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Updated: Jun 22, 2025

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
KCNT1 Channel Blockers: A Medicinal Chemistry Perspective
Francesca Di Matteo1, Francesca Mancuso2, Rita Turcio1
1Department of Pharmacy, University of Salerno, Via G. Paolo II, 84084 Fisciano, Italy.
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.
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