One-pot hydrazide-based native chemical ligation for efficient chemical synthesis and structure determination of toxin Mambalgin-1.

One-pot hydrazide-based native chemical ligation for efficient chemical synthesis and structure determination of toxin Mambalgin-1.
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DOI:
10.1039/c4cc00779d
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发表时间:
2014-05
影响因子:
4.9
通讯作者:
M. Pan;Yao He;Ming Wen;Fangming Wu;Demeng Sun;Sijian Li;Long-hua Zhang;Yiming Li;C. Tian
M. Pan;Yao He;Ming Wen;Fangming Wu;Demeng Sun;Sijian Li;Long-hua Zhang;Yiming Li;C. Tian
中科院分区:
化学2区
文献类型:
--
作者:
M. Pan;Yao He;Ming Wen;Fangming Wu;Demeng Sun;Sijian Li;Long-hua Zhang;Yiming Li;C. Tian

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使用叠氮开关策略与基于酰肼的天然化学连接相结合,实现了蛇毒毒素 Mambalgin-1 的高效一锅化学合成。合成的 Mambalgin-1 在体外连续折叠后表现出明确的结构。核磁共振波谱揭示了三指毒素家族结构,合成毒素抑制人类酸敏感离子通道1a。
An efficient one-pot chemical synthesis of snake venom toxin Mambalgin-1 was achieved using an azide-switch strategy combined with hydrazide-based native chemical ligation. Synthetic Mambalgin-1 exhibited a well-defined structure after sequential folding in vitro. NMR spectroscopy revealed a three-finger toxin family structure, and the synthetic toxin inhibited human acid-sensing ion channel 1a.