Search Results - "Mitcheson, John S"
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hERG Potassium Channels and the Structural Basis of Drug-Induced Arrhythmias
Published in Chemical research in toxicology (01-05-2008)“…hERG potassium channels have a critical role in the normal electrical activity of the heart. The block of hERG channels can cause the drug-induced form of long…”
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2
A mechanism for CO regulation of ion channels
Published in Nature communications (02-03-2018)“…Despite being highly toxic, carbon monoxide (CO) is also an essential intracellular signalling molecule. The mechanisms of CO-dependent cell signalling are…”
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A heme-binding domain controls regulation of ATP-dependent potassium channels
Published in Proceedings of the National Academy of Sciences - PNAS (05-04-2016)“…Heme iron has many and varied roles in biology. Most commonly it binds as a prosthetic group to proteins, and it has been widely supposed and amply…”
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Molecular determinants of HERG channel block
Published in Molecular pharmacology (01-05-2006)“…Drug-induced block of cardiac hERG K+ channels causes acquired long QT syndrome. Here, we characterized the molecular mechanism of hERG block by two…”
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hERG potassium channel blockade by the HCN channel inhibitor bradycardic agent ivabradine
Published in Journal of the American Heart Association (24-04-2015)“…Ivabradine is a specific bradycardic agent used in coronary artery disease and heart failure, lowering heart rate through inhibition of sinoatrial nodal…”
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6
A Structural Basis for Drug-Induced Long QT Syndrome
Published in Proceedings of the National Academy of Sciences - PNAS (24-10-2000)“…Mutations in the HERG K+channel gene cause inherited long QT syndrome (LQT), a disorder of cardiac repolarization that predisposes affected individuals to…”
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7
Drug block of the hERG potassium channel: Insight from modeling
Published in Proteins, structure, function, and bioinformatics (01-08-2007)“…Many commonly used, structurally diverse, drugs block the human ether‐a‐go‐go‐related gene (hERG) K+ channel to cause acquired long QT syndrome, which can lead…”
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Author Correction: A mechanism for CO regulation of ion channels
Published in Nature communications (17-08-2018)“…The originally published version of this article contained an error in the subheading ‘Heme is required for CO-dependent channel activation’, which was…”
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Drug binding to HERG channels: evidence for a ‘non‐aromatic’ binding site for fluvoxamine
Published in British journal of pharmacology (01-07-2003)“…British Journal of Pharmacology (2003) 139, 883–884. doi:10.1038/sj.bjp.0705336…”
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Drug binding interactions in the inner cavity of HERG channels: molecular insights from structure-activity relationships of clofilium and ibutilide analogs
Published in Molecular pharmacology (01-02-2006)“…Block of human ether-a-go-go related gene (hERG) K(+) channels by otherwise useful drugs is the most common cause of long QT syndrome, a disorder of cardiac…”
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Trapping of a methanesulfonanilide by closure of the HERG potassium channel activation gate
Published in The Journal of general physiology (01-03-2000)“…Deactivation of voltage-gated potassium (K(+)) channels can slow or prevent the recovery from block by charged organic compounds, a phenomenon attributed to…”
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12
The S4-S5 Linker Couples Voltage Sensing and Activation of Pacemaker Channels
Published in Proceedings of the National Academy of Sciences - PNAS (25-09-2001)“…Voltage-gated channels are normally opened by depolarization and closed by repolarization of the membrane. Despite sharing significant sequence homology with…”
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13
Modulation of hERG potassium channels by a novel small molecule activator
Published in British journal of pharmacology (01-10-2017)Get full text
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14
Mechanistic Insight into Human ether-à-go-go-related Gene (hERG) K+ Channel Deactivation Gating from the Solution Structure of the EAG Domain
Published in The Journal of biological chemistry (25-02-2011)“…Human ether-à-go-go-related gene (hERG) K+ channels have a critical role in cardiac repolarization. hERG channels close (deactivate) very slowly, and this is…”
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Predicting drug–hERG channel interactions that cause acquired long QT syndrome
Published in Trends in pharmacological sciences (Regular ed.) (01-03-2005)“…Avoiding drug-induced cardiac arrhythmia is recognized as a major hurdle in the successful development of new drugs. The most common problem is acquired long…”
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Discovery of a heme-binding domain in a neuronal voltage-gated potassium channel
Published in The Journal of biological chemistry (18-09-2020)“…The EAG (ether-à-go-go) family of voltage-gated K+ channels are important regulators of neuronal and cardiac action potential firing (excitability) and have…”
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A Novel Mechanism for Calmodulin-Dependent Inactivation of Transient Receptor Potential Vanilloid 6
Published in Biochemistry (Easton) (08-05-2018)“…The paralogues TRPV5 and TRPV6 belong to the vanilloid subfamily of the transient receptor potential (TRP) superfamily of ion channels, and both play an…”
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Correction: Discovery of a heme-binding domain in a neuronal voltage-gated potassium channel
Published in The Journal of biological chemistry (01-03-2022)Get full text
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New pyrimido-indole compound CD-160130 preferentially inhibits the KV11.1B isoform and produces antileukemic effects without cardiotoxicity
Published in Molecular pharmacology (01-02-2015)“…KV11.1 (hERG1) channels are often overexpressed in human cancers. In leukemias, KV11.1 regulates pro-survival signals that promote resistance to chemotherapy,…”
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Calmodulin Regulates Human Ether à Go-Go 1 (hEAG1) Potassium Channels through Interactions of the Eag Domain with the Cyclic Nucleotide Binding Homology Domain
Published in The Journal of biological chemistry (19-08-2016)“…The ether à go-go family of voltage-gated potassium channels is structurally distinct. The N terminus contains an eag domain (eagD) that contains a…”
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