Issues
Generation and characterization of cell lines stably expressing different isoforms of kcnq potassium channels suitable for drug screening
Voltage-gated Kv7.2 and Kv7.3 channels, belonging to the Kv7 or KCNQ potassium channel family, are responsible for regulation of M-currents,1 a low-threshold, depolarization-activated K+ current, uniquely suited to suppress bursting and epileptiform activity, while permitting maintenance of responses to ordinary excitatory inputs.2 Pharmacological activation of such channels may be a strategy to treat hyperexcitability conditions such as epilepsy and neuropathic pain. After discontinuation of the anticonvulsant retigabine,3 the identification of novel Kv7.2/Kv7.3 channel activators is an unmet medical need with promising therapeutic efficacy. In the present work, we show the generation of cell lines stably expressing different isoforms of KCNQ potassium channels and their characterization in functional assays to allow generation of High-Throughput Screening (HTS) data for the identification of novel Kv7.2/Kv7.3 (KCNQ 2/3) openers.
