Results 191 to 200 of about 28,801 (226)
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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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Effects of fluoroquinolones on HERG currents
European Journal of Pharmacology, 2000We 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 +3 more
exaly +3 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.
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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.
openaire +2 more sources
hERG-related drug toxicity and models for predicting hERG liability and QT prolongation
Expert Opinion on Drug Metabolism & Toxicology, 2009hERG 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 +3 more
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GraphDeep-hERG: Graph Neural Network PharmacoAnalytics for Assessing hERG-Related Cardiotoxicity
Pharmaceutical ResearchThe 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 +9 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
Eckhard, Ficker +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
Eckhard, Ficker +4 more
openaire +1 more source
HERG channel and cancer: A mechanistic review of carcinogenic processes and therapeutic potential
Biochimica Et Biophysica Acta: Reviews on Cancer, 2020Mohamed Taha Moutaoufik +2 more
exaly
Cryo-EM Structure of K+-Bound hERG Channel Complexed with the Blocker Astemizole
Structure, 2021Takamitsu Maru +2 more
exaly