Results 241 to 250 of about 33,807 (258)

Investigating cardiotoxicity related with hERG channel blockers using molecular fingerprints and graph attention mechanism

Comput. Biol. Medicine, 2022
Tianyi Wang, Jianqiang Sun, Qi Zhao
semanticscholar   +1 more source

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.
Pierre Ducrot, Isabelle Theret, Marine Ciantar, Peter Schmidtke   +3 more
openaire   +3 more sources

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
Olaf Pongs, Ulrike Bischoff, Rainer Netzer, Christine Schmidt   +3 more
openaire   +3 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   +3 more sources

The Catch-22 of Predicting hERG Blockade Using Publicly Accessible Bioactivity Data

Journal of Chemical Information and Modeling, 2018
Drug-induced inhibition of the human ether-à-go-go-related gene (hERG)-encoded potassium ion channels can lead to fatal cardiotoxicity. Several marketed drugs and promising drug candidates were recalled because of this concern.
Vishal B. Siramshetty, Qiaofeng Chen, Prashanth Devarakonda, R. Preissner   +3 more
semanticscholar   +1 more source

Blockade of HERG and Kv1.5 by Ketoconazole

The Journal of Pharmacology and Experimental Therapeutics, 1998
Ketoconazole, a widely used fungicide in patients, has been associated with Q-T prolongation and torsade de pointes when co-administered with terfenadine (Seldane). Both compounds use the same cytochrome-P450 metabolic pathway, resulting in an increase in plasma concentration of terfenadine.
R, Dumaine, M L, Roy, A M, Brown
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

Intracellular Mechanism of Rosuvastatin-Induced Decrease in Mature hERG Protein Expression on Membrane.

Molecular Pharmaceutics, 2019
The hERG potassium channel (IKr) encoded by human ether-a-go-go-related gene plays an important role in cardiac repolarization. Decreased IKr may lead to long QT syndrome, which subsequently causes torsade de pointes and sudden cardiac death.
Pan-feng Feng, Bo Zhang, Lei Zhao, Q. Fang, Yan Liu, Junnan Wang, Xueqi Xu, Hui Xue, Yang Li, Cai Yan, Xin Zhao, Bao-Xin Li   +11 more
semanticscholar   +1 more source

Generation of an antibody toolbox to characterize hERG

Biochemical and Biophysical Research Communications, 2013
The human ether-a-go-go related gene (hERG) potassium channel plays a major role in the repolarization of the cardiac action potential. Inhibition of the hERG function by mutations or a wide variety of pharmaceutical compounds cause long QT syndrome and lead to potentially lethal arrhythmias.
Hausammann, Georg J, Heitkamp, Thomas, Matile, Hugues, Gsell, Bernard, Thoma, Ralf, Schmid, Georg, Frasson, David, Sievers, Martin, Hennig, Michael, Grütter, Markus G   +9 more
openaire   +3 more sources

The EGFP/hERG fusion protein alter the electrophysiological properties of hERG channels in HEK293 cells

Cell Biology International, 2011
EGFP (enhanced green fluorescent protein) tagged to either the N (amino)-terminus [EGFP/hERG (human ether-a-go-go-related gene)] or C (carboxyl)-terminus (hERG/EGFP) of hERG channel is used to study mutant channel protein trafficking for several years. However, it has been reported that the process can alter hERG channel properties.
Jiang‑Fang Lian, Tu Sheng Song, Na Huang, Li Ying Liu, Jian‑Hua Huo, Xi Yang, Chen Huang, Lei Ni, Jian‑Qing Zhou, Zongfang Li   +9 more
openaire   +3 more sources