Article
One drug-sensitive subunit is sufficient for a near-maximal retigabine effect in KCNQ channels.
The Journal of general physiology - 1 Oct 2018
Yau Michael C, Kim Robin Y, Wang Caroline K, Li Jingru, Ammar Tarek, Yang Runying Y, Pless Stephan A, Kurata Harley T
Abstract excerpt
Retigabine is an antiepileptic drug and the first voltage-gated potassium (Kv) channel opener to be approved for human therapeutic use. Retigabine is thought to interact with a conserved Trp side chain in the pore of KCNQ2-5 (Kv7.2-7.5) channels, causing a pronounced hyperpolarizing shift in the voltage dependence of activation. In this study, we investigate the functional stoichiometry of retigabine actions by...
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