Insights into the stimulatory mechanism of 2-aminoethoxydiphenyl borate on TREK-2 potassium channel

Highlights • C-terminus is essential for 2-APB effects on TREK-2. • The distal Ct regulates the interaction between 2-APB and TREK-2 negatively. • His368 is essential for the stimulatory effects of 2-APB on TREK-2. • The bottom of M2 is a secondary active site of 2-APB in TREK-2. • The key elements...

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Veröffentlicht in:	Neuroscience 2015-08, Vol.300, p.85-93
Hauptverfasser:	Zhuo, R.-G, Liu, X.-Y, Zhang, S.-Z, Wei, X.-L, Zheng, J.-Q, Xu, J.-P, Ma, X.-Y
Format:	Artikel
Sprache:	eng
Schlagworte:	2-APB Animals Boron Compounds - pharmacology C-terminal domain Catalytic Domain gate mechanism Humans Membrane Potentials - drug effects Membrane Potentials - physiology Membrane Transport Modulators - pharmacology Mutation Neurology Oocytes Patch-Clamp Techniques Potassium Channels, Tandem Pore Domain - genetics Potassium Channels, Tandem Pore Domain - metabolism selectivity filter TREK-1 TREK-2 Xenopus laevis
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Zusammenfassung:	Highlights • C-terminus is essential for 2-APB effects on TREK-2. • The distal Ct regulates the interaction between 2-APB and TREK-2 negatively. • His368 is essential for the stimulatory effects of 2-APB on TREK-2. • The bottom of M2 is a secondary active site of 2-APB in TREK-2. • The key elements required for 2-APB function are not involved in SF gating.
ISSN:	0306-4522 1873-7544
DOI:	10.1016/j.neuroscience.2015.05.012