Results 181 to 190 of about 28,801 (226)
Some of the next articles are maybe not open access.
Science, 1996
Since our 7 July 1995 report “HERG, a human inward rectifier in the voltage-gated potassium channel family” was published ([1][1]), two previously undetected differences between our expression clone and the published nucleotide sequence ([2][2]) have been identified: T593A, yielding amino acid change V198E; and C605T, yielding P202L.
M C, Trudeau +3 more
openaire +3 more sources
Since our 7 July 1995 report “HERG, a human inward rectifier in the voltage-gated potassium channel family” was published ([1][1]), two previously undetected differences between our expression clone and the published nucleotide sequence ([2][2]) have been identified: T593A, yielding amino acid change V198E; and C605T, yielding P202L.
M C, Trudeau +3 more
openaire +3 more sources
A Composite Model for hERG Blockade [PDF]
ChemMedChem, 2008 AbstracthERG blockade is one of the major toxicological problems in lead structure optimization. Reliable ligand‐based in silico models for predicting hERG blockade therefore have considerable potential for saving time and money, as patch‐clamp measurements are very expensive and no crystal structures of the hERG‐encoded channel are available.
Kramer, C. +3 more
openaire +2 more sources
Journal of Chemical Information and Modeling, 2013
A detailed analysis of the hERG content inside the ChEMBL database is performed. The correlation between the outcome from binding assays and functional assays is probed. On the basis of descriptor distributions, design paradigms with respect to structural and physicochemical properties of hERG active and hERG inactive compounds are challenged. Finally,
openaire +2 more sources
A detailed analysis of the hERG content inside the ChEMBL database is performed. The correlation between the outcome from binding assays and functional assays is probed. On the basis of descriptor distributions, design paradigms with respect to structural and physicochemical properties of hERG active and hERG inactive compounds are challenged. Finally,
openaire +2 more sources
EFFECT OF HERG CURRENT BY DRUGS IN hERG TRAFFICKING MUTANTS
Journal of Pharmacological and Toxicological Methods, 2007Mutations in the potassium channel encoded by the human ether-a-go-go-related gene (hERG) have been linked to inherited long QT syndrome (LQTS), a cardiac disease associated with an increased susceptibility to life-threatening ventricular arrhythmias and sudden death. Among these mutations, LQT2 mutation caused in cyclic nucleotide binding domain (CNBD)
Ki-Suk Kim +4 more
openaire +1 more source
Characterization of A-935142, a hERG enhancer, in the presence and absence of standard hERG blockers
Life Sciences, 2012In a previous study we found that A-935142 enhanced hERG current in a concentration-dependent manner by facilitating activation, reducing inactivation, and slowing deactivation (Su et al., 2009). A-935142 also shortened action potential duration (APD90) in canine Purkinje fibers and guinea pig atrial tissue.
Xiaoqin, Liu +7 more
openaire +2 more sources
Indexing molecules for their hERG liability
European Journal of Medicinal Chemistry, 2013The human Ether-a-go-go-Related-Gene (hERG) potassium (K(+)) channel is liable to drug-inducing blockage that prolongs the QT interval of the cardiac action potential, triggers arrhythmia and possibly causes sudden cardiac death. Early prediction of drug liability to hERG K(+) channel is therefore highly important and preferably obligatory at earlier ...
Anwar, Rayan +6 more
openaire +2 more sources
Revisiting the hERG safety margin after 20 years of routine hERG screening
Journal of Pharmacological and Toxicological Methods, 2020It has been two decades since screening new molecules and potential clinical drug candidates against the hERG potassium channel became a routine part of safety pharmacology. The earliest heuristic for what was an adequate safety margin to separate molecules with a potential liability to cause the arrhythmia torsade de pointes (TdP) from those with no ...
Derek J, Leishman +2 more
openaire +2 more sources
Blockade of HERG and Kv1.5 by Ketoconazole
The Journal of Pharmacology and Experimental Therapeutics, 1998Ketoconazole, 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
Journal of Molecular and Cellular Cardiology, 2001
G.-N. Tseng. I(Kr): The hERG Channel. Journal of Molecular and Cellular Cardiology (2001) 33, 835-849. The rapid delayed rectifier (I(Kr)) channel is important for cardiac action potential repolarization. Suppressing I(Kr)function, due to either genetic defects in its pore-forming subunit (hERG) or adverse drug effects, can lead to long-QT (LQT ...
openaire +2 more sources
G.-N. Tseng. I(Kr): The hERG Channel. Journal of Molecular and Cellular Cardiology (2001) 33, 835-849. The rapid delayed rectifier (I(Kr)) channel is important for cardiac action potential repolarization. Suppressing I(Kr)function, due to either genetic defects in its pore-forming subunit (hERG) or adverse drug effects, can lead to long-QT (LQT ...
openaire +2 more sources
Dynamics of hERG Closure Allow Novel Insights into hERG Blocking by Small Molecules
Journal of Chemical Information and Modeling, 2014Today, 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 +3 more
openaire +2 more sources