Article
A benzodiazepine activator locks Kv7.1 channels open by electro-mechanical uncoupling.
Communications biology - 1 Apr 2022
Schreiber Julian A, Möller Melina, Zaydman Mark, Zhao Lu, Beller Zachary, Becker Sebastian, Ritter Nadine, Hou Panpan, Shi Jingyi, Silva Jon, Wrobel Eva, Strutz-Seebohm Nathalie, Decher Niels, Schmitt Nicole, Meuth Sven G, Düfer Martina, Wünsch Bernhard, Cui Jianmin, Seebohm Guiscard
Abstract excerpt
Loss-of-function mutations in Kv7.1 often lead to long QT syndrome (LQTS), a cardiac repolarization disorder associated with arrhythmia and subsequent sudden cardiac death. The discovery of agonistic IKs modulators may offer a new potential strategy in pharmacological treatment of this disorder. The benzodiazepine derivative (R)-L3 potently activates Kv7.1 channels and shortens action potential duration, thus may...
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