Revealing the structural basis of action of hERG potassium channel activators and blockers.

@article{Perry2010RevealingTS,
  title={Revealing the structural basis of action of hERG potassium channel activators and blockers.},
  author={Matthew Perry and Michael C Sanguinetti and John S. Mitcheson},
  journal={The Journal of physiology},
  year={2010},
  volume={588 Pt 17},
  pages={3157-67}
}
Human ether-á-go-go related gene (hERG) potassium (K(+)) channels play a critical role in cardiac action potential repolarization. This is due, in large part, to the unique gating properties of these channels, which are characterized by relatively slow activation and an unusually fast and voltage-dependent inactivation. A large number of structurally diverse compounds bind to hERG and carry an unacceptably high risk of causing arrhythmias. On the other hand, drugs that increase hERG current may… CONTINUE READING

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