Results 171 to 180 of about 17,722 (214)

hERG potassium channels and cardiac arrhythmia

Nature, 2006
hERG potassium channels are essential for normal electrical activity in the heart. Inherited mutations in the HERG gene cause long QT syndrome, a disorder that predisposes individuals to life-threatening arrhythmias. Arrhythmia can also be induced by a blockage of hERG channels by a surprisingly diverse group of drugs.
Michael C, Sanguinetti, Martin, Tristani-Firouzi   +1 more
openaire   +4 more sources

Pharmacophore modeling for hERG channel facilitation

Biochemical and Biophysical Research Communications, 2012
Human ether-a-go-go-related gene (hERG) channels play a critical role in cardiac action potential repolarization. The unintended block of hERG channels by compounds can prolong the cardiac action potential duration and induce arrhythmia. Several compounds not only block hERG channels but also enhance channel activation after the application of a ...
Yuko, Yamakawa, Kazuharu, Furutani, Atsushi, Inanobe, Yuko, Ohno, Yoshihisa, Kurachi   +4 more
openaire   +2 more sources

Molecular Determinants of hERG Channel Block

Molecular Pharmacology, 2006
Drug-induced block of cardiac hERG K+ channels causes acquired long QT syndrome. Here, we characterized the molecular mechanism of hERG block by two low-potency drugs (Nifekalant and bepridil) and two high-potency drugs 1-[2-(6-methyl-2pyridyl)ethyl]-4-(4-methylsulfonyl aminobenzoyl)piperidine (E-4031) and dofetilide).
Kamiya, K, Niwa, R, Mitcheson, JS, Sanguinetti, MC   +3 more
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Escitalopram block of hERG potassium channels

Naunyn-Schmiedeberg's Archives of Pharmacology, 2013
Escitalopram, a selective serotonin reuptake inhibitor, is the pharmacologically active S-enantiomer of the racemic mixture of RS-citalopram and is widely used in the treatment of depression. The effects of escitalopram and citalopram on the human ether-a-go-go-related gene (hERG) channels expressed in human embryonic kidney cells were investigated ...
Yun Ju, Chae, Ji Hyun, Jeon, Hong Joon, Lee, In-Beom, Kim, Jin-Sung, Choi, Ki-Wug, Sung, Sang June, Hahn   +6 more
openaire   +2 more sources

HERG K+ channels: friend and foe

Trends in Pharmacological Sciences, 2001
The K+ channel encoded by the human ether-à-go-go related gene (HERG) is one of many ion channels that are crucial for normal action potential repolarization in cardiac myocytes. HERG encodes the pore-forming subunit of the rapid component of the delayed rectifier K+ channel, I(K(Vr)).
J I, Vandenberg, B D, Walker, T J, Campbell   +2 more
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IKr: The hERG Channel

Journal of Molecular and Cellular Cardiology, 2001
G.-N. Tseng. I(Kr): The hERG Channel. Journal of Molecular and Cellular Cardiology (2001) 33, 835-849. The rapid delayed rectifier (I(Kr)) channel is important for cardiac action potential repolarization. Suppressing I(Kr)function, due to either genetic defects in its pore-forming subunit (hERG) or adverse drug effects, can lead to long-QT (LQT ...
openaire   +2 more sources

Open Channel Block of HERG K⁺Channels by Vesnarinone

Molecular Pharmacology, 2001
Vesnarinone, a cardiotonic agent, blocks I(Kr) and, unlike other I(Kr) blockers, produces a frequency-dependent prolongation of action potential duration (APD). To elucidate the mechanisms, we studied the effects of vesnarinone on HERG, the cloned human I(Kr) channel, heterologously expressed in Xenopus laevis oocytes.
K, Kamiya, J S, Mitcheson, K, Yasui, I, Kodama, M C, Sanguinetti   +4 more
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Curcumin inhibits hERG potassium channels in vitro

Toxicology Letters, 2012
Curcumin 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, Yue, Sheng, Qin, Zhang, Hui-Bin, Liu, Xin, Xie, Wen-Chao, Ma, Rong, Huo, De-Li, Dong   +7 more
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The Phenothiazine Drugs Inhibit hERG Potassium Channels

Drug and Chemical Toxicology, 2005
Cardiovascular adverse effects from phenothiazine drugs are common. The most serious consequences of treatment, arrhythmias and sudden death, are probably rare and most likely to be caused primarily by blockade of cardiac potassium channels such as the human ether-a-go-go-related gene (hERG) channel, which plays a central role in arrhythmogenesis. This
Ki-Suk, Kim, Eun-Joo, Kim
openaire   +2 more sources