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Efficient Generation of Hydrazides in Proteins by RadA Split Intein
ChemBioChem ( IF 3.2 ) Pub Date : 2020-01-21 , DOI: 10.1002/cbic.202000013
Jun Liu 1, 2 , Oshini Ekanayake 1 , Dominic Santoleri 1, 3 , Kelsi Walker 1 , Sharon Rozovsky 1
Affiliation  

Hydrazides at proteins’ C termini are much desired because of their straightforward use for bioconjugations and chemical modifications. However, traditional preparation methods often lack the necessary biocompatibility. In their full paper, J. Liu, S. Rozovsky, et al. show that combining thiols and hydrazine under mild conditions results in the high‐yield generation of such C‐terminal hydrazides. The addition of thiols not only accelerates the formation of the transient thioester intermediate, and the subsequent hydrazinolysis that promotes hydrazide formation at proteins’ C terminus, but also alleviates the problem of destructive protein aggregation. Employing split inteins to trigger hydrazinolysis provides an additional level of control of this now biocompatible generation method.
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中文翻译:

RadA Split Intein可有效产生蛋白质中的酰肼

非常需要蛋白质C末端的酰肼,因为它们可直接用于生物缀合和化学修饰。但是,传统的制备方法通常缺乏必要的生物相容性。J. Liu,S。Rozovsky等在其完整论文中。结果表明,在温和的条件下结合硫醇和肼会导致高产C端酰肼的产生。硫醇的添加不仅加速了瞬态硫酯中间体的形成,而且促进了蛋白C末端酰肼形成的随后肼解反应,还减轻了破坏性蛋白聚集的问题。利用分裂的内含蛋白引发肼解为这种现在生物相容的生成方法提供了更高水平的控制。
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更新日期:2020-01-22
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