Gambierol and n-alkanols inhibit Shaker Kv channel via distinct binding sites outside the K+ pore

摘要

The marine polycyclic-ether toxin gambierol and 1-butanol (n-allcanol) inhibit Shaker-type K-v channels by interfering with the gating machinery. Competition experiments indicated that both compounds do not share an overlapping binding site but gambierol is able to affect 1-butanol affinity for Shaker through an allosteric effect. Furthermore, the Shaker-P475A mutant, which inverses 1-butanol effect, is inhibited by gambierol with nM affinity. Thus, gambierol and 1-butanol inhibit Shaker-type K-v channels via distinct parts of the gating machinery. (C) 2016 Elsevier Ltd. All rights reserved.