KCNT1 Channel Blockers: A Medicinal Chemistry Perspective

Author:

Di Matteo Francesca1ORCID,Mancuso Francesca2ORCID,Turcio Rita1,Ciaglia Tania1ORCID,Stagno Claudio2ORCID,Di Chio Carla2,Campiglia Pietro1ORCID,Bertamino Alessia1,Giofrè Salvatore Vincenzo2,Ostacolo Carmine1ORCID,Iraci Nunzio2ORCID

Affiliation:

1. Department of Pharmacy, University of Salerno, Via G. Paolo II, 84084 Fisciano, Italy

2. Department of Chemical, Biological, Pharmaceutical and Environmental Sciences (CHIBIOFARAM), University of Messina, Viale F. Stagno d’Alcontres 31, 98166 Messina, 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.

Funder

Italian Ministry for University and Research

University of Salerno

Regione Campania project

University of Messina

Publisher

MDPI AG

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