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Paper | Special issue | Vol 79, No. 1, 2009, pp.925-933
Published online, 8th December, 2008
DOI: 10.3987/COM-08-S(D)67
A Synthetic Approach to Develop Peptide Inhibitors Selective for Brain-Type Sodium Channels on the Basis of Pompilidotoxin Structure

Sawana Yokote, Ritsuko Setoguchi, Eisuke Shimizu, Naoki Mishima, Kohichi Kawahara, Akihiko Kuniyasu, Tetsuya Shirasaki, Kazuo Takahama, Katsuhiro Konno, Nobufumi Kawai, Kaoru Yamaoka, Eiji Kinoshita, and Hitoshi Nakayama*

*Faculty of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-hon-machi, Kumamoto 862-0973, Japan

Abstract

To develop inhibitors that are selective for brain-type sodium channels, several peptides were synthesized on the basis of pompilidotoxin structure. A peptide having N-terminal 7 amino acids and its homologs in which Phe7 is substituted into more hydrophobic amino acids, selectively inhibit sodium current of brain-type sodium channels.