Results 1 to 10 of about 613 (70)

Up-regulation of hERG K⁺ channels by B-RAF. [PDF]

PLoS ONE, 2014
Human ether-a-go-go related-gene K⁺ channels (hERG) participate in the regulation of tumor cell proliferation and apoptosis. HERG channel activity is up-regulated by growth factors.
Tatsiana Pakladok, Zohreh Hosseinzadeh, Ahmad Almilaji, Aleksandra Lebedeva, Ekaterina Shumilina, Ioana Alesutan, Florian Lang   +6 more
doaj   +1 more source

Hysteretic hERG channel gating current recorded at physiological temperature

Scientific Reports, 2022
Cardiac hERG channels comprise at least two subunits, hERG 1a and hERG 1b, and drive cardiac action potential repolarization. hERG 1a subunits contain a cytoplasmic PAS domain that is absent in hERG 1b.
David K. Jones
doaj   +1 more source

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

Inhibitory effects and mechanism of dihydroberberine on hERG channels expressed in HEK293 cells. [PDF]

PLoS ONE, 2017
The human ether-a-go-go-related gene (hERG) potassium channel conducts rapid delayed rectifier potassium currents (IKr) and contributes to phase III cardiac action potential repolarization.
Dahai Yu, Lin Lv, Li Fang, Bo Zhang, Junnan Wang, Ge Zhan, Lei Zhao, Xin Zhao, Baoxin Li   +8 more
doaj   +1 more source

hERG-deficient human embryonic stem cell-derived cardiomyocytes for modelling QT prolongation

Stem Cell Research & Therapy, 2021
Background Long-QT syndrome type 2 (LQT2) is a common malignant hereditary arrhythmia. Due to the lack of suitable animal and human models, the pathogenesis of LQT2 caused by human ether-a-go-go-related gene (hERG) deficiency is still unclear.
Yun Chang, Ya-nan Li, Rui Bai, Fujian Wu, Shuhong Ma, Amina Saleem, Siyao Zhang, Youxu Jiang, Tao Dong, Tianwei Guo, Chengwen Hang, Wen-jing Lu, Hongfeng Jiang, Feng Lan   +13 more
doaj   +1 more source

Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin. [PDF]

PLoS ONE, 2013
Treatment of LQT2 is inadequate. Many drugs which can pharmacologically rescue defective protein trafficking in LQT2 also result in potent blockade of HERG current, negating their therapeutic benefit.
Haiyan Mao, Xiaoli Lu, Justin Michael Karush, Xiaoyan Huang, Xi Yang, Yanna Ba, Ying Wang, Ningsheng Liu, Jianqing Zhou, Jiangfang Lian   +9 more
doaj   +1 more source

Trafficking-deficient G572R-hERG and E637K-hERG activate stress and clearance pathways in endoplasmic reticulum. [PDF]

PLoS ONE, 2012
Long QT syndrome type 2 (LQT2) is the second most common type of all long QT syndromes. It is well-known that trafficking deficient mutant human ether-a-go-go-related gene (hERG) proteins are often involved in LQT2.
Ying Wang, Xiaoyan Huang, Jianqing Zhou, Xi Yang, Di Li, Haiyan Mao, Huan Huan Sun, Ningsheng Liu, Jiangfang Lian   +8 more
doaj   +1 more source

Action potential clamp and pharmacology of the variant 1 Short QT Syndrome T618I hERG K⁺ channel.

PLoS ONE, 2012
BackgroundThe familial Short QT Syndrome (SQTS) is associated with an increased risk of cardiac arrhythmia and sudden death. Gain-of-function mutations in the hERG K(+) channel protein have been linked to variant 1 of the SQTS. A hERG channel pore (T618I)
Aziza El Harchi, Dario Melgari, Yi Hong Zhang, Henggui Zhang, Jules C Hancox   +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

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