Pharmacological activation of the hERG K+ channel for the management of the long QT syndrome: A review
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Arrhythmia"
DOI: 10.1002/joa3.12741
Abstract: In the human heart, the rapid delayed rectifier K+ current (IKr) contributes significantly to ventricular action potential (AP) repolarization and to set the duration of the QT interval of the surface electrocardiogram (ECG). The pore‐forming… read more here.
Keywords: review; long syndrome; management; herg channel ... See more keywords
Modeling of the hERG K+ Channel Blockage Using Online Chemical Database and Modeling Environment (OCHEM)
Sign Up to like & getrecommendations! Published in 2017 at "Molecular Informatics"
DOI: 10.1002/minf.201700074
Abstract: Human ether‐a‐go‐go related gene (hERG) K+ channel plays an important role in cardiac action potential. Blockage of hERG channel may result in long QT syndrome (LQTS), even cause sudden cardiac death. Many drugs have been… read more here.
Keywords: herg channel; ochem; modeling environment; blockage ... See more keywords
Cryo-EM structure of K+-bound hERG channel complexed with the blocker astemizole.
Sign Up to like & getrecommendations! Published in 2020 at "Structure"
DOI: 10.1016/j.str.2020.12.007
Abstract: The hERG channel is a voltage-gated potassium channel involved in cardiac repolarization. Off-target hERG inhibition by drugs has become a critical issue in the pharmaceutical industry. The three-dimensional structure of the hERG channel was recently… read more here.
Keywords: herg channel; channel; channel complexed; structure ... See more keywords
Predicting hERG channel blockers with directed message passing neural networks
Sign Up to like & getrecommendations! Published in 2022 at "RSC Advances"
DOI: 10.1039/d1ra07956e
Abstract: Compounds with human ether-à-go-go related gene (hERG) blockade activity may cause severe cardiotoxicity. Assessing the hERG liability in the early stages of the drug discovery process is important, and the in silico methods for predicting… read more here.
Keywords: predicting herg; herg; message passing; channel blockers ... See more keywords
Molecular Insights Into the Gating Kinetics of the Cardiac hERG Channel, Illuminated by Structure and Molecular Dynamics
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2021.687007
Abstract: 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. The unique inward rectification characteristics of the hERG channel… read more here.
Keywords: herg channel; molecular dynamics; herg; cardiac herg ... See more keywords