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Curcumin inhibits hERG potassium channels in vitro
Toxicology Letters, 2012Curcumin is reported to exert antioxidant, anti-inflammatory, antiviral, antibacterial, antifungal, and anti-tumor activities. The human ether-a-go-go related gene (hERG) encodes the rapid component of the delayed rectifier K⁺ currents. Inhibition of hERG K⁺ channels leads to cardiac repolarization prolongation, which contributes to either the anti ...
Chao-Wei, Hu +7 more
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Structure of the pore-helix of the hERG K+ channel
European Biophysics Journal, 2009The hERG K(+) channel undergoes rapid inactivation that is mediated by 'collapse' of the selectivity filter, thereby preventing ion conduction. Previous studies have suggested that the pore-helix of hERG may be up to seven residues longer than that predicted by homology with channels with known crystal structures.
Pages, Guilhem +6 more
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Modulation of HERG channel inactivation by external cations
European Biophysics Journal, 2003We investigated the effect of external cations on the permeability characteristics and gating kinetics of the human ether- à- go- go-related gene (HERG) current using the whole-cell patch-clamp technique. Inward HERG currents were recorded on hyperpolarization in 140 mM external Cs(+) and Rb(+), as well as K(+). The permeability ratios of Rb(+) and Cs(+
Jae Boum, Youm +2 more
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Unique interaction of scorpion toxins with the hERG channel
Journal of Molecular Recognition, 2004AbstractERG potassium channels specify one component of the delayed rectifier in the heart and are likely to play an important functional role in other excitable cells. Compared to other K+ channels, the human ERG (hERG) channel possesses an unusually long S5‐P linker that presumably forms an alpha‐helix important for channel function.
Yuliya V, Korolkova +2 more
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Toxin modulators and blockers of hERG K+ channels
Toxicon, 2012The K(+) channel encoded by the Ether-á-go-go-Related Gene (ERG) is expressed in different tissues of different animal species. There are at least three subtypes of this channel, being the sub-type 1 (ERG1) crucial in the repolarization phase of the cardiac action potential.
J M, Jiménez-Vargas +2 more
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A model for identifying HERG K+ channel blockers
Bioorganic & Medicinal Chemistry, 2004Acquired long QT syndrome (LQTS) occurs frequently as a side effect of blockade of cardiac HERG K(+) channels by commonly used medications. A large number of structurally diverse compounds have been shown to inhibit K(+) current through HERG. There is considerable interest in developing in silico tools to filter out potential HERG blockers early in the
Alex M, Aronov, Brian B, Goldman
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Comparison of the Effects of Metoclopramide and Domperidone on HERG Channels
Pharmacology, 2005Torsades de pointes (TdP) is a potentially fatal form of ventricular arrhythmia that occurs under conditions where cardiac repolarization is delayed (as indicated by prolonged QT intervals from electrocardiographic recordings). A likely mechanism for QT prolongation and TdP is blockade of the rapid component of the cardiac delayed rectifier K<sup>
Sonja, Claassen, Bernd J, Zünkler
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The Interactions Between hERG Potassium Channel and Blockers
Current Topics in Medicinal Chemistry, 2009The human ether-a-go-go related gene (hERG) potassium channel is critical to the QT interval in the human heart measured by the electrocardiogram (ECG). The blockade of hERG would induce undesired lethal arrhythmia, named torsades de pointes (TdP), a rare but life-threatening symptom.
Lupei, Du, Minyong, Li, Qidong, You
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Inhibition of HERG channels by the local anaesthetic articaine
European Journal of Anaesthesiology, 2007Articaine is an amide local anaesthetic widely used in dentistry. Human ether-a-go-go-related gene (HERG) potassium channels constitute potential targets involved in cardiotoxic side-effects of various pharmacological agents including amide local anaesthetics.
C C, Siebrands, P, Friederich
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[The effect of lidocaine on hERG (+) channels].
Yao xue xue bao = Acta pharmaceutica Sinica, 2018We studied the effects of the lidocaine on the hERG K(+) channels with a focus on the electrophysiology of the heart. The hERG current was recorded using the conventional whole-cell patch clamp technique and the channel protein expression level was measured with Western blot in HEK 293 cells stablely expressed hERG K(+) channels.
Yu-hong, Wang +4 more
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