Key result
Retigabine stabilizes the conducting conformation of the pore and activated voltage sensor conformation of KCNQ channels, an effect that is attenuated upon disruption of channel:PIP2 interactions.
PIP2 plays an important role in coupling retigabine binding to altered voltage-sensing domain function in KCNQ channels.
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May guide KCNQ modulator development; leaves open cardiovascular translation pending clinical data.
Kim et al. (2017) studied this question. Retigabine vs. Disrupted channel:PIP2 interactions was evaluated on Conformational changes of KCNQ3 voltage-sensing domains and ionic conductance. Retigabine stabilizes the conducting conformation of the pore and activated voltage sensor conformation of KCNQ channels, an effect that is attenuated upon disruption of channel:PIP2 interactions.
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