Search Results - "Vandenberg, Jamie I."
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hERG K(+) channels: structure, function, and clinical significance
Published in Physiological reviews (01-07-2012)“…The human ether-a-go-go related gene (hERG) encodes the pore-forming subunit of the rapid component of the delayed rectifier K(+) channel, Kv11.1, which are…”
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Towards a Structural View of Drug Binding to hERG K+ Channels
Published in Trends in pharmacological sciences (Regular ed.) (01-10-2017)“…The human ether-a-go-go-related gene (hERG) K+ channel is of great medical and pharmaceutical relevance. Inherited mutations in hERG result in congenital…”
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3
Molecular Docking Guided Grid-Independent Descriptor Analysis to Probe the Impact of Water Molecules on Conformational Changes of hERG Inhibitors in Drug Trapping Phenomenon
Published in International journal of molecular sciences (10-07-2019)“…Human ether a-go-go related gene (hERG) or KV11.1 potassium channels mediate the rapid delayed rectifier current ( in cardiac myocytes. Drug-induced inhibition…”
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A New Perspective in the Field of Cardiac Safety Testing through the Comprehensive In Vitro Proarrhythmia Assay Paradigm
Published in Journal of biomolecular screening (01-01-2016)“…For the past decade, cardiac safety screening to evaluate the propensity of drugs to produce QT interval prolongation and Torsades de Pointes (TdP) arrhythmia…”
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Assessing drug safety by identifying the axis of arrhythmia in cardiomyocyte electrophysiology
Published in eLife (11-12-2023)“…Many classes of drugs can induce fatal cardiac arrhythmias by disrupting the electrophysiology of cardiomyocytes. Safety guidelines thus require all new drugs…”
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Potassium currents in the heart: functional roles in repolarization, arrhythmia and therapeutics
Published in The Journal of physiology (01-04-2017)“…This is the second of the two White Papers from the fourth UC Davis Cardiovascular Symposium Systems Approach to Understanding Cardiac Excitation–Contraction…”
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Development of automated patch clamp assays to overcome the burden of variants of uncertain significance in inheritable arrhythmia syndromes
Published in Frontiers in physiology (27-11-2023)“…Advances in next-generation sequencing have been exceptionally valuable for identifying variants in medically actionable genes. However, for most missense…”
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Potassium channels in the heart: structure, function and regulation
Published in The Journal of physiology (01-04-2017)“…This paper is the outcome of the fourth UC Davis Systems Approach to Understanding Cardiac Excitation–Contraction Coupling and Arrhythmias Symposium, a…”
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Structural basis of promiscuous substrate transport by Organic Cation Transporter 1
Published in Nature communications (11-10-2023)“…Organic Cation Transporter 1 (OCT1) plays a crucial role in hepatic metabolism by mediating the uptake of a range of metabolites and drugs. Genetic variations…”
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High-throughput discovery of trafficking-deficient variants in the cardiac potassium channel KV11.1
Published in Heart rhythm (01-12-2020)“…KCHN2 encodes the KV11.1 potassium channel responsible for IKr, a major repolarization current during the cardiomyocyte action potential. Variants in KCNH2…”
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Arrhythmogenic effects of ultra-long and bistable cardiac action potentials
Published in PLoS computational biology (01-02-2021)“…Contemporary accounts of the initiation of cardiac arrhythmias typically rely on after-depolarizations as the trigger for reentrant activity. The…”
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Potassium dependent structural changes in the selectivity filter of HERG potassium channels
Published in Nature communications (29-08-2024)“…The fine tuning of biological electrical signaling is mediated by variations in the rates of opening and closing of gates that control ion flux through…”
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Development of a robust induced pluripotent stem cell atrial cardiomyocyte differentiation protocol to model atrial arrhythmia
Published in Stem cell research & therapy (27-07-2023)“…Atrial fibrillation is the most common arrhythmia syndrome and causes significant morbidity and mortality. Current therapeutics, however, have limited…”
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Domain Reorientation and Rotation of an Intracellular Assembly Regulate Conduction in Kir Potassium Channels
Published in Cell (11-06-2010)“…Potassium channels embedded in cell membranes employ gates to regulate K + current. While a specific constriction in the permeation pathway has historically…”
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R222Q SCN5A Mutation Is Associated With Reversible Ventricular Ectopy and Dilated Cardiomyopathy
Published in Journal of the American College of Cardiology (16-10-2012)“…Objectives The goal of this study was to characterize a variant in the SCN5A gene that encodes the alpha-subunit of the cardiac sodium channel, Nav1.5, which…”
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Multiple Interactions between Cytoplasmic Domains Regulate Slow Deactivation of Kv11.1 Channels
Published in The Journal of biological chemistry (12-09-2014)“…The intracellular domains of many ion channels are important for fine-tuning their gating kinetics. In Kv11.1 channels, the slow kinetics of channel…”
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Reduced connexin-43 expression, slow conduction and repolarisation dispersion in a model of hypertrophic cardiomyopathy
Published in Disease models & mechanisms (01-08-2024)“…Hypertrophic cardiomyopathy (HCM) is an inherited heart muscle disease that is characterised by left ventricular wall thickening, cardiomyocyte disarray and…”
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Experimentally Validated Pharmacoinformatics Approach to Predict hERG Inhibition Potential of New Chemical Entities
Published in Frontiers in pharmacology (19-09-2018)“…The hERG (human ether-a-go-go-related gene) encoded potassium ion (K ) channel plays a major role in cardiac repolarization. Drug-induced blockade of hERG has…”
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Drug binding to the inactivated state is necessary but not sufficient for high-affinity binding to human ether-à-go-go-related gene channels
Published in Molecular pharmacology (01-11-2008)“…Drug block of the human ether-à-go-go-related gene K(+) channel (hERG) is the most common cause of acquired long QT syndrome, a disorder of cardiac…”
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The diagnostic role of T wave morphology biomarkers in congenital and acquired long QT syndrome: A systematic review
Published in Annals of noninvasive electrocardiology (01-01-2023)“…Introduction QTc prolongation is key in diagnosing long QT syndrome (LQTS), however 25%–50% with congenital LQTS (cLQTS) demonstrate a normal resting QTc. T…”
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