Results 51 to 60 of about 12,393 (207)

High-Throughput Chemical Screening and Structure-Based Models to Predict hERG Inhibition

Biology, 2022
Chemical inhibition of the human ether-a -go-go-related gene (hERG) potassium channel leads to a prolonged QT interval that can contribute to severe cardiotoxicity.
Shagun Krishna, Alexandre Borrel, Ruili Huang, Jinghua Zhao, Menghang Xia, Nicole Kleinstreuer   +5 more
doaj   +1 more source

Functional consequences of methionine oxidation of hERG potassium channels [PDF]

Biochemical Pharmacology, 2007
Reactive species oxidatively modify numerous proteins including ion channels. Oxidative sensitivity of ion channels is often conferred by amino acids containing sulfur atoms, such as cysteine and methionine. Functional consequences of oxidative modification of methionine in human ether à go-go related gene 1 (hERG1), which encodes cardiac I(Kr ...
Zhi, Su, James, Limberis, Ruth L, Martin, Rong, Xu, Katrin, Kolbe, Stefan H, Heinemann, Toshinori, Hoshi, Bryan F, Cox, Gary A, Gintant   +8 more
openaire   +2 more sources

Molecular Insights into hERG Potassium Channel Blockade by Lubeluzole [PDF]

Cellular Physiology and Biochemistry, 2018
Background/Aims: Lubeluzole is a benzothiazole derivative that has shown neuroprotective properties in preclinical models of ischemic stroke. However, clinical research on lubeluzole is now at a standstill, since lubeluzole seems to be associated with the acquired long QT syndrome and ventricular arrhythmias.
Gualdani, Roberta, Cavalluzzi, Maria Maddalena, Tadini-Buoninsegni, Francesco, Convertino, Marino, Gailly, Philippe, Stary-Weinzinger, Anna, Lentini, Giovanni   +6 more
openaire   +8 more sources

hiPSC-Derived Cardiomyocyte Model of LQT2 Syndrome Derived from Asymptomatic and Symptomatic Mutation Carriers Reproduces Clinical Differences in Aggregates but Not in Single Cells

Cells, 2020
Mutations in the HERG gene encoding the potassium ion channel HERG, represent one of the most frequent causes of long QT syndrome type-2 (LQT2). The same genetic mutation frequently presents different clinical phenotypes in the family. Our study aimed to
Disheet Shah, Chandra Prajapati, Kirsi Penttinen, Reeja Maria Cherian, Jussi T. Koivumäki, Anna Alexanova, Jari Hyttinen, Katriina Aalto-Setälä   +7 more
doaj   +1 more source

Endocytosis of HERG is clathrin-independent and involves arf6. [PDF]

PLoS ONE, 2013
The hERG potassium channel is critical for repolarisation of the cardiac action potential. Reduced expression of hERG at the plasma membrane, whether caused by hereditary mutations or drugs, results in long QT syndrome and increases the risk of ...
Rucha Karnik, Melanie J Ludlow, Nada Abuarab, Andrew J Smith, Matthew E L Hardy, David J S Elliott, Asipu Sivaprasadarao   +6 more
doaj   +1 more source

Development of models for predicting Torsade de Pointes cardiac arrhythmias using perceptron neural networks

, 2017
Blockage of some ion channels and in particular, the hERG cardiac potassium channel delays cardiac repolarization and can induce arrhythmia. In some cases it leads to a potentially life-threatening arrhythmia known as Torsade de Pointes (TdP).
Buzatu, Dan, Harris, Stephen, Sharifi, Mohsen, Wilkes, Jon   +3 more
core   +1 more source

Antidepressive and anxiolytic effects of ostruthin, a TREK-1 channel activator [PDF]

, 2018
We screened a library of botanical compounds purified from plants of Vietnam for modulators of the activity of a two-pore domain K+ channel, TREK-1, and we identified a hydroxycoumarin-related compound, ostruthin, as an activator of this channel ...
Joseph, Ancy, Okada, Masayoshi, Thanh, Le Tat, Thuy, Tran Thi Thu   +3 more
core   +2 more sources

Conformable Microelectrode Arrays Integrated with a Scoop‐Shaped Slide‐Well for Dynamic Electrophysiological Profiling of Patient‐Derived Cardiac Organoids

Advanced Science, EarlyView.
A flexible, ultrathin multi‐channel microelectrode array (MEA) conformally integrated onto a curved slide‐well enables stable electrical interfacing with 3D cardiac organoids. The geometry‐guided self‐alignment allows simultaneous recording of extracellular field potentials and contractile motion from irregular, beating tissues.
Ye Seul Kim, Jeonghwa Jeong, Gyeonghwa Heo, Young Woo Kwon, Jeongha Lee, Yoon Ji Jeong, Gyu Tae Park, Seongdo Jeong, Ki Won Hwang, Murim Choi, Jinhong Shin, Suck Won Hong, Jae Ho Kim   +12 more
wiley   +1 more source

Facilitation of I Kr current by some hERG channel blockers suppresses early afterdepolarizations. [PDF]

, 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.
Chen, I-Shan, Furutani, Kazuharu, Handa, Kenichiro, Kurachi, Yoshihisa, Sack, Jon T, Tsumoto, Kunichika, Yamakawa, Yuko   +6 more
core   +1 more source

Early LQT2 Nonsense Mutation Generates N-Terminally Truncated hERG Channels with Altered Gating Properties by the Reinitiation of Translation

, 2012
Mutations in the human ether-a-go-go-related gene (hERG) result in long QT syndrome type 2 (LQT2). The hERG gene encodes a K+ channel that contributes to the repolarization of the cardiac action potential.
Gong, Qiuming, Packer, Jonathan D., Stump, Matthew R., Zhou, Zhengfeng   +3 more
core   +1 more source