Common Structural Pattern for Flecainide Binding in Atrial-Selective K_v1.5 and Na_v1.5 Channels: A Computational Approach.

ABSTRACT: Atrial fibrillation (AF) is the most common cardiac arrhythmia. Its treatment includes antiarrhythmic drugs (AADs) to modulate the function of cardiac ion channels. However, AADs have been limited by proarrhythmic effects, non-cardiovascular toxicities as well as often modest antiarrhythmic efficacy. Theoretical models showed that a combined blockade of Na_v1.5 (and its current, I_Na) and K_v1.5 (and its current, I_Kur) ion channels yield a synergistic anti-arrhythmic effect without alterations in ventricles. We focused on K_v1.5 and Na_v1.5 to search for structural similarities in their binding site (BS) for flecainide (a common blocker and widely prescribed AAD) as a first step for prospective rational multi-target

SUBMITTER: Mazola Y 

PROVIDER: S-EPMC9318806 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature