ArticlePloS one2012
Effects of the small molecule HERG activator NS1643 on Kv11.3 channels.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 18 citations in OpenAlex.
- Protective function of the voltage-gated potassium channel Kv11.3 in a mouse model of cardiac ischemia/reperfusion injury.PloS one · 2025Article
- Ion Channel Drugs Suppress Cancer Phenotype in NG108-15 and U87 Cells: Toward Novel Electroceuticals for Glioblastoma.Cancers · 2022Article
- The ERG1 KFrontiers in molecular neuroscience · 2022Review
- Functional study of a KCNH2 mutant: Novel insights on the pathogenesis of the LQT2 syndrome.Journal of cellular and molecular medicine · 2019Article
- Potassium channel activity controls breast cancer metastasis by affecting β-catenin signaling.Cell death & disease · 2019Article
- Action potential shortening rescues atrial calcium alternans.The Journal of physiology · 2019Article
- ERG3 potassium channel-mediated suppression of neuronal intrinsic excitability and prevention of seizure generation in mice.The Journal of physiology · 2018Article
- Manipulation-free cultures of human iPSC-derived cardiomyocytes offer a novel screening method for cardiotoxicity.Acta pharmacologica Sinica · 2018Article
- Drug-Mediated Shortening of Action Potentials in LQTS2 Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes.Stem cells and development · 2017Article
- Trigger vs. Substrate: Multi-Dimensional Modulation of QT-Prolongation Associated Arrhythmic Dynamics by a hERG Channel Activator.Frontiers in physiology · 2017Article
- Effects of Temperature on Heteromeric Kv11.1a/1b and Kv11.3 Channels.Biophysical journal · 2016Article
- HERG1 channel agonists and cardiac arrhythmia.Current opinion in pharmacology · 2014Review
- Structure driven design of novel human ether-a-go-go-related-gene channel (hERG1) activators.PloS one · 2014Article
- Major channels involved in neuropsychiatric disorders and therapeutic perspectives.Frontiers in genetics · 2013Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents. We now investigated whether NS1643 is also able to act as an activator of Kv11.3 (erg3) channels expressed in CHO cells. Activation of rat Kv11.3 current occurred in a dose-dependent manner and maximal current increasing effects were obtained with 10 µM NS1643. At this concentration, steady-state outward current increased by about 80% and the current increase was associated with a significant shift in the voltage dependence of activation to more negative potentials by about 15 mV. In addition, activation kinetics were accelerated, whereas deactivation was slowed. There was no significant effect on the kinetics of inactivation and recovery from inactivation. The strong current-activating agonistic effect of NS1643 did not result from a shift in the voltage dependence of Kv11.3 channel inactivation and was independent from external Na(+) or Ca(2+). At the higher concentration of 20 µM, NS1643 induced clearly less current increase. The left shift in the voltage dependence of activation reversed and the voltage sensitivity of activation dramatically decreased along with a slowing of Kv11.3 channel activation. These data show that, in comparison to other Kv11 family members, NS1643 exerts distinct effects on Kv11.3 channels with especially pronounced partial antagonistic effects at higher concentration.
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