Results 11 to 20 of about 33,807 (258)
Facilitation of IKr current by some hERG channel blockers suppresses early afterdepolarizations [PDF]
The Journal of General Physiology, 2019 Drug-induced block of the cardiac rapid delayed rectifying potassium current (IKr), carried by the human ether-a-go-go-related gene (hERG) channel, is the most common cause of acquired long QT syndrome.
Kazuharu Furutani +6 more
semanticscholar +4 more sources
Biophysical Journal, 2013 The delayed rectifier, IKr, is formed by homo/heterotetramers of the 2 HERG splice variants HERG1a and HERG1b. The only difference between isoforms is that HERG1b has a shorter N-terminal than HERG1a. Despite their similarities, HERG1a and 1b have profoundly different gating kinetics: HERG1b has faster activation and deactivation kinetics than HERG1a ...
Qinlian Zhou +2 more
openaire +2 more sources
Homozygous Premature Truncation of the HERG Protein [PDF]
Circulation, 1999 Background —In long-QT syndrome (LQTS), heterozygosity for a mutation in 1 of the K + channel genes leads to prolongation of the cardiac action potential, because the aberrant protein exhibits “loss of function.” HERG, which is involved in LQT2, is the gene encoding the rapid component of the delayed ...
T. Hoorntje +7 more
openaire +3 more sources
Prediction of hERG inhibition of drug discovery compounds using biomimetic HPLC measurements
ADMET and DMPK, 2021 The major causes of failure of drug discovery compounds in clinics are the lack of efficacy and toxicity. To reduce late-stage failures in the drug discovery process, it is essential to estimate early the probability of adverse effects and potential ...
Chrysanthos Stergiopoulos +2 more
semanticscholar +1 more source
hERG Function in Light of Structure [PDF]
Biophysical Journal, 2020 The human ether-a-go-go-related gene1 (hERG) ion channel has been the subject of fascination since it was identified as a target of long QT syndrome more than 20 years ago. In this Biophysical Perspective, we look at what makes hERG intriguing and vexingly unique. By probing recent high-resolution structures in the context of functional and biochemical
João H. Morais-Cabral +2 more
openaire +3 more sources
Structural modeling of the hERG potassium channel and associated drug interactions
bioRxiv, 2021 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. Gating of hERG channel is characterized by
J. Malý +7 more
semanticscholar +1 more source
Journal of Cardiovascular Electrophysiology, 2016 miRNAs Regulate hERGBackgroundThe human ether‐a‐go‐go‐related gene (hERG) is the major molecular component of the rapidly activating delayed rectifier K+ current (Ikr). Impairment of hERG function is believed to be a mechanism causing long‐QT syndromes (LQTS). Growing evidences have shown that microRNAs (miRNAs) are involved in functional modulation of
Xiaoyan Huang +8 more
openaire +3 more sources
Journal of Cellular and Molecular Medicine, 2021 Drug‐mediated or medical condition‐mediated disruption of hERG function accounts for the main cause of acquired long‐QT syndrome (acLQTs), which predisposes affected individuals to ventricular arrhythmias (VA) and sudden death.
G. Zhan +10 more
semanticscholar +1 more source
Modulation of hERG 1a Trafficking by hERG 1b Subunits in Heart [PDF]
Biophysical Journal, 2016 In human heart the rapid component of the delayed rectifier potassium current (IKr), is an important contributor to repolarization. IKr exists as heterotetrameric channel complexes composed of hERG 1a/1b subunits. hERG 1b is defined by a shorter and unique N-terminus that lacks the Per-Arnt-Sim or ether-a-go-go, domain with implications for its role in
R. Suzanne Zukin +6 more
openaire +2 more sources
Design, synthesis and antibacterial activity of minor groove binders: the role of non-cationic tail groups [PDF]
, 2012 he design and synthesis of a new class of minor groove binder (MGBs) in which, the cationic tail group has been replaced by a neutral, polar variant including cyanoguanidine, nitroalkene, and trifluoroacetamide groups.
Bourdin, Claire +9 more
core +1 more source