IndraLab

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Celastrol inhibits KCNH2. 13 / 14
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"The fact that the inhibition of Celastrol changes neither the steady state of activation nor the steady state of inactivation also indirectly supports the idea that Celastrol directly blocks the channels.Our mutagenesis data suggests that Celastrol directly blocks hERG channels by binding the pore region of the channels."
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"The model explains the reason very well that S624A makes the most reduction of Celastrol inhibition and indicts that Celastrol inhibits hERG channels by directly blocking the channels.Celastrol has many pharmacological activities."
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"Sun et al. [15] demonstrated that, at 200 nM, celastrol inhibits cardiac Kir2.1 and hERG potassium channels with dual effects on both ion conductivity and protein trafficking, leading to QT prolongation."
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"Moreover, celastrol can block the ion conduction of cardiac Kir2.1 and hERG potassium channels [55] ."
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"Considering Celastrol is one of TWHF main components and has in many aspects to TWHF, a potential mechanism of cardiac toxicity of TWHF is likely due to hERG channel blockade by Celastrol."
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"In addition, celastrol blocks ion conduction of cardiac Kir2.1 and hERG potassium channels and reduces channel density on cell surface upon chronic treatment, which may predict cardiotoxicity."
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"Mol Pharmacol 2004; 65:214-9; PMID :14722253; http://dx.doi.org/ 10.1124/mol.65.1.214 [35] Sun H, Liu X, Xiong Q, Shikano S, Li M. Chronic inhibition of cardiac Kir2.1 and HERG potassium channels by celastrol with dual effects on both ion conductivity and protein trafficking."
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"Chronic inhibition of cardiac Kir2.1 and HERG potassium channels by celastrol with dual effects on both ion conductivity and protein trafficking."
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"Celastrol inhibited the activities of hERG potassium channels, causal to QT interval prolongation."
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"Celastrol has additionally been shown to suppress hERG potassium channel activity by inhibiting hERG maturation ( Sun et al., 2006 ), which is seen with existing HSP90 inhibitors and is hypothesized t[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"We further found that Celastrol, one of main components of TWHF, inhibits hERG with an IC 50 of 0.83 muM."
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"Celastrol blocks the ion conduction of cardiac Kir2.1 and hERG potassium channels and reduces channel density on the cell surface upon chronic treatment, which may predict cardiotoxicity."
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"4 The inhibition of hERG channels by celastrol was frequency dependent."
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