Comparison of different strategies towards the chemical synthesis of long-chain scorpion toxin AaH-II,Journal of Peptide Science

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Comparison of different strategies towards the chemical synthesis of long-chain scorpion toxin AaH-II
Journal of Peptide Science ( IF 1.8 ) Pub Date : 2021-08-31 , DOI: 10.1002/psc.3365
Yu-Lei Li _{1,

2} , Qian Qu _{1,

3} , Yun-Kun Qi ₂ , Lei Liu ₁ , Ke Wei Wang ₂ , Yani Liu ₂ , Ge-Min Fang ₃

Affiliation

Long-chain scorpion toxin AaH-II isolated from Androctonus australis Hector can selectively inhibit mammalian voltage-gated sodium ion channel Na_v1.7 responsible for pain sensation. Efficient chemical synthesis of AaH-II and its derivatives is beneficial to the study of the function and mechanism of Na_v1.7 and the development of potential peptide inhibitors. Herein, we compared three different strategies, namely, direct solid-phase peptide synthesis, hydrazide-based two-segment native chemical ligation, and hydrazide-based three-segment native chemical ligation for the synthesis of AaH-II. The hydrazide-based two-segment native chemical ligation affords the target toxin with the optimal efficiency, which provides a practically robust procedure for the preparation of tool molecules derived from AaH-II to study the biological functions and modulation of Na_v1.7. Our work highlights the importance of selecting suitable segment condensation approach in the chemical synthesis of protein toxins.

中文翻译：

长链蝎毒AaH-II化学合成不同策略的比较

从Androctonus australis Hector中分离出的长链蝎毒素 AaH-II可以选择性地抑制负责疼痛感的哺乳动物电压门控钠离子通道 Na _{v 1.7。}AaH-II及其衍生物的高效化学合成有利于Na _{v功能和机制的研究}1.7和潜在肽抑制剂的开发。在这里，我们比较了三种不同的策略，即直接固相肽合成、基于酰肼的两段天然化学连接和基于酰肼的三段天然化学连接用于合成 AaH-II。基于酰肼的两段天然化学连接提供了具有最佳效率的目标毒素，这为制备源自 AaH-II 的工具分子以研究 Na _v 1.7 的生物学功能和调节提供了一个实际稳健的程序。我们的工作强调了在蛋白质毒素的化学合成中选择合适的片段缩合方法的重要性。

更新日期：2021-08-31

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