Results 31 to 40 of about 30,487 (240)

The EAG Voltage-Dependent K+ Channel Subfamily: Similarities and Differences in Structural Organization and Gating

Frontiers in Pharmacology, 2020
EAG (ether-à-go-go or KCNH) are a subfamily of the voltage-gated potassium (Kv) channels. Like for all potassium channels, opening of EAG channels drives the membrane potential toward its equilibrium value for potassium, thus setting the resting ...
Francisco Barros, Pilar de la Peña, Pedro Domínguez, Luisa Maria Sierra, Luis A. Pardo   +4 more
doaj   +1 more source

Calculations of the binding free energies of the Comprehensive in vitro Proarrhythmia Assay (CiPA) reference drugs to cardiac ion channels

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
doaj   +1 more source

Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator [PDF]

Proceedings of the National Academy of Sciences, 2007
Activation of human ether-a-go-go-related gene 1 (hERG1) K + channels mediates cardiac action potential repolarization. Drugs that activate hERG1 channels represent a mechanism-based approach for the treatment of long QT syndrome, a disorder of cardiac repolarization associated with ventricular arrhythmia and sudden
Matthew, Perry, Frank B, Sachse, Michael C, Sanguinetti   +2 more
openaire   +2 more sources

Novel intramolecular photoinduced electron transfer-based probe for the Human Ether-a-go-go-Related Gene (hERG) potassium channel [PDF]

The Analyst, 2015
A novel conformation-mediated intramolecular photoinduced electron transfer fluorogenic system based-on naphthalimide fluorophore was established for hERG potassium channel herein. After careful evaluation, probe N4 and N6 showed good activity and may have a promising application in hERG channel imaging and drug cardiotoxicity evaluation.
Zhenzhen Liu, Yubin Zhou, Lüpei Du, Minyong Li   +3 more
openalex   +3 more sources

The Human Ether-a-go-go-related Gene (hERG) Potassium Channel Represents an Unusual Target for Protease-mediated Damage [PDF]

Journal of Biological Chemistry, 2016
The human ether-a-go-go-related gene (hERG) encodes the pore-forming subunit of the rapidly activating delayed rectifier potassium channel (IKr), which is important for cardiac repolarization. Dysfunction of hERG causes long QT syndrome and sudden death, which occur in patients with cardiac ischemia. Cardiac ischemia is also associated with activation,
Shawn M. Lamothe, Guo Jun Liu, Wentao Li, Tonghua Yang, Shetuan Zhang   +4 more
openalex   +4 more sources

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, Valentyna Kostiuk, Jie Zhu, M. Cecilia Guerra, Leonid Tyan, Woong Hwang, Elena Camacho-Aguilar, Michael J. Caplan, David Zenisek, Aryeh Warmflash, Nick D. L. Owens, Mustafa K. Khokha   +11 more
doaj   +1 more source

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, Junlian, Xing, Antao, Luo, Juan, Feng, Zhipei, Liu, Chenghao, Gao, Jihua, Ma   +6 more
openaire   +2 more sources

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, Hong Yao, Hao-Lan Yin, Qi-Lei Zhu, Jia-Liang Sun, Wei Ma, Yuan-Qi Shi, Zhao-Guang Liang, Bao-Xin Li   +8 more
doaj   +1 more source

Comprehensive translational assessment of human-induced pluripotent stem cell derived cardiomyocytes for evaluating drug-induced arrhythmias [PDF]

, 2016
Induced pluripotent stem cell-derived cardiomyocytes (iPSC-CM) hold promise for assessment of drug-induced arrhythmias and are being considered for use under the comprehensive in vitro proarrhythmia assay (CiPA).
Blinova, Ksenia, Brock, Mathew, Chan, Dulciana, Chvatal, Stacie, Crumb, William J., Galeotti, Loriano, Hortigon-Vinagre, Maria P., Johannesen, Lars, Lyn-Cook, Beverly, Millard, Daniel, Pang, Li, Ross, James, Smith, Godfrey, Stockbridge, Norman, Stohlman, Jayna, Strauss, David G., Vicente, Jose, Zamora Rodriguez, Victor   +17 more
core   +1 more source

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, Steve Peigneur, Diogo T. Galan, Edwin De Pauw, Lászlo Béress, Etienne Waelkens, Luis A. Pardo, Loïc Quinton, Jan Tytgat   +8 more
doaj   +1 more source