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Vandetanib activates KCNH2. 10 / 10
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"As shown in Figure 9(b), D, the inactivation time constant was shortened by treatment with vandetanib with or without Gin Rg3; no effect was acted on the group between vandetanib and vandetanib with Gin Rg3, which indicated that vandetanib could accelerate the inactivation process of the hERG channel, while Rg3 has no action to reverse the effect on van-induced inactivation time constant shortening."
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"As shown in Figure 6(f), the inactivation time constant was shortened by treatment with vandetanib, which indicated that vandetanib can accelerate the inactivation process of the hERG K channel."
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"The dynamic characteristics of hERG channel caused by vandetanib have not been analyzed."
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"An ion channel study of the effects of vandetanib in hiPSC-CMs showed that the vandetanib induced prolongation of the APD and decrease in V max were caused by inhibition of I hERG and I Na, respectively (XREF_FIG)."
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"In this study, we analyzed the hERG current dynamics induced by vandetanib, including activation, inactivation, and deactivation."
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"A serum and glucocorticoid kinase 1 (SGK1) activator, C 4 -ceramide, prevented the nilotinib-and vandetanib-induced hERG protein downregulation and thus the incidence of cellrrhythmias."
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"This suggests that vandetanib prolongs the duration of cardiac action potential by affecting the activation and inactivation of hERG current."
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"In addition, some tyrosine kinase inhibitors (vandetanib) can inhibit hERG potassium channels and/or impair channel transport, thereby causing prolongation of the QT interval and increasing the risk of ventricular arrhythmias (Carpenter et al. 2020; Cubeddu et al. 2022)."
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"These results suggest that van accelerated hERG channel inactivation, and Gin Rg3 3 μM had no effect on hERG channel inactivation induced by vandetanib."
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"The results showed that vandetanib accelerated hERG channel inactivation.The representative current traces are shown in Figure 9(b), A–C, the time constant of inactivation process."
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