Study on the Structure Activity Relationships of NPTX-594, a Spider Toxin Belonging to the Type-B Acylpolyamine Structure
Por:
Wakamiya T., Kinoshita T., Hattori Y., Yamaguchi Y., Naoki H., Corzo G., Nakajimal T.
Publicada:
1 ene 2004
Resumen:
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.
Filiaciones:
Wakamiya T.:
Faculty of Science and Technology, Kinki University, Higashi-osaka, Osaka 577-8502, Japan
Kinoshita T.:
Faculty of Science and Technology, Kinki University, Higashi-osaka, Osaka 577-8502, Japan
Hattori Y.:
Faculty of Science and Technology, Kinki University, Higashi-osaka, Osaka 577-8502, Japan
Yamaguchi Y.:
Faculty of Science and Technology, Kinki University, Higashi-osaka, Osaka 577-8502, Japan
Naoki H.:
Suntory Inst. for Bioorg. Research, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan
Corzo G.:
Suntory Inst. for Bioorg. Research, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan
Nakajimal T.:
Suntory Inst. for Bioorg. Research, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan
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