Key result
The PTK inhibitors genistein and AG556 decreased human atrial IKur and cloned hKv1.5 channels by inhibiting EGFR TK, whereas the Src kinase inhibitor PP2 increased these currents.
Population
Human atrial cells and HEK 293 cells stably expressing hKv1.5 channels
Design
Preclinical
Authors
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Suppresses human atrial IKur via EGFR inhibition; leaves open whether EGFR TK targeting modulates atrial arrhythmias.
EGFR TK and soluble Src kinases have opposite effects on human atrial IKur, suggesting a complex regulatory mechanism for atrial repolarization.
Xiao et al. (2017) studied Human atrial repolarization. PTK inhibitors (genistein, tyrphostin AG556, PP2) vs. Baseline / Orthovanadate was evaluated on IKur and hKv1.5 current amplitude and tyrosine phosphorylation. The PTK inhibitors genistein and AG556 decreased human atrial IKur and cloned hKv1.5 channels by inhibiting EGFR TK, whereas the Src kinase inhibitor PP2 increased these currents.
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