Inhibition of the K+ conductance and Cole-Moore shift of the oncogenic Kv10.1 channel by amiodarone
| Autor: | Arturo Picones, Arturo Hernández-Cruz, A Huanosta-Gutiérrez, Froylan Gómez-Lagunas, A. Reyes-Vaca, Carolina Barriga-Montoya |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Physiology Chemistry Clinical Biochemistry Conductance Gating K+ conductance Amiodarone Molecular medicine Phenotype 03 medical and health sciences 030104 developmental biology 0302 clinical medicine Physiology (medical) medicine Biophysics Patch clamp Receptor 030217 neurology & neurosurgery medicine.drug |
| Zdroj: | Pflügers Archiv - European Journal of Physiology. 470:491-503 |
| ISSN: | 1432-2013 0031-6768 |
| DOI: | 10.1007/s00424-017-2092-x |
| Popis: | The ectopic overexpression of the voltage-dependent Eag1 (Kv10.1) K+ channel is associated with the cancerous phenotype in about 70% of human cancers and tumor cell lines. Recent reports showed 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. Using whole-cell patch clamp, we found that amiodarone inhibits Kv10.1 channel conductance with nanomolar affinity. Additionally, and interestingly, we also report that amiodarone inhibits the characteristic Cole-Moore shift of Eag1 channels. Our observations are interpreted considering the structural-functional characteristics of these channels. We conclude that amiodarone possibly binds with high affinity to the voltage sensor module, altering the gating of Kv10.1. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full text from SpringerLink