AMPA receptor inhibitors.Furthermore, this aptamer is broadly active in all AMPA receptor subunits, but has no unwanted activity in either kainate or NMDA receptors, the two other glutamate receptor subtypes.
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