Structural Determinants of HERG Channel Block by Clofilium and Ibutilide

@article{Perry2004StructuralDO,
  title={Structural Determinants of HERG Channel Block by Clofilium and Ibutilide},
  author={Matthew D Perry and Marcel J. de Groot and Ray M Helliwell and Derek J. Leishman and Martin Tristani-Firouzi and Michael C Sanguinetti and John S. Mitcheson},
  journal={Molecular Pharmacology},
  year={2004},
  volume={66},
  pages={240 - 249}
}
Block of human ether-a-go-go related gene (HERG) K+ channels by a variety of medications has been linked to acquired long QT syndrome, a disorder of cardiac repolarization that predisposes to lethal arrhythmias. The drug-binding site is composed of residues that face into the central cavity of the channel. Two aromatic residues located on the S6 domain (Tyr652 and Phe656) are particularly important structural determinants of drug block. The role of pore helix residues (Thr623, Ser624, Val625… 

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