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KCNH2 activates potassium(1+). 38 / 38
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"However, ivabradine also inhibits human ether-a-go-go (hERG) mediated potassium currents."
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"For these reasons we and others have attempted to define the functional role for HERG mediated K+ currents in repolarization of the action potential in the human ventricle."
17919688
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"Due to the presence of this characteristic PY motif, we investigated whether the potassium current mediated by hERG1 (I hERG1) is regulated by the ubiquitin ligase Nedd4-2, as it has been observed for[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
21463633
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"We investigated the effects of DW-224a on the human ether-a-go-go-related gene (hERG) mediated potassium currents to evaluate its potential to induce QT interval prolongation."
15573468
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"Inhibition of hERG channels will reduce the potassium efflux during repolarization, and will result in an increase in human cardiac AP duration, concomitantly leading to a prolongation of the QT interval (XREF_FIG) [XREF_BIBR]."
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"The human ether-a-go-go-related gene (hERG) channel mediates the rapid delayed rectifier potassium current (IKr) responsible for shaping the repolarization phase of cardiac action potentials."
25947924
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"HERG (human Ether-a-go-go Related Gene) is responsible for ion channels mediating rapid delayed rectifier potassium current, I Kr, which is key to cardiac action potential repolarization."
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"Paroxysmal atrial fibrillation (AF) can be caused by gain-of-function mutations in genes, encoding the cardiac potassium channel subunits KCNJ2, KCNE1, and KCNH2 that mediate the repolarizing potassium currents I k1, I ks, and I kr, respectively."
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"The HERG mediated potassium and the SCN5A mediated sodium currents, however, were only slightly reduced by estradiol at concentrations of up to 30 microM."
16480714
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"The site mutation (p.N588K) in KCNH2 increases the expression of HERG channels and thus enhances outward potassium current, shortens action potential duration, and promotes proarrhythmic activity in short QT-syndrome-cardiomyocytes."
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"The hERG channel mediates the rapid delayed rectifier potassium current (I Kr) and can be overexpressed in HEK293 (Human Embryonic Kidney 293) or CHO (Chinese Hamster Ovary) cell lines."
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"HERG current increased in direct proportion to [K+] e, although the shape of the I-V relationship was not altered."
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"Interestingly and in contrast to previous studies, when expressed in Xenopus oocytes, the interaction between Sig-1Rs and hERG channels resulted in increased hERG mediated K+ currents -- a mechanism that seemed to occur through a regulation of channels subunits maturation and stability [XREF_BIBR]."
23102998
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"The hERG channel mediates the delayed rectifier potassium current, which is essential for cardiac repolarization."
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"As blockade of the human Ether-a-go-go-Related Gene (hERG)-mediated potassium current is the most common mechanism of drug induced prolongation of the myocardial action potential and QT-interval prolongation, data showing that dabigatran did not modify the hERG mediated potassium current in human embryonic kidney cells agree with the previously mentioned pre-clinical results [XREF_BIBR]."
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"Of these, the Kv11.1 (hERG, KCNH2) channel mediates the cardiac potassium current IKr, involved in the repolarization of the cardiac action potential and playing a crucial role to prevent arrhythmias induced by early after depolarizations or ectopic beats, such that mutations in Kv11.1 lead to inherited type 2 long QT syndrome."
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"This variant has subsequently been shown to slow I Ks potassium channel, when studied in Xenopus oocytes [XREF_BIBR], and to exhibit significant loss-of-function effects on both the KCNQ1- and KCNH2 mediated potassium currents, as measured in Chinese hamster ovarian cells [XREF_BIBR]."
21244686
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"Isavuconazole simultaneously blocks hERG mediated potassium and the L-type calcium channels in the myocardium thereby shortening, as opposed to lengthening, the QTc interval [XREF_BIBR, XREF_BIBR]."
33499209
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"HERG mediates the cardiac delayed rectifier potassium current I Kr and mutations in the hERG gene and drug inhibition of hERG channels underlie inherited and acquired type 2 long-QT syndrome."
22470342
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"The majority of drug induced arrhythmias are related to the prolongation of action potential duration following inhibition of rapidly activating delayed rectifier potassium current (I (Kr)) mediated by the hERG channel."
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"XREF_BIBR, XREF_BIBR The hERG potassium channel underlies the delayed rectifier potassium current (I Kr), and is the most common potassium channel associated with drug induced QT prolongation."
31911979
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"Fluoxetine, a commonly used antidepressant, was reported to block the currents of several potassium channels, which are mediated by Kv1.1, Kv1.3, Kv1.4, Kv1.5, Kv3.1, Kv4.3, hERG and TREK-1 XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR."
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"KCNH2 variants associated with lone AF have been characterized by slower deactivation and increased repolarizing potassium current with no QTc prolongation observed in affected subects."
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"KCNH2 mediates the rapid activation of delayed rectifier potassium current (IKr), which is important for normal ventricular repolarization [XREF_BIBR]."
32565909
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"Lacosamide was tested in vitro on sodium and L-type calcium currents from isolated human atrial myocytes and on hERG mediated potassium currents from stably transfected HEK293 cells."
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"The hERG (or “Kv11.1”) potassium channel (encoded by human Ether-à-go-go Related Gene; alternative nomenclature KCNH2) mediates the rapid component of cardiac delayed rectifier K+ current (also known as IKr)."
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"This includes (1) testing for blockade of I (Kr) or hERG mediated potassium current in heterologous cell systems, (2) measurement of effects on the myocardial action potential in vitro; and (3) assessment of effects on the ECG in a well conducted in vivo study."
15172012
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"In general, drug induced QTc prolongation is the result of an intrinsic ability to block cardiac hERG mediated potassium channels resulting in delayed cardiac repolarization and/or mechanisms which increase the exposure of co-administered QTc prolonging drugs [XREF_BIBR]."
33499209
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"In vitro and animal studies with empagliflozin demonstrated no relevant interactions with the hERG mediated potassium current and no effect on action potentials (unpublished data)."
23617452
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"In addition to I to, f and I Kur, human atrial myocytes also exhibit a rapidly activating and inactivating current (I Kr) and a slowly activating current (I Ks), mediated by hERG1 and KCNQ1 channels, respectively, but they are much smaller outward potassium currents relative to I to, f and I Kur [XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR]."
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"In humans, the delayed rectifier potassium current is mediated by the ion channel KCNH2 encoded by the human ether-a-go-go-related gene (HERG) [XREF_BIBR]."
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"(A) Expression of HERG channels in Xenopus oocytes induced K+ channels with characteristic properties, i.e. fast inactiva- tion at positive potentials and large, slowly decaying tail cur- rents upon r[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
9315735
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"Human ether-a-go-go-related gene (HERG) subunits mediate a K+ current that is required for normal repolarization of the cardiac action potential."
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"Attenuation of repolarizing K+ current caused by mutations in HERG or channel block by common medications prolongs ventricular action potentials and increases the risk of arrhythmia and sudden death."
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"Raising the extracellular potassium to 10 mmol/l, HERG block by azimilide, dofetilide, quinidine and sotalol was significantly decreased, while the block by amiodarone was unchanged."
16960444
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"System specific maximal achievable Delta QTc was estimated to 28% from baseline in both dog and human, while% hERG block leading to half-maximal effects was 58% lower in human, suggesting a higher contribution of hERG mediated potassium current to cardiac repolarization."
28097003
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"At 1M concentration testosterone decreased the amplitude of HERG directed IKr (rapid component of cardiac delayed rectifier K+ current) by 30% within 30 min of exposure, while 17-estradiol had no effect."
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"A hypothesis is that HERG produces the repolarizing cardiac potassium current IKr with the consequence that mutations in HERG prolong the QT interval by reducing IKr."
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