A selective blocker of Kv1.2 and Kv1.3 potassium channels from the venom of the scorpion Centruroides suffusus suffusus

Gerardo Corzo, Ferenc Papp, Zoltan Varga, Omar Barraza, Pavel G. Espino-Solis, Ricardo C. Rodríguez de la Vega, Rezso Gaspar, Gyorgy Panyi, Lourival D. Possani

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Abstract

A novel potassium channel blocker peptide was purified from the venom of the scorpion Centruroides suffusus suffusus by high-performance liquid chromatography and its amino acid sequence was completed by Edman degradation and mass spectrometry analysis. It contains 38 amino acid residues with a molecular weight of 4000.3 Da, tightly folded by three disulfide bridges. This peptide, named Css20, was shown to block preferentially the currents of the voltage-dependent K+-channels Kv1.2 and Kv1.3. It did not affect several other ion channels tested at 10 nM concentration. Concentration-response curves of Css20 yielded an IC50 of 1.3 and 7.2 nM for Kv1.2- and Kv1.3-channels, respectively. Interestingly, despite the similar affinities for the two channels the association and dissociation rates of the toxin were much slower for Kv1.2, implying that different interactions may be involved in binding to the two channel types; an implication further supported by in silico docking analyses. Based on the primary structure of Css20, the systematic nomenclature proposed for this toxin is α-KTx 2.13.

Original languageEnglish
Pages (from-to)1142-1154
Number of pages13
JournalBiochemical Pharmacology
Volume76
Issue number9
DOIs
Publication statusPublished - Oct 30 2008

Keywords

  • Centruroides suffusus suffusus
  • K ion-channel
  • Lymphocytes
  • Molecular modeling
  • Scorpion toxin

ASJC Scopus subject areas

  • Biochemistry
  • Pharmacology

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    Corzo, G., Papp, F., Varga, Z., Barraza, O., Espino-Solis, P. G., Rodríguez de la Vega, R. C., Gaspar, R., Panyi, G., & Possani, L. D. (2008). A selective blocker of Kv1.2 and Kv1.3 potassium channels from the venom of the scorpion Centruroides suffusus suffusus. Biochemical Pharmacology, 76(9), 1142-1154. https://doi.org/10.1016/j.bcp.2008.08.018