[HTML][HTML] hERG K+ channels: structure, function, and clinical significance
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 …
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 …
pointes (TdP) risk, the International Council for Harmonisation (ICH) released guidelines in …
Predicting new molecular targets for known drugs
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 …
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 …
Background—The current proarrhythmia safety testing paradigm, although highly efficient in
preventing new torsadogenic drugs from entering the market, has important limitations that …
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 …
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 …
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 …
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 …
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
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 …
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 …
pharmacoresistant form of infantile epilepsy. MMPSI has been linked to multiple gain-of …