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Mostrando 121 - 140 Resultados de 775 Para Buscar '"Hergé"', tiempo de consulta: 0.20s Limitar resultados
  1. 121
    “…Clinically, drug-induced torsades de pointes (TdP) are rare events, whereas the reduction of the human ether-à-go-go-related gene (hERG) current is common. In this study, we aimed to explore the specific factors that contribute to the deterioration of hERG inhibition into malignant ventricular arrhythmias. …”
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    Vicious LQT induced by a combination of factors different from hERG inhibition
  2. 122
    “…hERG1 potassium channels are widely expressed in human cancers of different origins, where they affect several key aspects of cellular behaviour. …”
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    Prognostic role of hERG1 Potassium Channels in Neuroendocrine Tumours of the Ileum and Pancreas
  3. 123
    “…The hERG channel is one of the essential ion channels composing the cardiac action potential and the toxicity assay for new drug. …”
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    Improving the hERG model fitting using a deep learning-based method
  4. 124
    “…Our study demonstrates utilization of traditional machine learning techniques such as random forest (RF), support-vector machine (SVM), extreme gradient boosting (XGBoost), deep neural network (DNN) as well as advanced deep learning techniques like gated recurrent unit-based DNN (GRU-DNN) and graph neural network (GNN), towards predicting human ether-á-go-go related gene (hERG) derived toxicity. Using the largest hERG dataset derived to date, we have utilized 203,853 and 87,366 compounds for training and testing the models, respectively. …”
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    hERG-toxicity prediction using traditional machine learning and advanced deep learning techniques
  5. 125
    “…The transmembrane domains of HERG (S1–S3) contain six negative charges: three are conserved in all voltage-gated K channels (D456 and D466 in S2, D501 in S3) and three are unique to the EAG family (D411 in S1, D460 in S2, and D509 in S3). …”
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    Negative Charges in the Transmembrane Domains of the HERG K Channel Are Involved in the Activation- and Deactivation-gating Processes
  6. 126
    “…When the first 16 amino acids are deleted from the amino terminus of HERG, the deactivation rate is much faster (Wang, J., M.C. …”
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    Dynamic Control of Deactivation Gating by a Soluble Amino-Terminal Domain in HERG K(+) Channels
  7. 127
    “…A HEK293 cell stably expressing the HERG potassium channel was voltage clamped and exposed to hyperosmotic solutions for short periods of time (<1 s) by an ultrafast solution switching system (the osmotic pulse [quick jump-and-away] method). …”
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    Coupled K(+)–Water Flux through the HERG Potassium Channel Measured by an Osmotic Pulse Method
  8. 128
    “…The cytoplasmic N–terminal domain of the human ether–a–go–go related gene (hERG) K(+) channel is critical for the slow deactivation kinetics of the channel. …”
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    The N–Terminal Tail of hERG Contains an Amphipathic α–Helix That Regulates Channel Deactivation
  9. 129
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    Winnow based identification of potent hERG inhibitors in silico: comparative assessment on different datasets
  10. 130
    “…These factors combine to create a resurgent hERG current, where the current amplitude is paradoxically larger with repolarization than with depolarization. …”
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    The eag domain regulates hERG channel inactivation gating via a direct interaction
  11. 131
    “…Analysis of transcriptional profiles generated in three independent cell lines revealed clusters enriched for hERG inhibitors annotated using a database of experimental measurements (hERGcentral) and clinical indications. …”
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    Integrated Analysis of Drug-Induced Gene Expression Profiles Predicts Novel hERG Inhibitors
  12. 132
    “…Many proteins, such as the hERG K(+) channel or the HIV-1 protease, have a high degree of rotational symmetry. …”
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    How to Solve the Problems of Docking into a Symmetric Binding Site: The Example of the hERG Channel
  13. 133
    “…Chimaera containing the S1–S6 transmembrane region of HERG showed functional and pharmacological properties similar to hERG and could be overexpressed and purified from Pichia. …”
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    A functional Kv1.2-hERG chimaeric channel expressed in Pichia pastoris
  14. 134
    “…Whole‐cell patch‐clamp measurements of hERG current were made at 37°C from hERG channels expressed in HEK293 cells. …”
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    Suppression of the hERG potassium channel response to premature stimulation by reduction in extracellular potassium concentration
  15. 135
    “…Our data show that mexiletine inhibits hERG in a time- and voltage-dependent manner, with an IC(50) of 3.7 ± 0.7 μmol/L. …”
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    Inhibition of hERG potassium channel by the antiarrhythmic agent mexiletine and its metabolite m-hydroxymexiletine
  16. 136
    “…This study aimed to elucidate molecular determinants of amiodarone binding to the hERG channel. Whole-cell patch-clamp recordings were made at 37 °C of ionic current (I(hERG)) carried by wild-type (WT) or mutant hERG channels expressed in HEK293 cells. …”
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    Interactions between amiodarone and the hERG potassium channel pore determined with mutagenesis and in silico docking
  17. 137
    “…A higher in vivo than in vitro potency for hERG‐mediated QTc prolongation has been suggested. …”
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    Application of a systems pharmacology model for translational prediction of hERG‐mediated QTc prolongation
  18. 138
    “…BACKGROUND: Pilsicainide, classified as a relatively selective Na(+) channel blocker, also has an inhibitory action on the rapidly-activating delayed-rectifier K(+) current (I(Kr)) through human ether-a-go-go-related gene (hERG) channels. We studied the effects of chronic exposure to pilsicainide on the expression of wild-type (WT) hERG proteins and WT-hERG channel currents, as well as on the expression of mutant hERG proteins, in a heterologous expression system. …”
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    Molecular mechanisms underlying the pilsicainide-induced stabilization of hERG proteins in transfected mammalian cells
  19. 139
    “…One of the primary targets for therapeutic intervention has been the human ether a go-go (hERG) K(+) channel that, together with the KCNQ channel, controls the rate and efficiency of repolarization in human myocardial cells. …”
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    Age-dependent electrical and morphological remodeling of the Drosophila heart caused by hERG/seizure mutations
  20. 140
    “…The hERG (human ether-a-go-go-related gene) encoded potassium ion (K(+)) channel plays a major role in cardiac repolarization. …”
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    Experimentally Validated Pharmacoinformatics Approach to Predict hERG Inhibition Potential of New Chemical Entities
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