ArticleBritish journal of pharmacology2008
Drugs and trafficking of ion channels: a new pro-arrhythmic threat on the horizon?
Article in British journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 65 citations in OpenAlex.
- Ion channel traffic jams: the significance of trafficking deficiency in long QT syndrome.Cell discovery · 2025Review
- In silico analysis of the dynamic regulation of cardiac electrophysiology by KThe Journal of physiology · 2023Article
- Probucol-induced hERG Channel Reduction can be Rescued by Matrine and OxymatrineCurrent pharmaceutical design · 2020Article
- Drug-likeness of linear pentamidine analogues and their impact on the hERG KRSC advances · 2019Article
- Comprehensive review of cardiovascular toxicity of drugs and related agents.Medicinal research reviews · 2018Review
- Article
- The rescuable function and mechanism of resveratrol on As₂O₃-induced hERG K⁺ channel deficiency.Naunyn-Schmiedeberg's archives of pharmacology · 2014Article
- Improved functional expression of human cardiac kv1.5 channels and trafficking-defective mutants by low temperature treatment.PloS one · 2014Article
- Structure-activity relationships of pentamidine-affected ion channel trafficking and dofetilide mediated rescue.British journal of pharmacology · 2013Article
- Mechanisms of zolpidem-induced long QT syndrome: acute inhibition of recombinant hERG K(+) channels and action potential prolongation in human cardiomyocytes derived from induced pluripotent stem cells.British journal of pharmacology · 2013Article
- Inhibiting the clathrin-mediated endocytosis pathway rescues K(IR)2.1 downregulation by pentamidine.Pflugers Archiv : European journal of physiology · 2013Article
- Long-term treatment with ivabradine in post-myocardial infarcted rats counteracts f-channel overexpression.British journal of pharmacology · 2012Article
- Dynamic monitoring of beating periodicity of stem cell-derived cardiomyocytes as a predictive tool for preclinical safety assessment.British journal of pharmacology · 2012Article
- Molecular determinants of pentamidine-induced hERG trafficking inhibition.Molecular pharmacology · 2012Article
- hERG K+ channel-associated cardiac effects of the antidepressant drug desipramine.Naunyn-Schmiedeberg's archives of pharmacology · 2011Article
- Finding inward rectifier channel inhibitors: why and how?Frontiers in pharmacology · 2011Article
- Ion channel trafficking: a new therapeutic horizon for atrial fibrillation.Heart rhythm · 2010Review
- Forward trafficking of ion channels: what the clinician needs to know.Heart rhythm · 2010Review
- Rescue of mutated cardiac ion channels in inherited arrhythmia syndromes.Journal of cardiovascular pharmacology · 2010Review
- Multiple mechanisms of hERG liability: K+ current inhibition, disruption of protein trafficking, and apoptosis induced by amoxapine.Naunyn-Schmiedeberg's archives of pharmacology · 2010Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Tuning of functional expression levels of the ion channels that make up the cardiac action potential (AP) is crucial for preserving correct AP duration (APD) and QTc times. Many compounds inhibit human ether-à-go-go related gene (hERG)-mediated delayed rectifier currents and thus prolong cardiac repolarization that may cause life-threatening arrhythmias like Torsades de Pointes. An increasing number of drugs are found to inhibit hERG function by a dual mechanism of short-term channel block and long-term trafficking defects that operate over different time and concentration scales. In safety screens at present used by pharmaceutical companies, the short-term effect of channel block is covered. In contrast, specific screening for long-term trafficking defects is not common, with the consequent risk of drugs that disturb trafficking entering the market. Whether that poses another pro-arrhythmic threat for the patients treated has to be determined, but is not unlikely.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.