Results 231 to 240 of about 33,807 (258)
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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.
Gary A. Gintant +7 more
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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
Barbara A. Wible +4 more
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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
Barbara A. Wible +4 more
openaire +3 more sources
2008
Publisher Summary Regulatory agencies insist on having experimental hERG data for all compounds moving into clinical development because of the risk of death from arrhythmia in a small portion of the population. Pharmaceutical companies need to develop a strategy for hERG block assessment during drug discovery to avoid investment in a chemical series ...
Li Di, Edward H. Kerns
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Publisher Summary Regulatory agencies insist on having experimental hERG data for all compounds moving into clinical development because of the risk of death from arrhythmia in a small portion of the population. Pharmaceutical companies need to develop a strategy for hERG block assessment during drug discovery to avoid investment in a chemical series ...
Li Di, Edward H. Kerns
openaire +3 more sources
2008
Publisher Summary hERG is a gene that codes for a cardiac potassium ion channel. If this channel is blocked, a mechanism is initiated that can lead to cardiac arrhythmia. hERG has rapidly emerged as an important safety issue in drug discovery. Awareness about the details of hERG and its impact is growing among discovery scientists. Recent efforts have
Li Di, Edward H. Kerns
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Publisher Summary hERG is a gene that codes for a cardiac potassium ion channel. If this channel is blocked, a mechanism is initiated that can lead to cardiac arrhythmia. hERG has rapidly emerged as an important safety issue in drug discovery. Awareness about the details of hERG and its impact is growing among discovery scientists. Recent efforts have
Li Di, Edward H. Kerns
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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,
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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,
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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 ...
Hilal Zaid +6 more
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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 ...
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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 ...
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Prediction of hERG K+ channel blockage using deep neural networks
Chemical Biology and Drug Design, 2019Human 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 +9 more
semanticscholar +1 more source
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.
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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.
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The hERG potassium channel and hERG screening for drug-induced torsades de pointes
Pharmacology & Therapeutics, 2008Drug-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 +3 more
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