Key result
Efsevin restores rhythmic cardiac contractions in zebrafish tremblor embryos and mammalian cardiomyocytes by binding to VDAC2 and potentiating mitochondrial Ca2+ uptake.
Why the study?
Does efsevin restore rhythmic cardiac contractions in models of Ca2+ overload-induced arrhythmia?
Does efsevin restore rhythmic cardiac contractions in models of Ca2+ overload-induced arrhythmia?
p-value: p=<0.001
Efsevin restores rhythmic cardiac contractions in models of calcium overload by potentiating VDAC2-dependent mitochondrial calcium uptake, highlighting a novel therapeutic target for arrhythmias.
Tightly regulated Ca(2+) homeostasis is a prerequisite for proper cardiac function. To dissect the regulatory network of cardiac Ca(2+) handling, we performed a chemical suppressor screen on zebrafish tremblor embryos, which suffer from Ca(2+) extrusion defects. Efsevin was identified based on its potent activity to restore coordinated contractions in tremblor. We show that efsevin binds to VDAC2, potentiates mitochondrial Ca(2+) uptake and accelerates the transfer of Ca(2+) from intracellular stores into mitochondria. In cardiomyocytes, efsevin restricts the temporal and spatial boundaries of Ca(2+) sparks and thereby inhibits Ca(2+) overload-induced erratic Ca(2+) waves and irregular contractions. We further show that overexpression of VDAC2 recapitulates the suppressive effect of efsevin on tremblor embryos whereas VDAC2 deficiency attenuates efsevin's rescue effect and that VDAC2 functions synergistically with MCU to suppress cardiac fibrillation in tremblor. Together, these findings demonstrate a critical modulatory role for VDAC2-dependent mitochondrial Ca(2+) uptake in the regulation of cardiac rhythmicity.
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Shimizu et al. (2015) studied Cardiac fibrillation (aberrant Ca2+ handling). Efsevin vs. Vehicle was evaluated on Restoration of rhythmic cardiac contractions (p=<0.001). Efsevin restores rhythmic cardiac contractions in zebrafish tremblor embryos and mammalian cardiomyocytes by binding to VDAC2 and potentiating mitochondrial Ca2+ uptake.
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