We have developed a novel bioorthogonal reaction that can selectively displace fluorine substitutions alpha to amide bonds. This fluorine-thiol displacement reaction (FTDR) allows for fluorinated cofactors or precursors to be utilized as chemical reporters, hijacking acetyltransferase-mediated acetylation both in vitro and in live cells, which cannot be achieved with azide- or alkyne-based chemical reporters. The fluoroacetamide labels can be further converted to biotin or fluorophore tags using FTDR, enabling the general detection and imaging of acetyl substrates. This strategy may lead to a steric-free labeling platform for substrate proteins, expanding our chemical toolbox for functional annotation of post-translational modifications in a systematic manner.

中文翻译：

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基于氟硫醇置换反应的乙酰化底物的无立体生物正交标记

我们开发了一种新的生物正交反应，可以选择性地将氟取代 α 替换为酰胺键。这种氟-硫醇置换反应 (FTDR) 允许将氟化辅因子或前体用作化学报告分子，在体外和活细胞中劫持乙酰转移酶介导的乙酰化，这是使用叠氮化物或炔烃基化学报告分子无法实现的。使用 FTDR 可以将氟乙酰胺标记进一步转化为生物素或荧光团标签，从而实现对乙酰基底物的一般检测和成像。这种策略可能会导致底物蛋白的无空间标记平台，扩展我们的化学工具箱，以系统的方式对翻译后修饰进行功能注释。