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
Molecular Insights Into the Gating Kinetics of the Cardiac hERG Channel, Illuminated by Structure and Molecular Dynamics [PDF]
Frontiers in Pharmacology, 2021 The rapidly activating delayed rectifier K+ current generated by the cardiac hERG potassium channel encoded by KCNH2 is the most important reserve current for cardiac repolarization.
Zheng Zequn, Lian Jiangfang
doaj +2 more sources
Data on the construction of a recombinant HEK293 cell line overexpressing hERG potassium channel and examining the presence of hERG mRNA and protein expression [PDF]
Data in Brief, 2017 The data presented in this article are related to the research article entitled “The effects of deoxyelephantopin on the cardiac delayed rectifier potassium channel current (IKr) and human ether-a-go-go-related gene (hERG) expression” (Y.F.
Yi Fan Teah +5 more
doaj +4 more sources
AttenhERG: a reliable and interpretable graph neural network framework for predicting hERG channel blockers [PDF]
Journal of CheminformaticsCardiotoxicity, particularly drug-induced arrhythmias, poses a significant challenge in drug development, highlighting the importance of early-stage prediction of human ether-a-go-go-related gene (hERG) toxicity.
Tianbiao Yang +7 more
doaj +2 more sources
Reassessing the Conduct of Patch Clamp Cardiac Ion Channel Assays to Improve Nonclinical Data Translation to Clinical ECG Changes and Proarrythmia Risk [PDF]
Clinical and Translational ScienceThe Comprehensive in vitro Proarrhythmia Assay (CiPA) initiative proposes integrating multi‐cardiac ion channel pharmacology to improve the prediction of drug‐induced Torsade de Pointes (TdP) risk.
Claudia Alvarez Baron +6 more
doaj +2 more sources
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
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
Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin. [PDF]
PLoS ONE, 2013 Treatment of LQT2 is inadequate. Many drugs which can pharmacologically rescue defective protein trafficking in LQT2 also result in potent blockade of HERG current, negating their therapeutic benefit.
Haiyan Mao +9 more
doaj +1 more source
Frontiers in Molecular Biosciences, 2021 Three environment-sensitive probes were developed for the hERG channel based on the nitrobenzoxadiazole fluorophore herein. After careful evaluation, probes M1 and M3 were found to have a high affinity for imaging the hERG channel in the cell-based ...
Qi Li +4 more
doaj +1 more source
Structural modeling of the hERG potassium channel and associated drug interactions
Frontiers in Pharmacology, 2022 The voltage-gated potassium channel, KV11.1, encoded by the human Ether-à-go-go-Related Gene (hERG), is expressed in cardiac myocytes, where it is crucial for the membrane repolarization of the action potential.
Jan Maly +12 more
doaj +1 more source