IndraLab

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Potassium(1+) inhibits KCNH2. 11 / 12
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"HERG Potassium Channel Inhibition."
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"This ion channel plays an important role in the repolarization phase of the cardiac action potential by mediating the rapid component of cardiac delayed rectifier K+ current.31,32 The most common mechanism of drug-induced QT prolongation is due to hERG inhibition.33,34 Several antitubercular agents and repurposed COVID-19 drugs have been reported to inhibit hERG and result in QT interval prolongation.35–38 Hence, there is an increased potential for DDIs due to QT prolongation."
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"These results demonstrate that [K+] o does not directly modulate drug block of hERG channels expressed in an HEK-293 cell line."
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"We have addressed whether some of the beta-adrenoceptor blockers commonly used to prevent the development of these arrhythmias could per se block the cardiac HERG (Human Ether-a-go-go-Related Gene) potassium channels, which would be a most unwanted side effect."
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"The other exciting feature of adding methyl group at the R 5 position was the elimination of hERG K+ channel inhibition ( 7 vs 3a and 37 vs 3v ), which was observed in early analogs ( 3a and 3v ) and was a major liability for the cores having a bridgehead nitrogen atom, such as imidazo[1,2- a ]pyridine ( 3a and 3v ), 1,2,4-triazolo[4,3- a ]pyridine ( 34 ) and imidazo[1,2- a ]pyrimidine ( 31 )."
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"The hERG potassium ion channel inhibition and analysis of this process is the basis in pharmacological safety research of new drugs beceause inhibition of this channel may lead for example to arrhythmia, which may occasionally have fatal results due to subsequent ventricular fibrillation [ xref ]."
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"As first reported by Guo and colleagues, low-extracellular potassium causes degradation of the 155 kD form of HERG through an endocytic mechanism involving mono-ubiquitination."
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"Prioritized analogs exhibiting EC 50 s ≤ 4 nM against all tested pseudotyped viruses and having optimal MLM metabolic stability profiles, as well as a lack of hERG K+ channel inhibition ( 7 , 35 , 37 , 38 , 39 , and 40 ), were selected for further advancement and evaluated for efficacy in replicative LASV plaque assay and LASV and JUNV viral yield reduction (VYR) assays ( xref )."
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"Our device was also tested for its response with E-4031, which is a potassium ion channel blocker of the HERG channel and is known to cause prolongation of QT interval without any effect on contraction force."
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"Secondly, low extracellular potassium can also increase the blockade of hERG currents by drugs [XREF_BIBR, XREF_BIBR]."
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"The lack of hERG K+ channel inhibition for a number of tested compounds suggests favorable potential for cardiac safety."
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