“…Based on the scaffold of astemizole and E-4031, four AIE light-up probes (L1–L4) for Human Ether-a-go-go-Related Gene (hERG) potassium channel were developed herein using AIE fluorogen(TPE). …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…In this Part II, we use this protocol to study the temperature dependence of hERG kinetics using Chinese hamster ovary cells overexpressing hERG1a on the Nanion SyncroPatch 384PE, a 384-well automated patch-clamp platform, with temperature control. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…The hERG (human-ether-à-go-go-related gene) channel underlies the rapid delayed rectifier current, I(kr), in the heart, which is essential for normal cardiac electrical activity and rhythm. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…As a result, the human erythroid CML cell line K562 and primary human CML cells functionally expressed hERG1. Irradiation stimulated in both cell types an increase in the activity of hERG1 K(+) channels which became apparent 1–2 h post-irradiation. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Human ether-a-go-go-related gene (hERG) potassium channel blockage by small molecules may cause severe cardiac side effects. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…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. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…In this work, a model proposed two decades ago addressing the ion specificity of potassium channels is extended to the human ether-à-gogo gene (hERG). hERG encodes the protein that assembles into the potassium channel responsible for the delayed rectifier current in ventricular cardiac myocytes that is often targeted by drugs associated with QT prolongation. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Because hERG channel blockade is implicated in drug-induced arrhythmias associated with both the open and inactivated states, we used Rosetta to simulate the effects of hERG S620T and S641A/T mutations to elucidate conformational changes associated with hERG channel inactivation and differences in drug binding between the two states. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…[Image: see text] 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 paramount importance. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Our findings demonstrate the presence of an electromechanical transduction path crucial for the non-domain-swapped hERG channel gating that resembles the noncanonical path identified in domain-swapped K(+) channels.…”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Therefore, assessing hERG liability of new drugs candidates is crucial to avoid undesired cardiotoxic effects. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…The purpose of this study was to determine the effect of amiodarone (Ami) on hERG-T618I currents in HEK293 cells. A transient transfection method was used to transfer hERG-T618I and hERG wild-type (WT) channel plasmids into HEK293 cells. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…C-type inactivation in the HERG channel is unique among voltage-gated K channels in having extremely fast kinetics and strong voltage sensitivity. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…We evaluated the in vitro effects of 4-aminopyridine on the human ether-à-go-go-related gene (hERG) channel current, since hERG current inhibition is associated with QT interval prolongation—a precursor to torsade de pointes (TdP). …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Mutations impairing hERG inactivation cause life-threatening cardiac arrhythmia, which also occur as undesired side effects of drugs. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…In human ether-a-go-go–related gene 1 (hERG1) K(+) channels, C-type inactivation is allosterically inhibited by ICA-105574, a substituted benzamide. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…We recently reported gating currents recorded from hERG channels expressed in mammalian TSA cells and assessed the kinetics at different voltages. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…In this article, we find that HERG1 expression is dramatically increased both in pancreatic cancer tissues and cell lines, and that increased HERG1 expression is significantly related to the development of pancreatic cancer. …”
Enlace del recurso
Enlace del recurso

“…Promiscuous inhibition of the human ether-à-go-go-related gene (hERG) potassium channel by drugs poses a major risk for life threatening arrhythmia and costly drug withdrawals. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…Indeed, hERG1 blockage impairs tumor cell growth both in vitro and in vivo in preclinical mouse model. hERG1-based tumor therapy in humans, however, encounters the major hindrance of the potential cardiotoxicity that many hERG1 blockers exert. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso