Structure-activity relationships of sarafotoxins: chemical syntheses of chimera peptides of sarafotoxins S6b and S6c

Chikahisa Takasaki, Saburo Aimoto, Kazuhiro Kitazumi, Kenji Tasaka, Toshiharu Shiba, Katsuyuki Nishiki, Yasuo Furukawa, Ryoichi Takayanagi, Keizo Ohnaka, Hajime Nawata

研究成果: Contribution to journalArticle査読

14 被引用数 (Scopus)

抄録

The three chimera peptides of sarafotoxins S6b (SRTb) and S6c (SRTc), [Thr2SRTb, [Asn4]SRTb and [Glu9]SRTb, were synthesized chemically. From the comparisons of lethality, vasoconstrictor activity and receptor binding activity of SRTb, SRTa ([Asn13]SRTb), SRTc ([Thr2Asn4Glu9Asn13]SRTb), [Thr2SRTb, [Asn4]SRTb and [Glu9SRTb, it appears that the Lys9 to Glu9 substitution greatly diminishes these activities while the Lys4 to Asn4 substitution does not affect them, and the Ser2 to Thr2 substitution or the Tyr13 to Asn13 substitution slightly diminishes these activities. There results suggest that the very low activities of SRTc are caused mainly by the Lys9 to Glu9 substitution, but not by the Ser2 to Thr2 substitution, which was suggested to be responsible for the weak bioactivities of SRTd ([Thr2,Ile19]SRTb).

本文言語英語
ページ(範囲)165-169
ページ数5
ジャーナルEuropean Journal of Pharmacology
198
2-3
DOI
出版ステータス出版済み - 6 6 1991

All Science Journal Classification (ASJC) codes

  • 薬理学

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