Gambierol and n-alkanols inhibit Shaker Kv channel via distinct binding sites outside the K(+) pore.
Toxicon
; 120: 57-60, 2016 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-27475861
ABSTRACT
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.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ciguatoxinas
/
1-Butanol
/
Bloqueadores dos Canais de Potássio
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Superfamília Shaker de Canais de Potássio
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article