Drug block of the hERG potassium channel: insight from modeling.

@article{Stansfeld2007DrugBO,
  title={Drug block of the hERG potassium channel: insight from modeling.},
  author={Phillip J. Stansfeld and Peter Gedeck and Martin Gosling and Brian Cox and John S. Mitcheson and Michael J. Sutcliffe},
  journal={Proteins},
  year={2007},
  volume={68 2},
  pages={568-80}
}
Many commonly used, structurally diverse, drugs block the human ether-a-go-go-related gene (hERG) K(+) channel to cause acquired long QT syndrome, which can lead to sudden death via lethal cardiac arrhythmias. This undesirable side effect is a major hurdle in the development of safe drugs. To gain insight about the structure of hERG and the nature of drug block we have produced structural models of the channel pore domain, into each of which we have docked a set of 20 hERG blockers. In the… CONTINUE READING
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