Development of safe drugs: the hERG challenge

S Kalyaanamoorthy, KH Barakat - Medicinal research reviews, 2018 - Wiley Online Library
Drug‐induced blockade of human ether‐a‐go‐go‐related gene (hERG) remains a major
impediment in delivering safe drugs to the market. Several drugs have been withdrawn from …

Potassium currents in the heart: functional roles in repolarization, arrhythmia and therapeutics

N Chiamvimonvat, Y Chen‐Izu… - The Journal of …, 2017 - Wiley Online Library
This is the second of the two White Papers from the fourth UC Davis Cardiovascular
Symposium Systems Approach to Understanding Cardiac Excitation–Contraction Coupling …

[HTML][HTML] Regulation of transport in the connecting tubule and cortical collecting duct

A Staruschenko - Comprehensive Physiology, 2012 - ncbi.nlm.nih.gov
The central goal of this overview article is to summarize recent findings in renal epithelial
transport, focusing chiefly on the connecting tubule (CNT) and the cortical collecting duct …

New potential binding determinant for hERG channel inhibitors

P Saxena, EM Zangerl-Plessl, T Linder, A Windisch… - Scientific Reports, 2016 - nature.com
Human ether-à-go-go related gene (hERG) 1 channels conduct the rapid delayed rectifier
K+ current (IKr) and are essential for the repolarization of the cardiac action potential …

In Silico Prediction of hERG Inhibition

Y **g, A Easter, D Peters, N Kim… - Future medicinal …, 2015 - Taylor & Francis
The voltage-gated potassium channel encoded by hERG carries a delayed rectifying
potassium current (IKr) underlying repolarization of the cardiac action potential …

Modeling of open, closed, and open-inactivated states of the hERG1 channel: structural mechanisms of the state-dependent drug binding

S Durdagi, S Deshpande, HJ Duff… - Journal of chemical …, 2012 - ACS Publications
The human ether-a-go-go related gene 1 (hERG1) K ion channel is a key element for the
rapid component of the delayed rectified potassium current in cardiac myocytes. Since there …

The ERG1 K+ Channel and Its Role in Neuronal Health and Disease

FG Sanchez-Conde, EN Jimenez-Vazquez… - Frontiers in Molecular …, 2022 - frontiersin.org
The ERG1 potassium channel, encoded by KCNH2, has long been associated with cardiac
electrical excitability. Yet, a growing body of work suggests that ERG1 mediates physiology …

A multiscale computational modelling approach predicts mechanisms of female sex risk in the setting of arousal‐induced arrhythmias

PC Yang, LL Perissinotti… - The Journal of …, 2017 - Wiley Online Library
Key points This study represents a first step toward predicting mechanisms of sex‐based
arrhythmias that may lead to important developments in risk stratification and may inform …

Assessing hERG1 blockade from Bayesian machine-learning-optimized site identification by ligand competitive saturation simulations

M Mousaei, M Kudaibergenova… - Journal of chemical …, 2020 - ACS Publications
Drug-induced cardiotoxicity is a potentially lethal and yet one of the most common side
effects with the drugs in clinical use. Most of the drug-induced cardiotoxicity is associated …

Utilizing Heteroatom Types and Numbers from Extensive Ligand Libraries to Develop Novel hERG Blocker QSAR Models Using Machine Learning-Based Classifiers

S Haddad, L Oktay, I Erol, K Sahin, S Durdagi - ACS omega, 2023 - ACS Publications
The human ether-à-go-go-related gene (hERG) channel plays a crucial role in membrane
repolarization. Any disruptions in its function can lead to severe cardiovascular disorders …