Emerging Concepts in Ion Channel Biophysics

Emerging Concepts in Ion Channel Biophysics

Poster Abstracts

33-POS Board 33 Inhibition of the K + -Conductance and Cole-moore Shift of the Tumor Related Kv10.1 Channel by Amiodarone Carolina Barriga-Montoya, Areli Huanosta-Gutiérrez, Arturo Reyes-Vaca, Arturo Hernández- Cruz, Arturo Picones, Froylán Gómez-Lagunas. Universidad Nacional Autónoma de México, Ciudad de México, Mexico. Ectopic overexpression of the voltage-dependent Eag1 (Kv10.1) K + channel is associated with the cancerous phenotype of about 70% of human cancers and tumor cell lines. Recent reports show that, compared with the canonical Shaker-related Kv family, Kv10.1 presents unique structural and functional properties. Herein we report the interaction of the class III anti- arrhythmic compound amiodarone with Kv10.1. We found that amiodarone inhibits the K+- conductance with nanomollar affinity. Additionally amiodarone inhibits the characteristic Cole- Moore shift of Eag channels. Our observations are interpreted considering the recently reported structure of the channel. We conclude that amiodarone binds both to the pore and voltage sensor modules, including within the latter the cytoplasmic Per-Arnt-Sim-domain which is known to regulate the voltage dependency of Kv10.1.

101 

Made with FlippingBook - Online magazine maker