Pharmacological activation of the hERG K+ channel for the management of the long QT syndrome: A review
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Arrhythmia"
DOI: 10.1002/joa3.12741
Abstract: In the human heart, the rapid delayed rectifier K+ current (IKr) contributes significantly to ventricular action potential (AP) repolarization and to set the duration of the QT interval of the surface electrocardiogram (ECG). The pore‐forming… read more here.
Keywords: review; long syndrome; management; herg channel ... See more keywords
Serine mutation of a conserved threonine in the hERG K+ channel S6-pore region leads to loss-of-function through trafficking impairment
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical and Biophysical Research Communications"
DOI: 10.1016/j.bbrc.2020.04.003
Abstract: The human Ether-à-go-go Related Gene (hERG) encodes a potassium channel responsible for the cardiac rapid delayed rectifier K+ current, IKr, which regulates ventricular repolarization. Loss-of-function hERG mutations underpin the LQT2 form of congenital long QT… read more here.
Keywords: herg; iherg; channel; herg t634s ... See more keywords
The Uremic Toxin P-Cresol Reduces Cell Surface Expression of Human Ether-A-Go Go-Related Gene (hERG) Channels via the Ubiquitin Ligase Nedd4-2
Sign Up to like & getrecommendations! Published in 2017 at "Biophysical Journal"
DOI: 10.1016/j.bpj.2016.11.2953
Abstract: 2695-Pos Board B302 The Uremic Toxin P-Cresol Reduces Cell Surface Expression of Human Ether-A-Go Go-Related Gene (hERG) Channels via the Ubiquitin Ligase Nedd4-2 Ellen G. Avery, Shawn Lamothe, Shetuan Zhang, Jun Guo, Wentao Li, Tonghua… read more here.
Keywords: toxin cresol; cresol; herg; herg channels ... See more keywords
The Fast Component of hERG Gating Charge: An Interaction between D411 in the S1 and S4 Residues.
Sign Up to like & getrecommendations! Published in 2017 at "Biophysical journal"
DOI: 10.1016/j.bpj.2017.09.004
Abstract: Kv11.1 (hERG) is a voltage-gated potassium channel that shows very slow ionic current activation kinetics, and an unusual underlying biphasic gating charge movement with fast and slow components that differ greatly in time course. The… read more here.
Keywords: gating charge; herg; charge; activation ... See more keywords
Effects of cariprazine on hERG 1A and hERG 1A/3.1 potassium channels.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of pharmacology"
DOI: 10.1016/j.ejphar.2019.04.006
Abstract: Cariprazine is a novel atypical antipsychotic drug that is widely used for the treatment of schizophrenia and bipolar mania/mixed disorder. We used the whole-cell patch-clamp technique to investigate the effects of cariprazine on hERG channels… read more here.
Keywords: herg; herg herg; cariprazine herg; effects cariprazine ... See more keywords
Ondansetron and teratogenicity in rats: Evidence for a mechanism mediated via embryonic hERG blockade.
Sign Up to like & getrecommendations! Published in 2018 at "Reproductive toxicology"
DOI: 10.1016/j.reprotox.2018.08.018
Abstract: The potent hERG channel blocking drug ondansetron is used off-label for treatment of nausea and vomiting in early pregnancy. Some human epidemiological studies have associated ondansetron with fetal cardiovascular defects and orofacial clefts. This study… read more here.
Keywords: mediated via; herg; ondansetron; ondansetron teratogenicity ... See more keywords
HergSPred: Accurate Classification of hERG Blockers/Nonblockers with Machine-Learning Models
Sign Up to like & getrecommendations! Published in 2022 at "Journal of chemical information and modeling"
DOI: 10.1021/acs.jcim.2c00256
Abstract: The human ether-à-go-go-related gene (hERG) K+ channel plays an important role in cardiac action potentials. The inhibition of the hERG channel may lead to long QT syndrome (LQTS) and even sudden cardiac death. Due to… read more here.
Keywords: hergspred accurate; classification; accurate classification; classification herg ... See more keywords
Early Steps in C-Type Inactivation of the hERG Potassium Channel
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Chemical Information and Modeling"
DOI: 10.1021/acs.jcim.2c01028
Abstract: Fast C-type inactivation confers distinctive functional properties to the hERG potassium channel, and its association to inherited and acquired cardiac arrythmias makes the study of the inactivation mechanism of hERG at the atomic detail of… read more here.
Keywords: potassium; type inactivation; selectivity filter; inactivation ... See more keywords
Deep Learning-Based Prediction of Drug-Induced Cardiotoxicity
Sign Up to like & getrecommendations! Published in 2019 at "Journal of chemical information and modeling"
DOI: 10.1021/acs.jcim.8b00769
Abstract: Blockade of the human ether-à-go-go-related gene (hERG) channel by small molecules induces the prolongation of the QT interval which leads to fatal cardiotoxicity and accounts for the withdrawal or severe restrictions on the use of… read more here.
Keywords: herg; deep learning; drug; cardiotoxicity ... See more keywords
A hERG mutation E1039X produced a synergistic lesion on IKs together with KCNQ1-R174C mutation in a LQTS family with three compound mutations
Sign Up to like & getrecommendations! Published in 2018 at "Scientific Reports"
DOI: 10.1038/s41598-018-21442-6
Abstract: Congenital long QT syndrome (LQTS) caused by compound mutations is usually associated with more severe clinical phenotypes. We identified a LQTS family harboring three compound mutations in different genes (KCNQ1-R174C, hERG-E1039X and SCN5A-E428K). KCNQ1-R174C, hERG-E1039X… read more here.
Keywords: herg; herg e1039x; mutation; kcnq1 r174c ... See more keywords
R534C mutation in hERG causes a trafficking defect in iPSC-derived cardiomyocytes from patients with type 2 long QT syndrome
Sign Up to like & getrecommendations! Published in 2019 at "Scientific Reports"
DOI: 10.1038/s41598-019-55837-w
Abstract: Patient-specific cardiomyocytes obtained from induced pluripotent stem cells (CM-iPSC) offer unprecedented mechanistic insights in the study of inherited cardiac diseases. The objective of this work was to study a type 2 long QT syndrome (LQTS2)-associated… read more here.
Keywords: r534c mutation; long syndrome; herg; ipsc ... See more keywords