Veratridine Can Bind to a Site at the Mouth of the Channel Pore at Human Cardiac Sodium Channel Na_V1.5.

ABSTRACT: The cardiac sodium ion channel (Na_V1.5) is a protein with four domains (DI-DIV), each with six transmembrane segments. Its opening and subsequent inactivation results in the brief rapid influx of Na⁺ ions resulting in the depolarization of cardiomyocytes. The neurotoxin veratridine (VTD) inhibits Na_V1.5 inactivation resulting in longer channel opening times, and potentially fatal action potential prolongation. VTD is predicted to bind at the channel pore, but alternative binding sites have not been ruled out. To determine the binding site of VTD on Na_V1.5, we perform docking calculations and high-throughput electrophysiology experiments in the present study. The docking calculations identified two distinct binding regions. The first site was in t

SUBMITTER: Gulsevin A 

PROVIDER: S-EPMC8878851 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature