Study on the Structure Activity Relationships of NPTX-594, a Spider Toxin Belonging to the Type-B Acylpolyamine Structure

Autor: Wakamiya, Tateaki, Kinoshita, Tomohiko, Hattori, Yoshihide, Yamaguchi, Yoshihiro, Naoki, Hideo, Corzo, Gerardo, Nakajima, Terumi
Zdroj: Bulletin of the Chemical Society of Japan; February 2004, Vol. 77 Issue: 2 p331-340, 10p
Abstrakt: In order to elucidate the structure activity relationships of the spider toxin termed NPTX-594, eleven toxin analogs were designed and synthesized, and their paralytic activities against cricket were tested. As a result of the present study, it was clarified that the Lys residue binding to the 1-amino group of 4,8-diaza-1,12-dodecanediamine (Dada) in the molecule of NPTX-594 is not an essential requisite for toxicity, and can be replaced with neutral or basic amino acids without any considerable loss of the activity. However, the replacement of the Lys residue with acidic amino acid residues, such as Asp or Glu, resulted in an extreme loss of the biological activity.
Databáze: Supplemental Index