hERG (the human Ether-à-go-go-Related Gene) is a gene that codes for a protein known as K v 11.1, the alpha subunit of a potassium ion channel. This ion channel (sometimes simply denoted as 'hERG') is best known for its contribution to the electrical activity of the heart : the hERG channel mediates the repolarizing I Kr current in the cardiac ...

Jun 1, 2020 · We provide in this concise review clear guidelines, based on described examples, illustrating successful optimization process to avoid hERG interactions as cases studies and to spur scientists to develop safe drugs.

The human ether-a-go-go-related gene (hERG) encodes the pore-forming subunit of the rapidly activating delayed rectifier potassium channel (IKr), which is important for cardiac repolarization. Dysfunction of hERG causes long QT syndrome and sudden ...

Based on ROC curves the optimal hERG margin thresholds to separate "Known risk of TdP" from "Not Listed" and, QTc prolongation positive from QTc negative were 37- and 50-fold, respectively.

Nov 24, 2014 · The human ether-à-go-go related gene (hERG) potassium channel is an obligatory anti-target for drug development on account of its essential role in cardiac repolarization and its close ...

Jun 1, 2020 · Early detection of hERG toxicity based on several practical tools is reviewed. hERG structure analysis offers new possibilities to predict detrimental binding. A guide for scientists involved in drug finding and development is provided.

Mar 22, 2006 · In this review we summarize the normal physiological functions of hERG channels, define the structural basis of their unusual gating and describe how mutations in the HERG gene or promiscuous...

Jan 24, 2020 · The human voltage-sensitive K + channel hERG plays a fundamental role in cardiac action potential repolarization, effectively controlling the QT interval of the electrocardiogram.

Nov 15, 1996 · Background The human ether-a-go-go–related gene (HERG) is one locus for the hereditary long-QT syndrome. A hypothesis is that HERG produces the repolarizing cardiac potassium current I Kr, with the consequence that mutations …

hERG is a tetrameric potassium channel formed by four subunits that are encoded by Kv11.1 (hERG). Voltage-dependent inactivation is caused by conformational changes in the outer mouth of the channel which is termed C-type inactivation. 1 This results in inward rectification.