PDF(Pubmed)
Abstract：
Potassium channels have recently emerged as suitable target for the treatment of epileptic diseases. Among potassium channels, KCNT1 channels are the most widely characterized as responsible for several epileptic and developmental encephalopathies. Nevertheless, the medicinal chemistry of KCNT1 blockers is underdeveloped so far. In the present review, we describe and analyse the papers addressing the issue of KCNT1 blockers\' development and identification, also evidencing the pros and the cons of the scientific approaches therein described. After a short introduction describing the epileptic diseases and the structure-function of potassium channels, we provide an extensive overview of the chemotypes described so far as KCNT1 blockers, and the scientific approaches used for their identification.
摘要：
钾通道最近已成为治疗癫痫疾病的合适靶标。在钾通道中，KCNT1通道被最广泛地表征为负责几种癫痫和发育性脑病。然而，到目前为止，KCNT1阻断剂的药物化学尚不发达。在本次审查中，我们描述和分析了解决KCNT1阻断剂开发和鉴定问题的论文，还证明了其中描述的科学方法的利弊。在简短介绍了癫痫性疾病和钾离子通道的结构功能之后，我们提供了到目前为止所描述的KCNT1阻断剂的化学型的广泛概述，以及用于识别它们的科学方法。
