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KCNH2 activates potassium(1+). 56 / 56
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"HERG encodes the core subunit of a K+ channel and mediates a cardiac delayed-rectifier K+ current, II ~ critical to myocardial action potential repolarization (Fig 1B, phase 3)."
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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]."
23519576
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"However, ivabradine also inhibits human ether-a-go-go (hERG) mediated potassium currents."
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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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"BmKDfsin5 (1 μM) was found to inhibit the potassium currents mediated by Kv1.1, Kv1.2, Kv1.3, IK, SK3 and hERG channels by approximately 8.7%, 10.2%, 9.0%, 9.1%, 46.3% and 16.9%, respectively ( Fig. 5[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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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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"When applied to the WTC and SCVI20 recordings (Fig. 6), these analyses predicted enhancement of the rapid delayed rectifier potassium current I (hERG) in WTC (Fig. 6D), which would directly contribute to the observed APD shortening."
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"The hERG channel contributes to repolarization of the cardiac action potential by selectively allowing potassium ions to flow out of the cell following depolarization [2]."
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"Inhibition of the potassium channel encoded by the human ether-a-go-go-related gene (HERG) KCNH2 , which mediates the potassium current I Kr , was indicated as a primary correlate with drug-induced ar[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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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."
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"In addition, high glucose decreases hERG channel expression, which in turn modulates the delayed rectifier potassium current IKr, another factor responsible for QT prolongation in diabetes [36, 37]."
39427200
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"In our study, we found that ethanol could inhibit hKv1.5 currents in a concentration-dependent manner, which might lead to the prolongation of atrial APD to generate preventive effect on AF.Rapid dela[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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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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"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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"(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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"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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"HERG (human Ether-a-go-go Related Gene)-encoded potassium channels underlie the cardiac rapid delayed rectifier (I Kr ) potassium current, which is a major target for antiarrhythmic agents and diverse non-cardiac drugs linked to the drug-induced form of long QT syndrome."
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"Data from all experiments were analyzed using non-linear curve fitting programs and results are given as K i values for binding affinity or K b values for antagonist potency.Blockade of hERG-mediated [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The most frequently observed forms of congenital LQTS arise from mutations to KCNQ1 and hERG (alternative nomenclature KCNH2), which respectively contribute to the slow delayed rectifier potassium current (I , LQT1) and the rapid delayed rectifier potassium current (I , LQT2); these account for 44% and 35% of cases, respectively [9]."
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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)."
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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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"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]"
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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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"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]."
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"One micromolar BmKDfsin3 inhibited the potassium ion currents mediated by Kv1.1, Kv1.2, Kv1.3, IK, SK3 and hERG channels by approximately 57.0%, 27.5, 84.3%, 15.1%, 87.5% and 30.4%, respectively ( Fig[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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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]."
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"In the heart, kratom inhibits hERG-mediated K+ currents and prolongs action duration, constituting a major risk of cardiotoxicity due to blockage of the human Ether-a-go-go-Related Gene (hERG) channel [137]."
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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]."
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"21 The IC values for the rapid component of the delayed rectifier potassium current mediated by hERG K channels are considerably lower (2–8 μM for CQ and 3–10 μM for HCQ).21,52,61,62 However, the sole validity of IC values for predicting proarrhythmic risks due to inhibition of hERG K channels have been challenged, noting that they do not account for dynamic time- and state-dependent drug–channel interactions."
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"Although pharmacological activation of K ATP channels has shown more anti-arrhythmic than pro-arrhythmic potential in several studies the profile of hERG1 channel activators can be hypothesized to be [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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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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"The large inner cavity of the hERG K + channels allows several molecules to enter and prevent potassium conduction denoting unique properties that make them an important, “promiscuous” drug binding si[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The most common type of LQTS, LQT2, is caused by mutations in the hERG gene, affecting a potassium ion channel."
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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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"HERG current increased in direct proportion to [K+] e, although the shape of the I-V relationship was not altered."
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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 may be related to clofazimine as a potent inhibitor of hERG potassium channel signaling, which mediates repolarization of the delayed rectifier potassium current, IKr, in the cardiac action potential."
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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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"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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"The potent hERG channel inhibition by non-cardiovascular medications could trigger the blockade of rapid delayed rectifier potassium current (IKr), leading to the drug-induced QT interval prolongation[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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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."
26044252
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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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"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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"Interestingly, however, inhibition of 86 Rb uptake in non-cancerous MCF-10A cells by dofetilide may suggest that inhibition of hERG reduces the rate of potassium exit causing the cell to suppress acti[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
23639630
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"Olanzapine, a thienobenzodiazepine derivative antipsychotic agent mainly metabolised via CYP1A2 and CYP2D6 isoenzymes, exhibits very low binding affinity for human ether-a-go-go-related gene (HERG) me[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
15935493
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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."
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"SP1 has been identified as a counter-activator of the hERG gene, upregulating hERG expression and activating the potassium ion channel [77]."
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"Type-2 LQTS patients’ iPSC-derived cardiomyocytes showed that a mutation in KCNH2 causes action-potential-duration prolongation by reducing the cardiac potassium current IKr and dysfunction of the sodium ion channel [7,8,9]."
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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 channel mediates the delayed rectifier potassium current, which is essential for cardiac repolarization."
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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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"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."
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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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"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]."
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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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"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."
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