Results 271 to 280 of about 36,434 (294)

Effects of fluoroquinolones on HERG currents

European Journal of Pharmacology, 2000
We have investigated the effects of four fluoroquinolones on the human ether-à-go-go-related gene (HERG) mediated K(+) currents to evaluate their potential to induce QT-prolongation. HERG currents were measured from stably transfected Chinese hamster ovary (CHO) cells by means of the patch-clamp technique. Bath application of sparfloxacin, moxifloxacin
U, Bischoff, C, Schmidt, R, Netzer, O, Pongs   +3 more
openaire   +2 more sources

Prediction of hERG K+ channel blockage using deep neural networks

Chemical Biology and Drug Design, 2019
Human ether‐a‐go‐go‐related gene (hERG) K+ channel blockage may cause severe cardiac side‐effects and has become a serious issue in safety evaluation of drug candidates.
Yanmin Zhang, Junnan Zhao, Yuchen Wang, Yuanrong Fan, Lu Zhu, Yan Yang, Xingye Chen, T. Lu, Yadong Chen, Haichun Liu   +9 more
semanticscholar   +1 more source

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

Pharmacology & Therapeutics, 2008
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 screens rely on surrogate markers of TdP to highlight potential problems with new drugs.
Hancox, JC, McPate, MJW, El Harchi, A, Zhang, YH   +3 more
openaire   +3 more sources

Dynamics of hERG Closure Allow Novel Insights into hERG Blocking by Small Molecules

Journal of Chemical Information and Modeling, 2014
Today, drug discovery routinely uses experimental assays to determine very early if a lead compound can yield certain types of off-target activity. Among such off targets is hERG. The ion channel plays a primordial role in membrane repolarization and altering its activity can cause severe heart arrhythmia and sudden death.
Peter, Schmidtke, Marine, Ciantar, Isabelle, Theret, Pierre, Ducrot   +3 more
openaire   +2 more sources

hERG-related drug toxicity and models for predicting hERG liability and QT prolongation

Expert Opinion on Drug Metabolism & Toxicology, 2009
hERG K(+) channels have been recognized as a primary antitarget in safety pharmacology. Their blockade, caused by several drugs with different therapeutic indications, may lead to QT prolongation and, eventually, to potentially fatal arrhythmia, namely torsade de pointes.
RASCHI, EMANUEL, CECCARINI, LUISA, DE PONTI, FABRIZIO, RECANATINI, MAURIZIO   +3 more
openaire   +2 more sources

Evaluation of Possible Proarrhythmic Potency: Comparison of the Effect of Dofetilide, Cisapride, Sotalol, Terfenadine, and Verapamil on hERG and Native IKr Currents and on Cardiac Action Potential

Toxicological Sciences, 2018
The proarrhythmic potency of drugs is usually attributed to the IKr current block. During safety pharmacology testing analysis of IKr in cardiomyocytes was replaced by human ether-a-go-go-related gene (hERG) test using automated patch-clamp systems in ...
P. Orvos, Z. Kohajda, Jozefina Szlovák, Péter Gazdag, Tamás Árpádffy-Lovas, Dániel Tóth, A. Geramipour, L. Tálosi, N. Jost, A. Varró, L. Virág   +10 more
semanticscholar   +1 more source

GraphDeep-hERG: Graph Neural Network PharmacoAnalytics for Assessing hERG-Related Cardiotoxicity

Pharmaceutical Research
The human Ether-a-go-go Related-Gene (hERG) encodes rectifying potassium channels that play a significant role during action potential repolarization of cardiomyocytes. Blockade of the hERG channel by off-target drugs can lead to long QT syndrome, significantly increasing the risk of proarrhythmic cardiotoxicity.
Yankang Jing, Yiyang Zhang, Guangyi Zhao, Terence McGuire, Jack Zhao, Ben Gibbs, Ganqian Hou, Zhiwei Feng, Ying Xue, Xiang-Qun Xie   +9 more
openaire   +2 more sources

HERG channel trafficking.

Novartis Foundation symposium, 2005
Mutations in the cardiac potassium channel hERG/IKr cause inherited long QT syndrome with increased susceptibility to ventricular arrhythmias. Several mutations in hERG produce trafficking-deficient channels that are retained in the endoplasmic reticulum (ER). Surface expression of certain mutations (i.e. hERG G601S) can be restored by specific channel
Eckhard, Ficker, Adrienne, Dennis, Yuri, Kuryshev, Barbara A, Wible, Arthur M, Brown   +4 more
openaire   +1 more source

HERG

2008
openaire   +2 more sources

Development of Safe Drugs: The hERG Challenge

Medicinal research reviews (Print), 2018
S. Kalyaanamoorthy, K. Barakat
semanticscholar   +1 more source