[HTML][HTML] hERG K+ channels: structure, function, and clinical significance

JI Vandenberg, MD Perry, MJ Perrin… - Physiological …, 2012 - journals.physiology.org
The human ether-a-go-go related gene (hERG) encodes the pore-forming subunit of the
rapid component of the delayed rectifier K+ channel, Kv11. 1, which are expressed in the …

Translational models and tools to reduce clinical trials and improve regulatory decision making for QTc and proarrhythmia risk (ICH E14/S7B updates)

DG Strauss, WW Wu, Z Li, J Koerner… - Clinical Pharmacology …, 2021 - Wiley Online Library
After multiple drugs were removed from the market secondary to drug‐induced torsade de
pointes (TdP) risk, the International Council for Harmonisation (ICH) released guidelines in …

Predicting new molecular targets for known drugs

MJ Keiser, V Setola, JJ Irwin, C Laggner, AI Abbas… - Nature, 2009 - nature.com
Although drugs are intended to be selective, at least some bind to several physiological
targets, explaining side effects and efficacy. Because many drug–target combinations exist …

Improving the in silico assessment of proarrhythmia risk by combining hERG (human ether-à-go-go-related gene) channel–drug binding kinetics and multichannel …

Z Li, S Dutta, J Sheng, PN Tran, W Wu… - Circulation …, 2017 - Am Heart Assoc
Background—The current proarrhythmia safety testing paradigm, although highly efficient in
preventing new torsadogenic drugs from entering the market, has important limitations that …

Targeting ion channels in cancer: a novel frontier in antineoplastic therapy

A Arcangeli, O Crociani, E Lastraioli… - Current medicinal …, 2009 - ingentaconnect.com
Targeted therapy is considerably changing the treatment and prognosis of cancer.
Progressive understanding of the molecular mechanisms that regulate the establishment …

The hERG potassium channel and hERG screening for drug-induced torsades de pointes

JC Hancox, MJ McPate, A El Harchi… - Pharmacology & …, 2008 - Elsevier
Drug-induced torsades de pointes (TdP) arrhythmia is a major safety concern in the process
of drug design and development. The incidence of TdP tends to be low, so early pre-clinical …

Physiological properties of hERG 1a/1b heteromeric currents and a hERG 1b-specific mutation associated with Long-QT syndrome

H Sale, J Wang, TJ O'Hara, DJ Tester… - Circulation …, 2008 - Am Heart Assoc
Cardiac I Kr is a critical repolarizing current in the heart and a target for inherited and
acquired long-QT syndrome (LQTS). Biochemical and functional studies have demonstrated …

Domperidone and risk of ventricular arrhythmia and cardiac death: a systematic review and meta-analysis

N Leelakanok, A Holcombe, ML Schweizer - Clinical drug investigation, 2016 - Springer
Abstract Background and Objective Domperidone is a drug used globally for relieving
nausea and vomiting and stimulating breast milk production. Several case reports and …

Drug binding to the inactivated state is necessary but not sufficient for high-affinity binding to human ether-a-go-go-related gene channels

MJ Perrin, PW Kuchel, TJ Campbell… - Molecular …, 2008 - ASPET
Drug block of the human ether-à-go-go-related gene K+ channel (hERG) is the most
common cause of acquired long QT syndrome, a disorder of cardiac repolarization that may …

Design, synthesis, and biological evaluation of a novel series of 1, 2, 4-oxadiazole inhibitors of SLACK potassium channels: Identification of in vitro tool VU0935685

MQ Alshaima'a, BD Spitznagel, Y Du… - Bioorganic & Medicinal …, 2023 - Elsevier
Malignant migrating partial seizure of infancy (MMPSI) is a devastating and
pharmacoresistant form of infantile epilepsy. MMPSI has been linked to multiple gain-of …