Title
Gambierol and n-alkanols inhibit Shaker Kv channel via distinct binding sites outside the <tex>$K^{+}$</tex> pore Gambierol and n-alkanols inhibit Shaker Kv channel via distinct binding sites outside the <tex>$K^{+}$</tex> pore
Author
Faculty/Department
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences . Biomedical Sciences
Publication type
article
Publication
Oxford ,
Subject
Pharmacology. Therapy
Source (journal)
Toxicon. - Oxford
Volume/pages
120(2016) , p. 57-60
ISSN
0041-0101
ISI
000383824100009
Carrier
E
Target language
Dutch (dut)
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
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.
E-info
https://repository.uantwerpen.be/docman/iruaauth/483b9b/135773.pdf
Full text (open access)
https://repository.uantwerpen.be/docman/irua/e80b8f/135773.pdf
Handle