Human ether-à-go-go-related potassium channel: exploring SAR to improve drug design
Drug Discovery Today, 2020hERG is best known as a primary anti-target, the inhibition of which is responsible for serious side effects. A renewed interest in hERG as a desired target, especially in oncology, was sparked because of its role in cellular proliferation and apoptosis.
Cavalluzzi MM+6 more
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Direct Block of Human Ether-a-go-go-Related Gene Potassium Channels by Caffeine
The Journal of Pharmacology and Experimental Therapeutics, 2006The human ether-a-go-go-related gene (hERG) potassium channel is expressed in a variety of cell types, including neurons, tumor cells, and cardiac myocytes. In the heart, it is important for repolarization of the cardiac action potential. Attenuation of hERG current can cause long QT syndrome and cardiac arrhythmias such as torsades de pointes ...
Cockerill, SL, Mitcheson, JS
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Potassium channel ether à go-go mRNA expression in the spiral ligament of the rat
Hearing Research, 1999Identification of the K+ transporters located in the lateral wall of the cochlea is essential for a better understanding of the mechanisms by which a positive endocochlear potential and a high K+ concentration are achieved in endolymph. In this study, we have determined the distribution of the K+ channel rat ether à go-go (eag) mRNA in the cochlea ...
Elisabeth Sauvaget+4 more
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Ether à-go-go Potassium Channels [PDF]
Ion transport is crucial for maintaining proper cellular function; this important task is performed by several ▶membrane transporters including ▶ ion channels. Among other functions, ion channels play key roles in neurotransmission, muscle contraction, metabolism, sensory transduction, ▶ apoptosis, and cell cycle progression.
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Ether à go-go potassium channels and cancer
Cancer Letters, 2006Ion channels play important roles in health and disease. In the last few years, an interesting relationship between potassium channels and cancer has evolved. Especially, members of the ether à go-go (EAG) potassium channels family have gained interest as research tools for detection and therapy of different cancers.
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Inhibition of Human Ether-A-Go-Go Potassium Channels by Cocaine
Molecular Pharmacology, 2001Cocaine is a potent cardiac stimulant and its use has been linked to life-threatening arrhythmias in humans. A prominent effect of cocaine in the heart is a suppression of the delayed-rectifier potassium current (I(K)) that is important for cardiac repolarization.
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Biophysical properties of zebrafish ether-à-go-go related gene potassium channels
Biochemical and Biophysical Research Communications, 2009The zebrafish is increasingly recognized as an animal model for the analysis of hERG-related diseases. However, functional properties of the zebrafish orthologue of hERG have not been analyzed yet. We heterologously expressed cloned ERG channels in Xenopus oocytes and analyzed biophysical properties using the voltage clamp technique.
Nora Niemer+12 more
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Identification of Ether à Go-Go and Calcium-Activated Potassium Channels in Human Melanoma Cells
Journal of Membrane Biology, 1999Ion channels and intracellular Ca2+ are thought to be involved in cell proliferation and may play a role in tumor development. We therefore characterized Ca(2+)-regulated potassium channels in the human melanoma cell lines IGR1, IPC298, and IGR39 using electrophysiological and molecular biological methods.
Oxana Gavrilova-Ruch+4 more
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Toxins interacting with ether-à-go-go-related gene voltage-dependent potassium channels
Toxicon, 2007The critical role that ether-à-go-go-related gene (erg) K(+) channels play in mating in Caenorhabditis elegans, neuronal seizures in Drosophila and cardiac action potential repolarization in humans has been well documented. Three erg genes (erg1, erg2 and erg3) have been identified and characterized.
Enzo Wanke, Rita Restano-Cassulini
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Mallotoxin Is a Novel Human Ether-a-go-go-Related Gene (hERG) Potassium Channel Activator
The Journal of Pharmacology and Experimental Therapeutics, 2006Human ether-a-go-go-related gene (hERG) encodes a rapidly activating delayed rectifier potassium channel that plays important roles in cardiac action potential repolarization. Although many drugs and compounds block hERG channels, activators of the channel have only recently been described.
David P. Brooks+5 more
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