Results 51 to 60 of about 36,434 (294)

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

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

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

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

Gain of function mutants: Ion channels and G protein-coupled receptors [PDF]

, 2000
Many ion channels and receptors display striking phenotypes for gain-of-function mutations but milder phenotypes for null mutations. Gain of molecular function can have several mechanistic bases: selectivity changes, gating changes including constitutive
Karschin, Andreas, Lester, Henry A.
core   +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

Structure-activity relationships of fluorene compounds inhibiting HCV variants [PDF]

, 2020
Approximately 71 million people suffer from hepatitis C virus (HCV) infection worldwide. Persistent HCV infection causes liver diseases such as chronic hepatitis, liver cirrhosis, and hepatocellular carcinoma, resulting in approximately 400,000 deaths ...
Gadhe, Changdev G., JANG, SUNG KEY, Keum, Gyochang, Kim, Byeong Moon, Kim, Hee Sun, Kohara, Michinori, Lee, Jae Seung, Moon, Heejo, Mun, Jaegon, Pae, Ae Nim, You, Youngsu   +10 more
core   +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

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, Aiyana M. Emigh Cortez, Kevin R. DeMarco, Kevin R. DeMarco, Kazuharu Furutani, Kazuharu Furutani, Slava Bekker, Slava Bekker, Jon T. Sack, Jon T. Sack, Heike Wulff, Colleen E. Clancy, Colleen E. Clancy, Colleen E. Clancy, Igor Vorobyov, Igor Vorobyov, Vladimir Yarov-Yarovoy, Vladimir Yarov-Yarovoy   +17 more
doaj   +1 more source

Capsule Networks Showed Excellent Performance in the Classification of hERG Blockers/Nonblockers

Frontiers in Pharmacology, 2020
Capsule networks (CapsNets), a new class of deep neural network architectures proposed recently by Hinton et al., have shown a great performance in many fields, particularly in image recognition and natural language processing. However, CapsNets have not
Yiwei Wang, Lei Huang, Siwen Jiang, Yifei Wang, Jun Zou, Hongguang Fu, Sheng-Yong Yang   +6 more
semanticscholar   +1 more source