Potassium channel block by a tripartite complex of two cationophilic ligands and a potassium ion.

@article{Zimin2010PotassiumCB,
  title={Potassium channel block by a tripartite complex of two cationophilic ligands and a potassium ion.},
  author={Pavel I Zimin and Bojan Garic and Silke B. Bodendiek and C{\'e}drick Mahieux and Heike Wulff and Boris S. Zhorov},
  journal={Molecular pharmacology},
  year={2010},
  volume={78 4},
  pages={588-99}
}
Voltage-gated potassium channels (Kv) are targets for drugs of large chemical diversity. Although hydrophobic cations block Kv channels with Hill coefficients of 1, uncharged electron-rich (cationophilic) molecules often display Hill coefficients of 2. The mechanism of the latter block is unknown. Using a combination of computational and experimental approaches, we mapped the receptor for the immunosuppressant PAP-1 (5-(4-phenoxybutoxy)psoralen), a high-affinity blocker of Kv1.3 channels in… CONTINUE READING

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