Results 51 to 60 of about 1,218,415 (224)
DataSheet1_Structural modeling of hERG channel–drug interactions using Rosetta.pdf
, 2023 The human ether-a-go-go-related gene (hERG) not only encodes a potassium-selective voltage-gated ion channel essential for normal electrical activity in the heart but is also a major drug anti-target.
Igor Vorobyov (1900024) +8 more
core +1 more source
Effects of cariprazine on hERG 1A and hERG 1A/3.1 potassium channels
European Journal of Pharmacology, 2019 Cariprazine is a novel atypical antipsychotic drug that is widely used for the treatment of schizophrenia and bipolar mania/mixed disorder. We used the whole-cell patch-clamp technique to investigate the effects of cariprazine on hERG channels that are stably expressed in HEK cells. Cariprazine inhibited the hERG 1A and hERG 1A/3.1 tail currents at -50
Hong Joon, Lee +3 more
openaire +2 more sources
Facilitation of I Kr current by some hERG channel blockers suppresses early afterdepolarizations. [PDF]
J Gen Physiol, 2019 Drug-induced block of the cardiac rapid delayed rectifying potassium current (I Kr), carried by the human ether-a-go-go-related gene (hERG) channel, is the most common cause of acquired long QT syndrome.
Furutani K +6 more
europepmc +2 more sources
Early identification of hERG liability in drug discovery programs by automated patch clamp
Frontiers in Pharmacology, 2014 Blockade of the cardiac ion channel coded by hERG can lead to cardiac arrhythmia, which has become a major concern in drug discovery and development.
Timm eDanker, Clemens eMöller
doaj +1 more source
Frontiers in Pharmacology, 2021 Aims: The short QT syndrome type 1 (SQT1) is linked to hERG channel mutations (e.g., N588K). Drug effects on hERG channel gating kinetics in SQT1-cells have not been investigated.Methods: This study used hiPSC-CMs of a healthy donor and a SQT1-patient ...
Mengying Huang +23 more
doaj +1 more source
British Journal of Clinical Pharmacology, EarlyView.. Aims Traditional pharmacovigilance detects single drug–event associations but cannot readily characterize multi‐system adverse‐event patterns such as fluoroquinolone‐associated disability. We evaluated unsupervised machine learning for this purpose, using fluoroquinolones as an exemplar.
Niaz Chalabianloo +3 more
wiley +1 more source
Effects of an hERG Activator, ICA-105574, on Electrophysiological Properties of Canine Hearts
Journal of Pharmacological Sciences, 2013 In short QT syndrome, inherited gain-of-function mutations in the human ether a-go-go-related gene (hERG) K+ channel have been associated with development of fatal arrhythmias. This implies that drugs that activate hERG as a side effect may likewise pose
Mahoko Asayama +8 more
doaj +1 more source
The genetic architecture of epilepsy across molecular mechanisms and clinical heterogeneity
Epilepsia Open, EarlyView.Abstract Epilepsy comprises a highly heterogeneous group of neurological disorders unified by a persistent predisposition to recurrent seizures, yet driven by remarkably diverse genetic, molecular, and network‐level mechanisms. Advances in genomic technologies have revealed that epilepsy arises from a multilayered genetic architecture encompassing rare
Mohammad Reza Seyedtaghia +4 more
wiley +1 more source
, 2011 The hERG voltage-gated potassium channel mediates the cardiac I(Kr) current, which is crucial for the duration of the cardiac action potential. Undesired block of the channel by certain drugs may prolong the QT interval and increase the risk of malignant
Sintra Grilo, Liliana +7 more
core +1 more source
Mechanisms of IhERG/IKr Modulation by α1-Adrenoceptors in HEK293 Cells and Cardiac Myocytes
Cellular Physiology and Biochemistry, 2016 Background: The rapid delayed rectifier K+ current (IKr), carried by the hERG protein, is one of the main repolarising currents in the human heart and a reduction of this current increases the risk of ventricular fibrillation.
Janire Urrutia +6 more
doaj +1 more source