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A SYNTHETIC APPROACH TO DEVELOP PEPTIDE INHIBITORS SELECTIVE FOR BRAIN-TYPE SODIUM CHANNELS ON THE BASIS OF POMPILIDOTOXIN STRUCTURE

  作者 YOKOTE SAWANA; SETOGUCHI RITSUKO; SHIMIZU EISUKE; MISHIMA NAOKI; KAWAHARA KOHICHI; KUNIYASU AKIHIKO; SHIRASAKI TETSUYA; TAKAHAMA KAZUO; KONNO KATSUHIRO; KAWAI NOBUFUMI; YAMAOKA KAORU; KINOSHITA EIJI; NAKAYAMA HITOSHI  
  选自 期刊  Heterocycles;  卷期  2009年79-1;  页码  925-933  
  关联知识点  
 

[摘要]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 Phe(7) is substituted into more hydrophobic amino acids, selectively inhibit sodium current of brain-type sodium channels.

 
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