Effect of tyrphostin AG879 on Kv 4.2 and Kv 4.3 potassium channels.

ABSTRACT:

Background and purpose

A-type potassium channels (IA) are important proteins for modulating neuronal membrane excitability. The expression and activity of Kv 4.2 channels are critical for neurological functions and pharmacological inhibitors of Kv 4.2 channels may have therapeutic potential for Fragile X syndrome. While screening various compounds, we identified tyrphostin AG879, a tyrosine kinase inhibitor, as a Kv 4.2 inhibitor from. In the present study we characterized the effect of AG879 on cloned Kv 4.2/Kv channel-interacting protein 2 (KChIP2) channels.

Experimental approach

To screen the library of pharmacologically active compounds, the thallium flux assay was performed on HEK-293 cells transiently-transfected with Kv 4.2 cDNA using the Maxcyte transfection system.

SUBMITTER: Yu H 

PROVIDER: S-EPMC4500372 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature