A small molecule that binds to the AMPA receptor subunit GluA2 has been shown to reduce glutamate-mediated excitotoxicity and provide neuroprotection in mouse models of multiple sclerosis (MS). Zhai et al. used a machine learning approach to identify small molecules that targeted an allosteric binding site within GluA2 and could modulate the receptor without abolishing glutamate signalling. One such molecule, ZCAN262, was found to restore myelination and axon integrity and to improve neurological function in experimental autoimmune encephalitis and cuprizone mouse models of MS.

中文翻译：

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GluA2 调节剂针对 MS 中的兴奋性毒性

一种与 AMPA 受体亚基 GluA2 结合的小分子已被证明可以减少谷氨酸介导的兴奋性毒性，并在多发性硬化症 (MS) 小鼠模型中提供神经保护。翟等人。使用机器学习方法来识别针对 GluA2 内变构结合位点的小分子，并且可以在不消除谷氨酸信号传导的情况下调节受体。其中一种分子 ZCAN262，被发现可以恢复髓鞘形成和轴突完整性，并改善实验性自身免疫性脑炎和多发性硬化症小鼠模型的神经功能。