ArticleScientific reports2016
New potential binding determinant for hERG channel inhibitors.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.
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Who cites it
49 citing papers in PubMed.
- Article
- Cardiosim-Tox: an interpretable multitask deep learning QSAR platform with multimodal feature fusion for predicting hERG, Cav1.2, and Nav1.5 blockade risk and potency.Archives of toxicology · 2026Article
- Allosteric Mechanisms Underlying Long QT Syndrome Type 2 (LQT2)-Associated Mutations in hERG Channels.bioRxiv : the preprint server for biology · 2026Article
- Discovery of a novel broad-spectrum inhibitor against influenza virus A.Virology journal · 2025Article
- Article
- Harnessing AlphaFold to reveal hERG channel conformational state secrets.bioRxiv : the preprint server for biology · 2025Article
- Computational identification of potential natural terpenoid inhibitors of MDM2 for breast cancer therapy: molecular docking, molecular dynamics simulation, and ADMET analysis.Frontiers in chemistry · 2025Article
- Article
- Inhibition of the hERG Potassium Channel by a Methanesulphonate-Free E-4031 Analogue.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Calculations of the binding free energies of the ComprehensiveBiophysics and physicobiology · 2023Article
- Structural modeling of hERG channel-drug interactions using Rosetta.Frontiers in pharmacology · 2023Article
- Ensemble of structure and ligand-based classification models for hERG liability profiling.Frontiers in pharmacology · 2023Article
- The voltage-sensing domain of a hERG1 mutant is a cation-selective channel.Biophysical journal · 2022Article
- The hEag1 KInternational journal of molecular sciences · 2022Article
- hERG Blockade Prediction by Combining Site Identification by Ligand Competitive Saturation and Physicochemical Properties.Chemistry (Basel, Switzerland) · 2022Article
- Structural modeling of the hERG potassium channel and associated drug interactions.Frontiers in pharmacology · 2022Article
- Inhibition of the hERG potassium channel by phenanthrene: a polycyclic aromatic hydrocarbon pollutant.Cellular and molecular life sciences : CMLS · 2021Article
- Article
- Structure-Based Prediction of hERG-Related Cardiotoxicity: A Benchmark Study.Journal of chemical information and modeling · 2021Article
- Toward Reducing hERG Affinities for DAT Inhibitors with a Combined Machine Learning and Molecular Modeling Approach.Journal of chemical information and modeling · 2021Article
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Authors and funding
8 authors.
Funding
Abstract
Human ether-à-go-go related gene (hERG) 1 channels conduct the rapid delayed rectifier K(+) current (IKr) and are essential for the repolarization of the cardiac action potential. hERG1 inhibition by structurally diverse drugs may lead to life threatening arrhythmia. Putative binding determinants of hERG1 channel blockers include T623, S624 and V625 on the pore helix, and residues G648, Y652 and F656, located on segment S6. We and others have previously hypothesized that additional binding determinants may be located on helix S5, which is in close contact with the S6 segments. In order to test this hypothesis, we performed a detailed investigation combining ionic current measurements with two-microelectrode voltage clamp and molecular modeling techniques. We identified a novel aromatic high affinity binding determinant for blockers located in helix S5, F557, which is equally potent as Y652. Modeling supports a direct interaction with the outer pore helix.
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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.