Approaches for the discovery of drugs that target K Na 1.1 channels in KCNT1-associated epilepsy

Miziak, Barbara; Czuczwar, Stanisław J.

doi:10.1080/17460441.2023.2150164

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2024

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“…Intracellular life activities are closely related to specific ion concentrations, which are regulated by channel proteins on the cell membrane. The imbalance of specific ions can lead to a series of channel diseases, such as cystic fibrosis (Cl − ) [ 1 , 2 ], iodine deficiency, paralysis (Na + ) [ 3 , 4 ], epilepsy (K + ) [ 5 , 6 ] and malignant hyperthermia (Ca 2+ ) [ 7 , 8 , 9 , 10 ]. Therefore, the study of ion transport by membrane channel proteins and their synthetic analogs is of great significance to human health.…”

Section: Introductionmentioning

confidence: 99%

An Exceptionally Active and Highly Selective Perchlorate Transporter Containing a Trimesic Amide Scaffold

Deng,

Li,

Yuan

et al. 2024

Molecules

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We report here a series of alkyl group-modified trimesic amide molecules (TAs) with excellent anion transport activities. Among them, TA6, with the highest ion transport activity and excellent selectivity, efficiently transports anions across the membrane in the order of ClO4− > I− > NO3− > Br− > Cl−, with an EC50 value as low as 17.6 nM (0.022 mol% relative to lipid molecules) for ClO4−, which outperforms other anions by 5- to 22-folds and manifests as the best perchlorate transporter ever reported.

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