Article
Discovery of Potent and Selective Blockers Targeting the Epilepsy-Associated KNa1.1 Channel.
Journal of medicinal chemistry - 14 Nov 2024
Zheng Ruqiu, Li Zhongtang, Wang Qiufeng, Liu Shiqi, Liu Ningfeng, Li Yiyan, Zhu Guiwang, Liu Zhenming, Huang Zhuo, Zhang Liangren
Abstract excerpt
Gain-of-function (GOF) mutations of the sodium-activated potassium channel KNa1.1 (Slack, Slo2.2, or KCa4.1) induce severe, drug-resistant forms of epilepsy in infants and children. Although quinidine has shown promise in treating KCNT1-related epilepsies compared to other drugs, its limited efficacy and substantial side effects necessitate the development of new KNa1.1 channel inhibitors. In this study, we...
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