KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting

Specificity of inhibitors of voltage-gated ion channels is crucial for their use as therapeutics. Here, the authors show that adamantane derivatives interact with a specific binding site on fenestrations that only become available when accessory subunits are bound to the channel.

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Detalles Bibliográficos
Autores principales: Eva Wrobel, Ina Rothenberg, Christoph Krisp, Franziska Hundt, Benjamin Fraenzel, Karina Eckey, Joannes T. M. Linders, David J. Gallacher, Rob Towart, Lutz Pott, Michael Pusch, Tao Yang, Dan M. Roden, Harley T. Kurata, Eric Schulze-Bahr, Nathalie Strutz-Seebohm, Dirk Wolters, Guiscard Seebohm
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2016
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Acceso en línea:https://doaj.org/article/6f13dc5b883d4828afc6c8522bd13d5d
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Descripción
Sumario:Specificity of inhibitors of voltage-gated ion channels is crucial for their use as therapeutics. Here, the authors show that adamantane derivatives interact with a specific binding site on fenestrations that only become available when accessory subunits are bound to the channel.