The hERG potassium channel and drug trapping: Insight from docking studies with propafenone derivatives

  • Thai K
  • Windisch A
  • Stork D
 et al. 
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Abstract

The inner cavity of the hERG potassium ion channel can accommodate large, structurally diverse compounds that can be trapped in the channel by closure of the activation gate. A small set of propafenone derivatives was synthesized, and both use-dependency and recovery from block were tested in order to gain insight into the behavior of these compounds with respect to trapping and non-trapping. Ligand-protein docking into homology models of the closed and open state of the hERG channel provides the first evidence for the molecular basis of drug trapping.

Author-supplied keywords

  • Docking
  • Drug trapping
  • Ion channels
  • Propafenone
  • hERG

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