Results 21 to 30 of about 28,801 (226)

hERG Blockade Prediction by Combining Site Identification by Ligand Competitive Saturation and Physicochemical Properties

Chemistry, 2022
The human ether-a-go-go-related gene (hERG) potassium channel is a well-known contributor to drug-induced cardiotoxicity and therefore is an extremely important target when performing safety assessments of drug candidates.
Himanshu Goel, Wenbo Yu, Alexander D. MacKerell   +2 more
doaj   +1 more source

In Vitro and In Silico Risk Assessment in Acquired Long QT Syndrome: The Devil Is in the Details

Frontiers in Physiology, 2017
Acquired long QT syndrome, mostly as a result of drug block of the Kv11. 1 potassium channel in the heart, is characterized by delayed cardiac myocyte repolarization, prolongation of the T interval on the ECG, syncope and sudden cardiac death due to the ...
William Lee, William Lee, Monique J. Windley, Monique J. Windley, Jamie I. Vandenberg, Jamie I. Vandenberg, Adam P. Hill, Adam P. Hill   +7 more
doaj   +1 more source

Characterization of the novel mutant A78T-HERG from a long QT syndrome type 2 patient: Instability of the mutant protein and stabilization by heat shock factor 1

Journal of Arrhythmia, 2016
Background: The human ether-a-go-go-related gene (HERG) encodes the α-subunit of rapidly activating delayed-rectifier potassium channels. Mutations in this gene cause long QT syndrome type 2 (LQT2).
Takehito Kondo, Ichiro Hisatome, Shouichi Yoshimura, Endang Mahati, Tomomi Notsu, Peili Li, Kazuhiko Iitsuka, Masaru Kato, Kazuyoshi Ogura, Junichiro Miake, Takeshi Aiba, Wataru Shimizu, Yasutaka Kurata, Shinji Sakata, Naoe Nakasone, Haruaki Ninomiya, Akira Nakai, Katsumi Higaki, Yasushi Kawata, Yasuaki Shirayoshi, Akio Yoshida, Kazuhiro Yamamoto   +21 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

NBD-Based Environment-Sensitive Fluorescent Probes for the Human Ether-a-Go-Go–Related Gene Potassium Channel

Frontiers in Molecular Biosciences, 2021
Three environment-sensitive probes were developed for the hERG channel based on the nitrobenzoxadiazole fluorophore herein. After careful evaluation, probes M1 and M3 were found to have a high affinity for imaging the hERG channel in the cell-based ...
Qi Li, Lijuan Chai, Gaopan Dong, Xiaomeng Zhang, Lupei Du   +4 more
doaj   +1 more source

Molecular mechanisms underlying the pilsicainide-induced stabilization of hERG proteins in transfected mammalian cells

Journal of Arrhythmia, 2017
Background: Pilsicainide, classified as a relatively selective Na+ channel blocker, also has an inhibitory action on the rapidly-activating delayed-rectifier K+ current (IKr) through human ether-a-go-go-related gene (hERG) channels.
Takeshi Onohara, MD, Ichiro Hisatome, MD, Yasutaka Kurata, MD, Peili Li, MD, Tomomi Notsu, PhD, Kumi Morikawa, PhD, Naoyuki Otani, MD, Akio Yoshida, MD, Kazuhiko Iitsuka, MD, Masaru Kato, MD, Junichiro Miake, MD, Haruaki Ninomiya, MD, Katsumi Higaki, PhD, Yasuaki Shirayoshi, PhD, Takashi Nishihara, BE, Toshiyuki Itoh, PhD, Yoshinobu Nakamura, MD, Motonobu Nishimura, MD   +17 more
doaj   +1 more source

HPLC-based activity profiling for pharmacologically and toxicologically relevant natural products – principles and recent examples

Pharmaceutical Biology, 2019
Context: Discovery of pharmacologically active natural products as starting points for drug development remains important and, for reasons of consumer safety, the identification of toxicologically relevant compounds in herbal drugs. Objective: To explain,
Matthias Hamburger
doaj   +1 more source

Structural modeling of the hERG potassium channel and associated drug interactions

Frontiers in Pharmacology, 2022
The voltage-gated potassium channel, KV11.1, encoded by the human Ether-à-go-go-Related Gene (hERG), is expressed in cardiac myocytes, where it is crucial for the membrane repolarization of the action potential.
Jan Maly, Jan Maly, Aiyana M. Emigh, Aiyana M. Emigh, Kevin R. DeMarco, Kevin R. DeMarco, Kazuharu Furutani, Jon T. Sack, Colleen E. Clancy, Colleen E. Clancy, Igor Vorobyov, Igor Vorobyov, Vladimir Yarov-Yarovoy   +12 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

The electric heart of hERG [PDF]

Journal of General Physiology, 2013
Potassium channels encoded by the human ether-a-go-go–related gene (hERG) are of crucial importance for the repolarization of the cardiac action potential, as they constitute the main component of the cardiac delayed rectifier current, IKr ([Sanguinetti et al., 1995][1]).
openaire   +2 more sources