CardioTox net: a robust predictor for hERG channel blockade based on deep learning meta-feature ensembles. [PDF]
J Cheminform, 2021 Motivation Ether-a-go-go-related gene (hERG) channel blockade by small molecules is a big concern during drug development in the pharmaceutical industry.
Karim A, Lee M, Balle T, Sattar A.
europepmc +2 more sources
Mechanisms underlying probucol-induced hERG-channel deficiency
Drug Design, Development and Therapy, 2015 Yuan-Qi Shi,1,* Cai-Chuan Yan,1,* Xiao Zhang,1 Meng Yan,1 Li-Rong Liu,1 Huai-Ze Geng,1 Lin Lv,1 Bao-Xin Li1,21Department of Pharmacology, Harbin Medical University, 2State-Province Key Laboratory of Biopharmaceutical Engineering, Harbin, Heilongjiang ...
Shi YQ +7 more
doaj +1 more source
In silico modelling--pharmacophores and hERG channel models.
Novartis Foundation symposium, 2005 In computational drug design, modelling studies are undertaken following two main strategies that depend on which information is available. If experimental data exist only for the molecules displaying the biological property of interest, a so-called ligand-based approach is taken; if information is available on the macromolecular target(s) of the ...
RECANATINI, MAURIZIO +2 more
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LncRNA MALAT1/Calpain-1 Axis in ATO Induced hERG Channel Deficiency. [PDF]
Drug Des Devel TherCaichuan Yan,* Yuexin Li,* Xiaoxu Li, Yang Li, Yuhao Zhang, Jinyang Sun, Qirui Ding, Xin Zhao, Baoxin Li Department of Pharmacology, College of Pharmacy, Harbin Medical University, Harbin, People’s Republic of China*These authors contributed ...
Yan C +8 more
europepmc +2 more sources
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 +6 more
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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 +8 more
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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 +9 more
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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 +4 more
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 +12 more
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hERG potassium channel blockage by scorpion toxin BmKKx2 enhances erythroid differentiation of human leukemia cells K562. [PDF]
PLoS ONE, 2013 The hERG potassium channel can modulate the proliferation of the chronic myelogenous leukemic K562 cells, and its role in the erythroid differentiation of K562 cells still remains unclear.The hERG potassium channel blockage by a new 36-residue scorpion ...
Jian Ma +5 more
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