Membrane potential drives the exit from pluripotency and cell fate commitment via calcium and mTOR
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
doaj +1 more source
Molecular determinants of interactions between the N-terminal domain and the transmembrane core that modulate hERG K+ channel gating. [PDF]
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
doaj +1 more source
Eag Domains Regulate LQT Mutant hERG Channels in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes. [PDF]
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
doaj +1 more source
Zebrafish Behavioral Profiling Links Drugs to Biological Targets and Rest/Wake Regulation [PDF]
A major obstacle for the discovery of psychoactive drugs is the inability to predict how small molecules will alter complex behaviors. We report the development and application of a high-throughput, quantitative screen for drugs that alter the behavior ...
Arvanites, Anthony+10 more
core +1 more source
APETx4, a Novel Sea Anemone Toxin and a Modulator of the Cancer-Relevant Potassium Channel KV10.1
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
doaj +1 more source
Novel roles for hERG K+ channels in cell proliferation and apoptosis [PDF]
The human ether-a-go-go-related gene potassium channel (hERG, Kv11.1, KCNH2) has an essential role in cardiac action potential repolarization. Electrical dysfunction of the voltage-sensitive ion channel is associated with potentially lethal ventricular ...
Jehle, J+3 more
core +2 more sources
Structural modeling of hERG channel–drug interactions using Rosetta
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
doaj +1 more source
Blockade of the human ether-a-go-go-related gene potassium channel by ketamine
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.
Antao Luo+6 more
openaire +2 more sources
Case report: Ivabradine induced Torsades de Pointes
Ivabradine is used to control heart rate in patients of heart failure with reduced ejection fraction. Although considered safe, it is reported to prolong QTc interval when given with other QTc prolonging drugs or in setting of hypokalemia or ...
Mohit M. Bhagwati+2 more
doaj
Environment-Sensitive Fluorescent Probe for the Human Ether-a-go-go-Related Gene Potassium Channel [PDF]
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 ...
Minyong Li+6 more
openaire +3 more sources