Combined Receptor and Ligand-Based Approach to the Universal Pharmacophore Model Development for Studies of Drug Blockade to the hERG1 Pore Domain

@article{Durdagi2011CombinedRA,
  title={Combined Receptor and Ligand-Based Approach to the Universal Pharmacophore Model Development for Studies of Drug Blockade to the hERG1 Pore Domain},
  author={Serdar Durdagi and Henry J. Duff and Sergei Yu Noskov},
  journal={Journal of chemical information and modeling},
  year={2011},
  volume={51 2},
  pages={463-74}
}
Long QT syndrome, LQTS, results in serious cardiovascular disorders, such as tachyarrhythmia and sudden cardiac death. A promiscuous binding of different drugs to the intracavitary binding site in the pore domain (PD) of human ether-a-go-go related gene (hERG) channels leads to a similar dysfunction, known as a drug-induced LQTS. Therefore, an assessment of the blocking ability for potent drugs is of great pragmatic value for molecular pharmacology and medicinal chemistry of hERGs. Thus, we… CONTINUE READING

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