Structural modeling of hERG channel–drug interactions using Rosetta [PDF]
Frontiers in Pharmacology, 2023 The human ether-a-go-go-related gene (hERG) not only encodes a potassium-selective voltage-gated ion channel essential for normal electrical activity in the heart but is also a major drug anti-target.
Aiyana M. Emigh Cortez +17 more
doaj +2 more sources
The Effect of a Synthetic Estrogen, Ethinylestradiol, on the hERG Block by E-4031 [PDF]
Biomolecules, 2021 Inhibition of K+-conductance through the human ether-a-go-go related gene (hERG) channel leads to QT prolongation and is associated with cardiac arrhythmias.
Fumiya Tamura +8 more
doaj +2 more sources
In vitro chronic effects on hERG channel caused by the marine biotoxin Yessotoxin.
Frontiers in Marine Science, 2014 INTRODUCTION Marine algal blooms caused by the overgrowth of marine phytoplankton have increased in frequency and severity in the last years; supposing a worldwide public health problem.
Sara Fernández Ferreiro
doaj +2 more sources
Integrating drug effects on individual cardiac ionic currents and cardiac action potentials to understand nonclinical translation to clinical ECG changes [PDF]
Frontiers in PharmacologyConcomitant inhibition of the late Na+ current (INaL) and/or the L-type Ca2+ current (ICaL) has been hypothesized to mitigate hERG block-mediated QTC prolongation.
Lars Johannesen +7 more
doaj +2 more sources
Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices [PDF]
Scientific ReportsAcute block of hERG channels is the most common mechanism underlying drug-induced QTC prolongation and potentially fatal Torsade de Pointes arrhythmia. Updates to ICH E14 Q&As now allow for using negative nonclinical data, including hERG, to support QTC ...
Claudia Alvarez Baron +25 more
doaj +2 more sources
Hydroxychloroquine induces long QT syndrome by blocking hERG channel
Frigid Zone Medicine, 2023 In March 2022, more than 600 million cases of Corona Virus Disease 2019 (COVID-19) and about 6 million deaths have been reported worldwide. Unfortunately, while effective antiviral therapy has not yet been available, chloroquine (CQ)/hydroxychloroquine ...
Zhao Xin +10 more
doaj +1 more source
Up-regulation of hERG K⁺ channels by B-RAF. [PDF]
PLoS ONE, 2014 Human ether-a-go-go related-gene K⁺ channels (hERG) participate in the regulation of tumor cell proliferation and apoptosis. HERG channel activity is up-regulated by growth factors.
Tatsiana Pakladok +6 more
doaj +1 more source
Hysteretic hERG channel gating current recorded at physiological temperature
Scientific Reports, 2022 Cardiac hERG channels comprise at least two subunits, hERG 1a and hERG 1b, and drive cardiac action potential repolarization. hERG 1a subunits contain a cytoplasmic PAS domain that is absent in hERG 1b.
David K. Jones
doaj +1 more source
Inhibitory effects and mechanism of dihydroberberine on hERG channels expressed in HEK293 cells. [PDF]
PLoS ONE, 2017 The human ether-a-go-go-related gene (hERG) potassium channel conducts rapid delayed rectifier potassium currents (IKr) and contributes to phase III cardiac action potential repolarization.
Dahai Yu +8 more
doaj +1 more source
hERG-deficient human embryonic stem cell-derived cardiomyocytes for modelling QT prolongation
Stem Cell Research & Therapy, 2021 Background Long-QT syndrome type 2 (LQT2) is a common malignant hereditary arrhythmia. Due to the lack of suitable animal and human models, the pathogenesis of LQT2 caused by human ether-a-go-go-related gene (hERG) deficiency is still unclear.
Yun Chang +13 more
doaj +1 more source