Molecular Determinants for Activation of Human Ether-à-go-go-related Gene 1 Potassium Channels by 3-Nitro-N-(4-phenoxyphenyl) Benzamide

@article{Garg2011MolecularDF,
  title={Molecular Determinants for Activation of Human Ether-{\`a}-go-go-related Gene 1 Potassium Channels by 3-Nitro-N-(4-phenoxyphenyl) Benzamide},
  author={V. Garg and A. Stary-Weinzinger and F. Sachse and M. Sanguinetti},
  journal={Molecular Pharmacology},
  year={2011},
  volume={80},
  pages={630 - 637}
}
Human ether-à-go-go-related gene 1 (hERG1) channels mediate repolarization of cardiac action potentials. Inherited long QT syndrome (LQTS) caused by loss-of-function mutations, or unintended blockade of hERG1 channels by many drugs, can lead to severe arrhythmia and sudden death. Drugs that activate hERG1 are a novel pharmacological approach to treat LQTS. 3-Nitro-n-(4-phenoxyphenyl) benzamide [ICA-105574 (ICA)] has been discovered to activate hERG1 by strong attenuation of pore-type… Expand
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References

SHOWING 1-10 OF 55 REFERENCES
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator
Discovery of a Small Molecule Activator of the Human Ether-a-go-go-Related Gene (HERG) Cardiac K+ Channel
Mechanism of Action of a Novel Human ether-a-go-go-Related Gene Channel Activator
PD-118057 contacts the pore helix of hERG1 channels to attenuate inactivation and enhance K+ conductance
Molecular determinants of dofetilide block of HERG K+ channels.
Molecular determinants of drug binding and action on L-type calcium channels.
Predicting drug-hERG channel interactions that cause acquired long QT syndrome.
...
1
2
3
4
5
...