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Targeting Arrhythmogenic Late Sodium Current by FHF1A-Derivative FixR in Heart Failure Cardiomyocytes - PubMed

4 hours ago
  • #late sodium current
  • #antiarrhythmic
  • #heart failure
  • Enhanced late sodium current (INa,L) contributes to proarrhythmia in heart failure (HF), with FHF family proteins and CaMKII as key modulators.
  • Expression of inhibitory FHF long isoforms is reduced in human, rabbit, and mouse failing hearts, correlating with increased INa,L in both HFrEF and HFpEF.
  • The FHF1A-derived peptide FixR selectively reduces pathological INa,L without affecting other major cardiac ion currents, showing potent antiarrhythmic effects in cellular models.
  • FixR mitigates proarrhythmic action potential changes and delays afterdepolarizations in failing cardiomyocytes, effects paralleled by the INa,L inhibitor GS967 and CaMKII inhibitor AIP.
  • In vivo delivery of FixR in transgenic mice attenuates QT prolongation and arrhythmia susceptibility, supporting its therapeutic potential in HF.