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Title
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Gambierol and n-alkanols inhibit Shaker Kv channel via distinct binding sites outside the pore
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Author
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Abstract
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| 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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Language
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Dutch, English
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Source (journal)
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Toxicon. - Oxford
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Publication
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Oxford
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2016
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ISSN
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0041-0101
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DOI
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10.1016/J.TOXICON.2016.07.017
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Volume/pages
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120
(2016)
, p. 57-60
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ISI
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000383824100009
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Pubmed ID
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27475861
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Full text (Publisher's DOI)
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Full text (open access)
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Full text (publisher's version - intranet only)
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