Click here to close Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly. We suggest using a current version of Chrome, FireFox, or Safari.
J Gen Physiol June 1, 2011; 137 (6): 563-77.

An electrostatic potassium channel opener targeting the final voltage sensor transition.

Börjesson SI , Elinder F .

Free polyunsaturated fatty acids (PUFAs) modulate the voltage dependence of voltage-gated ion channels. As an important consequence thereof, PUFAs can suppress epileptic seizures and cardiac arrhythmia. However, molecular details for the interaction between PUFA and ion channels are not well understood. In this study, we have localized the site of action for PUFAs on the voltage-gated Shaker K channel by introducing positive charges on the channel surface, which potentiated the PUFA effect. Furthermore, we found that PUFA mainly affects the final voltage sensor movement, which is closely linked to channel opening, and that specific charges at the extracellular end of the voltage sensor are critical for the PUFA effect. Because different voltage-gated K channels have different charge profiles, this implies channel-specific PUFA effects. The identified site and the pharmacological mechanism will potentially be very useful in future drug design of small-molecule compounds specifically targeting neuronal and cardiac excitability.

PubMed ID: 21624947
PMC ID: PMC3105513
Article link: J Gen Physiol

Species referenced: Xenopus
Genes referenced: kcna2 tbx2

Article Images: [+] show captions
References [+] :
Baker, Three transmembrane conformations and sequence-dependent displacement of the S4 domain in shaker K+ channel gating. 1998, Pubmed