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KCNH2 inhibits potassium(1+). 25 / 25
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"The acquired form of LQTS is far more prevalent than the congenital form and is predominantly related to the use of drugs blocking the human ether-a-go–go-related gene (hERG) potassium channel, thereby reducing the rapid component of the delayed rectifier potassium current I [3]."
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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]."
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"CMX-2043 produced no inhibition of hERG mediated potassium current at its limit of solubility (3000muM; 1220mug/mL) when assessed using whole-cell patch-clamp electrophysiological methods."
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"The activity of hERG1 potassium channels, which contributes to the outward K + currents and underlies the long QT syndrome when mutated, was found to be significantly inhibited during mild oxidative s[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The intracellular face of the hERG channel is large and is lined with a number of aromatic residues allowing drugs like CQ and HCQ and others to bind this part of the channel and block the outward potassium current57,67."
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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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"A half-maximal inhibiting concentration (IC value) for the effect of Aspidasept on the hERG-mediated potassium current could not be calculated, because no significant effect on the hERG channel current at the highest concentration successfully tested (10 µg/mL) could be observed (Figure 8)."
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"A Hodgkin-Huxley-style cardiac ionic model captured the different types of complex dynamics following blockage of the hERG mediated potassium current."
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"Mutations in the KCNH2 gene decrease the current of potassium ions per channel, and thus lengthen the action potential in cardiomyocytes and neurons [51]."
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"The proarrhythmogenic effect is also caused by the interaction of PTX with HERG K channels (human ether-a-go-go), which causes a rapid decrease in the influx of potassium into the cardiomyocytes and causes a prolongation of the QT interval [116]."
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"Of note, inhibition of different isoforms of hERG-mediated potassium currents was described at concentrations between 2.07 μM and 3.31 μM [5] ."
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"Based on these studies, in particular the inhibition of hERG-mediated potassium currents most likely explains the antiarrhythmic effect of AF observed in the present study.The present study demonstrat[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"At 10 µM, aconitine, 14-benzoylaconine 8- O-palmitate, songoramine, gigactonine and neolinine demonstrated significant hERG K+ channel inhibition; all other compounds exerted only low (6-21%) inhibitory activity."
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"In vitro studies found that supratherapeutic circulating concentration of loperamide is an effective inhibitor of both NaV1.5 and potassium human ether-a-go-go related gene (hERG) cardiac ion channels, with consequences on ventricular arrhythmogenesis and function.We recently performed an analysis of the World Health Organization pharmacovigilance database (VigiBase), encompassing more than 22 million reports from more than 130 countries."
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"Lowering the extracellular potassium concentration ([K +] o) decreases the magnitude of I Kr and of outward HERG K + currents."
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"Moxifloxacin is a selective blocker of hERG-mediated potassium current and causes a prolongation of QT in the ECG."
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"Ng and colleagues at the Cardiological Society of Australia and New Zealand (CSANZ) annual meeting presented their data on IC-105574, a hERG channel activator which was shown to attenuate inactivation of the potassium (K) channel in Chinese hamster ovarian cell lines with inactivator mutations [2]."
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"Minimal Inhibition of hERG-mediated K+ current in HEK293 cells was observed at 3 μM ( Table 2 )."
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"Pharmacokinetic properties, druglikeness as well as other significant descriptors, such as molecular weight, H-bond donors, H-bond acceptors, solvent accessible surface area, log HERG (blockage of K+ channels), log S (aqueous solubility), log P (octanol and water), and human oral absorption, for the selected hits were determined by QikProp (XREF_TABLE)."
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"However, compared to other inward rectifiers which block potassium conductance via an intracellular polyamine block, HERG channels prevent potassium outflow by rapid inactivation."
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"Class III (HERG channel-mediated rapid potassium current blockers) D, L-sotalol is generally avoided in frail patients with multiple comorbidities, polypharmacy, and frequent electrolytes disorders, but may be used in selected patients, more commonly for ventricular arrhythmias, if certain provision is followed such as QT interval monitoring and ensuing there is no significant left ventricular hypertrophy."
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"Cardiac toxicity was based on the hERG model, which predicts whether the compound blocks the hERG K+ channel or not."
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"The mechanisms by which these three drugs inhibit potassium channels, hERG in particular, have been studied previously and involve direct block of the pore via the intracellular vestibule and are coordinated by aromatic side-chains, such as phenylalanine."
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"HERG1 channel subunit composition mediates proton inhibition of rapid delayed rectifier potassium current (I Kr ) in cardiomyocytes derived from hiPSCs."
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"Computer calculations were performed using pharmacokinetic and pharmacodynamic data, including affinity to block the rapid component of the delayed rectifier cardiac potassium current (I Kr) encoded by the human ether-a-go-go gene (hERG), propensity to prolong cardiac repolarization (QT interval) and cause torsade de pointes (TdP)."
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