Results 261 to 270 of about 36,434 (294)
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
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 ...
D. Leishman +2 more
semanticscholar +3 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
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
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
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
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
Cell Calcium, 2004
Early recognition of potential QT/TdP liability is now an essential component of the drug discovery/drug development program. The hERG assay is an indispensable step and a high-quality assay must accompany any investigational new drug (IND) application.
openaire +2 more sources
Early recognition of potential QT/TdP liability is now an essential component of the drug discovery/drug development program. The hERG assay is an indispensable step and a high-quality assay must accompany any investigational new drug (IND) application.
openaire +2 more sources