Department of Pharmacy, University of Salerno, Via G. Paolo II, 84084 Fisciano, Italy.
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences (CHIBIOFARAM), University of Messina, Viale F. Stagno d'Alcontres 31, 98166 Messina, Italy.
Molecules. 2024 Jun 20;29(12):2940. doi: 10.3390/molecules29122940.
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.
钾通道最近已成为治疗癫痫疾病的合适靶点。在钾通道中，KCNT1 通道是最广泛被认为与多种癫痫和发育性脑病有关的通道。然而，迄今为止，KCNT1 通道阻滞剂的药物化学发展仍不成熟。在本综述中，我们描述和分析了涉及 KCNT1 阻滞剂开发和鉴定问题的论文，并证明了其中描述的科学方法的优缺点。在简短介绍癫痫疾病和钾通道的结构-功能之后，我们提供了迄今为止作为 KCNT1 阻滞剂的化学型以及用于鉴定它们的科学方法的广泛概述。
