Does pharmacologic inhibition of NCX1 with ORM-10103 normalize action potential duration and reduce delayed afterdepolarizations in patient-derived iPSC-CMs with the ATP1A3-D801N variant?
Patient-derived induced pluripotent stem cell cardiomyocytes (iPSC-CMs) from individuals with alternating hemiplegia of childhood (AHC) heterozygous for the ATP1A3-D801N variant, and in silico models
Pharmacologic inhibition of NCX1 with ORM-10103
Untreated iPSC-CMsD801N and Wild-type (WT) iPSC-CMs
Action potential duration (APD), intracellular and sarcoplasmic reticulum Ca2+ levels, and delayed afterdepolarizations (DADs)surrogate
The ATP1A3-D801N variant causes arrhythmogenesis via NCX1-mediated calcium overload, identifying NCX1 as a potential therapeutic target for these patients.
Short QT syndrome is a heritable arrhythmia disorder linked to sudden cardiac death. We recently identified that individuals with alternating hemiplegia of childhood (AHC), a rare neurodevelopmental disorder, can exhibit shortened corrected QT intervals and elevated risk for ventricular fibrillation. This is especially true for patients with AHC heterozygous for the recurrent ATP1A3-D801N variant, though the underlying cardiac mechanism remains unclear. We hypothesized that the D801N missense impairs Na+/K+-ATPase function, causing Ca2+ overload, shortened action potential duration (APD), and arrhythmias. Using in silico modeling and patient-derived induced pluripotent stem cell cardiomyocytes (iPSC-CMsD801N), we observed shorter APD, elevated intracellular and sarcoplasmic reticulum Ca2+ levels, and delayed afterdepolarizations (DADs) compared with WT. Additionally, increased Ca²+ influx via the Na+/Ca2+ exchanger (NCX1) during depolarization was observed in iPSC-CMsD801N. Simulations and in vitro experiments suggest that reduced ATPase function accelerated inactivation of L-type Ca2+ channels. Pharmacologic inhibition of NCX1 with ORM-10103 normalized APD and reduced DADs. These findings support a Ca2+-mediated mechanism for arrhythmogenesis in ATP1A3-D801N carriers and identify NCX1 as a potential therapeutic target.
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Minu‐Tshyeto Bidzimou
Padmapriya Muralidharan
Zhushan Zhang
JCI Insight
Northwestern University
Duke University
University of California, Davis
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Bidzimou et al. (Tue,) studied this question.
www.synapsesocial.com/papers/69d893a86c1944d70ce04a78 — DOI: https://doi.org/10.1172/jci.insight.197721