Why the study?
Precise molecular structures of human Kv7 channel subtypes have only recently emerged, highlighting the need to summarize the synthetic and medicinal chemistry of small molecule modulators.
Provides a comprehensive overview of the medicinal chemistry and therapeutic potential of Kv7 potassium channel modulators.
Should not yet change practice; extends chemical leads for Kv7 modulator development in new indications.
The rising interest in Kv7 modulators originates from their ability to evoke fundamental electrophysiological perturbations in a tissue-specific manner. A large number of therapeutic applications are, in part, based on the clinical experience with two broad-spectrum Kv7 agonists, flupirtine and retigabine. Since precise molecular structures of human Kv7 channel subtypes in closed and open states have only very recently started to emerge, computational studies have traditionally been used to analyze binding modes and direct the development of more potent and selective Kv7 modulators with improved safety profiles. Herein, the synthetic and medicinal chemistry of small molecule modulators and the representative biological properties are summarized. Furthermore, new therapeutic applications supported by in vitro and in vivo assay data are suggested.
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Borgini et al. (2021) studied this question.
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