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Mostrando 81 - 100 Resultados de 775 Para Buscar '"Hergé"', tiempo de consulta: 0.16s Limitar resultados
  1. 81
    “…A series of 172 molecular structures that block the hERG K(+) channel were used to develop a classification model where, initially, eight types of PaDEL fingerprints were used for k-nearest neighbor model development. …”
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    A k-nearest neighbor classification of hERG K(+) channel blockers
  2. 82
    Publicado 2016
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    Mechanism and pharmacological rescue of berberine-induced hERG channel deficiency [Corrigendum]
  3. 83
    “…Inhibition of hERG K(+) channels by structurally diverse drugs prolongs the ventricular action potential and increases the risk of torsade de pointes arrhythmias and sudden cardiac death. …”
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    Drug trapping in hERG K(+) channels: (not) a matter of drug size?
  4. 84
    “…The development of a novel comprehensive approach for the prediction of hERG activity is herein presented. Software Phase has been used to derive a 3D-QSAR model, employing as alignment rule a common pharmacophore built on a subset of 22 highly active compounds (threshold Ki: 50 nM) against hERG K(+) channel. …”
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    Computational Tool for Fast in silico Evaluation of hERG K(+) Channel Affinity
  5. 85
    “…The voltage-gated potassium channel that gives rise to I (Kr), K(v)11.1 (hERG), is uniquely susceptible to high-affinity block by a wide range of drug classes. …”
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    Probing the molecular basis of hERG drug block with unnatural amino acids
  6. 86
    “…Whole-cell patch-clamp measurements were made at 37 °C from hERG-expressing HEK293 cells. Docking analysis was conducted using a recent cryo-EM structure of hERG. …”
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    Potent hERG channel inhibition by sarizotan, an investigative treatment for Rett Syndrome
  7. 87
    “…As the first attempt, we in this investigation adopted CapsNets to develop classification models of hERG blockers/nonblockers; drugs with hERG blockade activity are thought to have a potential risk of cardiotoxicity. …”
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    Capsule Networks Showed Excellent Performance in the Classification of hERG Blockers/Nonblockers
  8. 88
    “…We previously reported that physiological concentrations of some estrogens partially suppress the hERG channel currents by interacting with the S6 residue F656 and increase the sensitivity of hERG blockade by E-4031. …”
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    The Effect of a Synthetic Estrogen, Ethinylestradiol, on the hERG Block by E-4031
  9. 89
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    What Is the Potential for Lumacaftor as a Chemical Chaperone in Promoting hERG Trafficking?
  10. 90
    “…Compounds with human ether-à-go-go related gene (hERG) blockade activity may cause severe cardiotoxicity. …”
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    Predicting hERG channel blockers with directed message passing neural networks
  11. 91
    “…[Image: see text] Drug-induced blockade of the human ether-à-go-go-related gene (hERG) channel is today considered the main cause of cardiotoxicity in postmarketing surveillance. …”
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    Structure-Based Prediction of hERG-Related Cardiotoxicity: A Benchmark Study
  12. 92
    “…The results indicate that an anti-hERG siRNA requires a long exposure time (48 h) in the hERG assay to produce a maximal reduction in hERG current; short exposures (20 min–8 h) had no effect. …”
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    Time Is a Critical Factor When Evaluating Oligonucleotide Therapeutics in hERG Assays
  13. 93
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    Predicting hERG repolarization power at 37°C from recordings at room temperature
  14. 94
    “…This study utilized a methanesulphonate-lacking E-4031 analogue, “E-4031-17”, to evaluate the role of the methanesulphonamide group in E-4031 inhibition of hERG. Whole-cell patch-clamp measurements of the hERG current (I(hERG)) were made at physiological temperature from HEK 293 cells expressing wild-type (WT) and mutant hERG constructs. …”
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    Inhibition of the hERG Potassium Channel by a Methanesulphonate-Free E-4031 Analogue
  15. 95
    “…The functional consequence of AKAP-IS is a reversal of cAMP-dependent regulation of HERG channel activity. In further support of AKAP-mediated targeting of kinase to HERG, PKA activity was coprecipitated from HERG expressed in HEK cells. …”
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    A-Kinase Anchoring Protein Targeting of Protein Kinase A and Regulation of HERG Channels
  16. 96
    “…A Per-Arnt-Sim (PAS) domain in the cytoplasmic N-terminal region of hERG regulates slow deactivation by making a direct interaction with another part of the hERG channel. …”
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    hERG potassium channel gating is mediated by N- and C-terminal region interactions
  17. 97
    por Bilet, Arne, Bauer, Christiane K.
    Publicado 2012
    “…NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents. …”
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    Effects of the Small Molecule HERG Activator NS1643 on Kv11.3 Channels
  18. 98
    por Glinka, Anna, Polak, Sebastian
    Publicado 2012
    “…Mean APD90 for the 80 individuals with the WT version of the hERG gene and for the 20 K897T homo- and heterozygotes is respectively 349.08 ms (SD = 21.09 ms) and 363.95ms (SD = 20.41 ms). …”
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    Wild type and K897T polymorphisms of the hERG gene: modeling the APD in Caucasians
  19. 99
    “…Human ether-à-go-go–related gene (hERG, Kv11.1) potassium channels have unusually slow activation and deactivation kinetics. …”
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    Functional interactions of voltage sensor charges with an S2 hydrophobic plug in hERG channels
  20. 100
    “…HERG has unusual biophysical properties distinct from those of other K(+) channels. …”
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    New Aspects of HERG K(+) Channel Function Depending upon Cardiac Spatial Heterogeneity
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