IMIS

A new integrated search interface will become available in the next phase of marineinfo.org.
For the time being, please use IMIS to search available data

 

[ report an error in this record ]basket (0): add | show Print this page
Gambierol and n-alkanols inhibit Shaker Kv channel via distinct binding sites outside the K+ pore
Martínez-Morales, E.; Kopljar, I.; Rainier, J.D.; Tytgat, J.; Snyders, D.J.; Labro, A.J. (2016). Gambierol and n-alkanols inhibit Shaker Kv channel via distinct binding sites outside the K+ pore. Toxicon 120: 57-60. https://dx.doi.org/10.1016/j.toxicon.2016.07.017
In: Toxicon. Elsevier: Oxford. ISSN 0041-0101; e-ISSN 1879-3150, more
Peer reviewed article  
Available in  Authors 
Keyword
    Marine/Coastal
Author keywords
    Potassium channel; Gating modifier; Lipophilic marine toxin; 1-Alcohol;Electrophysiology
Authors  Top 
  • Martínez-Morales, E., more
  • Kopljar, I., more
  • Rainier, J.D.
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.
All data in the Integrated Marine Information System (IMIS) is subject to the VLIZ privacy policy Top | Authors