Results 181 to 190 of about 12,393 (207)

AMP-activated protein kinase regulates hERG potassium channel

Pflügers Archiv - European Journal of Physiology, 2013
Besides their role in cardiac repolarization, human ether-a-go-go-related gene potassium (hERG) channels are expressed in several tumor cells including rhabdomyosarcoma cells. The channels foster cell proliferation. Ubiquitously expressed AMP-dependent protein kinase (AMPK) is a serine-/threonine kinase, stimulating energy-generating and inhibiting ...
Almilaji, Ahmad, Elvira, Bernat, Fajol, Abul, Pakladok, Tatsiana, Honisch, Sabina, Shumilina, Ekaterina, Lang, Florian, Föller, Michael, Muñoz Hernando, Carlos   +8 more
openaire   +3 more sources

The Interactions Between hERG Potassium Channel and Blockers

Current Topics in Medicinal Chemistry, 2009
The 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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Phenytoin and phenobarbital inhibit human HERG potassium channels

Epilepsy Research, 2003
Drugs that inhibit the cardiac rapid delayed rectifier potassium ion current (IKr) channel can be proarrhythmic and their clinical use has been associated with sudden unexpected death (SUD). Since SUD is about 20 times more common among people with epilepsy than in the general population, and some data indicate that drug treatment may contribute, we ...
Bengt R, Danielsson, Kate, Lansdell, Leslie, Patmore, Torbjörn, Tomson   +3 more
openaire   +2 more sources

Modulation of HERG potassium channel properties by external pH

Pfl�gers Archiv European Journal of Physiology, 1999
We expressed the human eag-related gene (HERG), known to encode for the cardiac potassium channel IKr, in Chinese hamster ovary (CHO) cells. This study investigated effects of external pH (pHo) on HERG current properties using the whole-cell patch-clamp technique.
J, Bérubé, M, Chahine, P, Daleau
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The hERG potassium channel and hERG screening for drug-induced torsades de pointes

Pharmacology & Therapeutics, 2008
Drug-induced torsades de pointes (TdP) arrhythmia is a major safety concern in the process of drug design and development. The incidence of TdP tends to be low, so early pre-clinical screens rely on surrogate markers of TdP to highlight potential problems with new drugs.
Hancox, JC, McPate, MJW, El Harchi, A, Zhang, YH   +3 more
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Inhibition of cardiac HERG potassium channels by antidepressant maprotiline

European Journal of Pharmacology, 2006
Many drugs block delayed rectifier K+ channels and prolong the cardiac action potential duration. Here we investigate the molecular mechanisms of voltage-dependent block of human ether-a-go-go-related gene (HERG) K+ channels expressed in cells HEK-293 and Xenopus oocytes by maprotiline.
Tania, Ferrer-Villada, Ricardo A, Navarro-Polanco, Aldo A, Rodríguez-Menchaca, Dora E, Benavides-Haro, José A, Sánchez-Chapula   +4 more
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Cocaine Blocks HERG, but Not KvLQT1+minK, Potassium Channels

Molecular Pharmacology, 2001
Cocaine causes cardiac arrhythmias, sudden death, and occasionally long QT syndrome in humans. We investigated the effect of cocaine on the human K(+) channels HERG and KvLQT1+minK that encode native rapidly (I(Kr)) and slowly (I(Ks)) activating delayed rectifier K(+) channels in the heart. HERG and KvLQT1+minK channels were heterologously expressed in
S, Zhang, S, Rajamani, Y, Chen, Q, Gong, Y, Rong, Z, Zhou, A, Ruoho, C T, January   +7 more
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Molecular determinants of hERG potassium channel inhibition by disopyramide

Journal of Molecular and Cellular Cardiology, 2012
The Class Ia antiarrhythmic drug disopyramide (DISO) causes QT interval prolongation that is potentially dangerous in acquired Long QT Syndrome but beneficial in short QT syndrome, through inhibition of the hERG-encoded channels responsible for rapid delayed rectifier K(+) current (I(Kr)).
El Harchi, A, Zhang, YH, Hussein, LK, Dempsey, CE, Hancox, JC   +4 more
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Prediction of hERG potassium channel affinity by the CODESSA approach

Bioorganic & Medicinal Chemistry, 2006
The problem of predicting torsadogenic cardiotoxicity of drugs is afforded in this work. QSAR studies on a series of molecules, acting as hERG K+ channel blockers, were carried out for this purpose by using the CODESSA program. Molecules belonging to the analyzed dataset are characterized by different therapeutic targets and by high molecular diversity.
Coi A, Massarelli I, Murgia L, Saraceno M, CALDERONE, VINCENZO, BIANUCCI, ANNA MARIA PAOLA   +5 more
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Modulation of HERG Potassium Channels by Extracellular Magnesium and Quinidine

Journal of Cardiovascular Pharmacology, 1999
Torsades de pointes is a polymorphic ventricular arrhythmia resulting from congenital or drug-induced (acquired) QT prolongation. Pharmacologic suppression of repolarizing potassium currents is one mechanism causing the acquired long QT (LQT) syndrome. Recent studies have linked mutations in a gene encoding a potassium channel subunit (HERG) to the LQT
S S, Po, D W, Wang, I C, Yang, J P, Johnson, L, Nie, P B, Bennett   +5 more
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