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

Tijdschriftbijdrage - Tijdschriftartikel

The marine polycyclic-ether toxin gambierol and 1-butanol (n-alkanol) inhibit Shaker-type Kv 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 Kv channels via distinct parts of the gating machinery.
Tijdschrift: Toxicon
ISSN: 0041-0101
Volume: 120
Pagina's: 57 - 60
Jaar van publicatie:2016
Auteurs:International