An Update on the Structure of hERG
Frontiers in Pharmacology, 2020 The human voltage-sensitive K+ channel hERG plays a fundamental role in cardiac action potential repolarization, effectively controlling the QT interval of the electrocardiogram.
Andrew S Butler +2 more
exaly +3 more sources
Integrating drug effects on individual cardiac ionic currents and cardiac action potentials to understand nonclinical translation to clinical ECG changes [PDF]
Frontiers in PharmacologyConcomitant inhibition of the late Na+ current (INaL) and/or the L-type Ca2+ current (ICaL) has been hypothesized to mitigate hERG block-mediated QTC prolongation.
Lars Johannesen +7 more
doaj +2 more sources
Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices [PDF]
Scientific ReportsAcute block of hERG channels is the most common mechanism underlying drug-induced QTC prolongation and potentially fatal Torsade de Pointes arrhythmia. Updates to ICH E14 Q&As now allow for using negative nonclinical data, including hERG, to support QTC ...
Claudia Alvarez Baron +25 more
doaj +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
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 +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 +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 +13 more
doaj +1 more source
Lead optimisation of dehydroemetine for repositioned use in malaria [PDF]
, 2020 Drug repositioning offers an effective alternative to de novo drug design to tackle the urgent need for novel anti-malarial treatments. The anti-amoebic compound, emetine dihydrochloride, has been identified as a potent in-vitro inhibitor of the multi ...
Abubaker, M +8 more
core +3 more sources
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
doaj +1 more source