Biophysics and Physicobiology, 2023 The evaluation of the inhibitory activities of drugs on multiple cardiac ion channels is required for the accurate assessment of proarrhythmic risks.
Tatsuki Negami, Tohru Terada
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Membrane potential drives the exit from pluripotency and cell fate commitment via calcium and mTOR
Nature Communications, 2022 Transitioning from pluripotency to differentiated cell fates is fundamental to both embryonic development and adult tissue homeostasis. Improving our understanding of this transition would facilitate our ability to manipulate pluripotent cells into ...
Emily Sempou +11 more
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Blockade of the human ether-a-go-go-related gene potassium channel by ketamine
Journal of Pharmacy and Pharmacology, 2013 Abstract Objectives The inhibition of the cardiac rapid delayed rectifier potassium current (IKr) and its cloned equivalent human ether-a-go-go-related gene (hERG) channel illustrate QT interval prolonging effects of a wide range of clinically used drugs.
Peihua, Zhang +6 more
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Environment-Sensitive Fluorescent Probe for the Human Ether-a-go-go-Related Gene Potassium Channel [PDF]
Analytical Chemistry, 2016 A novel environment-sensitive probe S2 with turn-on switch for Human Ether-a-go-go-Related Gene (hERG) potassium channel was developed herein. After careful evaluation, this fluorescent probe showed high binding affinity with hERG potassium channel with an IC50 value of 41.65 nM and can be well applied to hERG channel imaging or cellular distribution ...
Liu, Zhenzhen +6 more
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Ginkgo biloba Extract and Ginkgolide Antiarrhythmic Potential by Targeting hERG and ICa-L Channel
Journal of Pharmacological Sciences, 2013 We investigated the effects of Ginkgo biloba extract (GBE) and ginkgolide (GLD) on human ether-a-go-go-related gene (hERG)-encoded K+ channels and its underlying mechanisms in the hERG-HEK293 cell line by determining GBE- and GLD-induced changes in ...
Xin Zhao +8 more
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Molecular determinants of interactions between the N-terminal domain and the transmembrane core that modulate hERG K+ channel gating. [PDF]
PLoS ONE, 2011 A conserved eag domain in the cytoplasmic amino terminus of the human ether-a-go-go-related gene (hERG) potassium channel is critical for its slow deactivation gating.
Jorge Fernández-Trillo +5 more
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APETx4, a Novel Sea Anemone Toxin and a Modulator of the Cancer-Relevant Potassium Channel KV10.1
Marine Drugs, 2017 The human ether-à-go-go channel (hEag1 or KV10.1) is a cancer-relevant voltage-gated potassium channel that is overexpressed in a majority of human tumors. Peptides that are able to selectively inhibit this channel can be lead compounds in the search for
Lien Moreels +8 more
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Eag Domains Regulate LQT Mutant hERG Channels in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes. [PDF]
PLoS ONE, 2015 Human Ether á go-go Related Gene potassium channels form the rapid component of the delayed-rectifier (IKr) current in the heart. The N-terminal 'eag' domain, which is composed of a Per-Arnt-Sim (PAS) domain and a short PAS-cap region, is a critical ...
Qiang-Ni Liu, Matthew C Trudeau
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Antidepressive and anxiolytic effects of ostruthin, a TREK-1 channel activator. [PDF]
PLoS ONE, 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 ...
Ancy Joseph +3 more
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Structural modeling of hERG channel–drug interactions using Rosetta
Frontiers in Pharmacology, 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.
Aiyana M. Emigh Cortez +17 more
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