Results 41 to 50 of about 1,218,415 (224)

The Effect of a Synthetic Estrogen, Ethinylestradiol, on the hERG Block by E-4031

Biomolecules, 2021
Inhibition of K+-conductance through the human ether-a-go-go related gene (hERG) channel leads to QT prolongation and is associated with cardiac arrhythmias.
Fumiya Tamura, Shintaro Sugimoto, Mana Sugimoto, Kazuho Sakamoto, Masahiko Yamaguchi, Takeshi Suzuki, Keiichi Fukuda, Masaki Ieda, Junko Kurokawa   +8 more
doaj   +1 more source

Toward a Consensus Model of the hERG Potassium Channel [PDF]

ChemMedChem, 2010
AbstractMalfunction of hERG potassium channels, due to inherited mutations or inhibition by drugs, can cause long QT syndrome, which can lead to life‐threatening arrhythmias. A three‐dimensional structure of hERG is a prerequisite to understand the molecular basis of hERG malfunction.
Stary, A., Wacker, S.J., Boukharta, L., Zachariae, U.G., Karimi-Nejad, Y., Aqvist, J., Vriend, G., Vriend, G., de Groot, B.L.   +8 more
openaire   +6 more sources

Harnessing AlphaFold to reveal hERG channel conformational state secrets. [PDF]

Elife
To design safe, selective, and effective new therapies, there must be a deep understanding of the structure and function of the drug target. One of the most difficult problems to solve has been the resolution of discrete conformational states of ...
Ngo K, Yang PC, Yarov-Yarovoy V, Clancy CE, Vorobyov I.   +4 more
europepmc   +2 more sources

In vitro chronic effects on hERG channel caused by the marine biotoxin Yessotoxin.

Frontiers in Marine Science, 2014
INTRODUCTION Marine algal blooms caused by the overgrowth of marine phytoplankton have increased in frequency and severity in the last years; supposing a worldwide public health problem.
Sara Fernández Ferreiro
doaj   +1 more source

In silico Exploration of Interactions Between Potential COVID-19 Antiviral Treatments and the Pore of the hERG Potassium Channel—A Drug Antitarget

Frontiers in Cardiovascular Medicine, 2021
Background: In the absence of SARS-CoV-2 specific antiviral treatments, various repurposed pharmaceutical approaches are under investigation for the treatment of COVID-19.
Ehab Al-Moubarak, Mohsen Sharifi, Jules C. Hancox   +2 more
doaj   +1 more source

Na+ Permeation and Block of hERG Potassium Channels [PDF]

The Journal of General Physiology, 2006
The inactivation gating of hERG channels is important for the channel function and drug–channel interaction. Whereas hERG channels are highly selective for K+, we have found that inactivated hERG channels allow Na+ to permeate in the absence of K+. This provides a new way to directly monitor and investigate hERG inactivation.
Gang, Hongying, Zhang, Shetuan
openaire   +2 more sources

Electrophysiological characterization of a small molecule activator on human ether-a-go-go-related gene (hERG) potassium channel

Journal of Pharmacological Sciences, 2019
The human ether-a-go-go-related gene (hERG) encodes the K+ channel that carries the rapid component of the delayed rectifier current in the human heart. Reduction of hERG activity induced by gene mutations or pharmacological inhibition is responsible for
Xiuming Dong, Yani Liu, Heling Niu, Gongxin Wang, Liying Dong, Anruo Zou, KeWei Wang   +6 more
doaj   +1 more source

Multiple mechanisms underlie reduced potassium conductance in the p.T1019PfsX38 variant of hERG

Physiological Reports, 2022
Long QT syndrome type II (LQT2) is caused by loss‐of‐function mutations in the hERG K+ channel, leading to increased incidence of cardiac arrest and sudden death.
Majid K. Al Salmani, Rezvan Tavakoli, Wajid Zaman, Ahmed Al Harrasi   +3 more
doaj   +1 more source

Calculation of absolute binding free energies between the hERG channel and structurally diverse drugs. [PDF]

Sci Rep, 2019
The human ether-a-go-go-related gene (hERG) encodes a voltage-gated potassium channel that plays an essential role in the repolarization of action potentials in cardiac muscle.
Negami T, Araki M, Okuno Y, Terada T.
europepmc   +2 more sources

New synthetic cannabinoids and the potential for cardiac arrhythmia risk

Journal of Molecular and Cellular Cardiology Plus, 2023
Synthetic cannabinoid receptor agonists (SCRAs) have been associated with QT interval prolongation. Limited preclinical information on SCRA effects on cardiac electrogenesis results from the rapid emergence of new compounds and restricted research ...
Jules C. Hancox, Caroline S. Copeland, Stephen C. Harmer, Graeme Henderson   +3 more
doaj   +1 more source