Key result
Crystal structures of the human TREK-2 channel in complex with norfluoxetine reveal mechanisms of channel mechanosensitivity and regulation by diverse stimuli.
Population
Human TREK-2 channel (KCNK10/K2P10)
Design
Preclinical
Authors
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Structural details of TREK-2 gating and norfluoxetine binding extend mechanistic understanding; clinical relevance for cardiovascular applications remains untested.
Structural elucidation of the TREK-2 channel provides a mechanistic basis for its mechanosensitivity and regulation by diverse stimuli, including off-target effects of fluoxetine.
Dong et al. (2015) studied this question. Norfluoxetine was evaluated on Crystal structures of the human TREK-2 channel. Crystal structures of the human TREK-2 channel in complex with norfluoxetine reveal mechanisms of channel mechanosensitivity and regulation by diverse stimuli.
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