Synthesis and characterization of amino acid deletion analogs of ¦Ê-hefutoxin 1, a scorpion toxin on potassium channels

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• 作者：Steve Peigneur ; Yoko Yamaguchi ; Hitomi Goto ; Kellathur N. Srinivasan ; Ponnampalam Gopalakrishnakone ; Jan Tytgat ; Kazuki Sato
• 关键词：¦Ê-Hefutoxin 1 ; Voltage-gated potassium channel ; Scorpion toxin ; Synthetic analogs ; Amino acid deletion ; Subtype selectivity
• 刊名：Toxicon
• 出版年：2013
• 出版时间：1 September, 2013
• 年：2013
• 卷：71
• 期：Complete
• 页码：25-30
• 全文大小：846 K

文摘

Nine analogs of scorpion toxin peptide ¦Ê-hefutoxin 1 were synthesized by stepwise deletion of its amino acid residues. Disulfide bond pairings of the synthetic analogs were confirmed by enzymatic digestion followed by MALDI-TOF-MS measurements. Functional characterization shows that analogs in which N-terminal residues were deleted retained biological activity, whereas deletion of middle part residues resulted in loss of activity. Furthermore, ¦Ê-hefutoxin 1 and analogs were subjected to a screening on voltage-gated potassium channels in order to determine their subtype selectivity. It is shown that ¦Ê-hefutoxin 1 is suitable as template for peptidomimetics in order to design small peptide-based therapeutic compounds.