GlaxoSmithKline, Gunnels Wood Road, Stevenage, HertfordshireSG1 2NY, United Kingdom.
University of Strathclyde, 295 Cathedral Street, GlasgowG11XL, United Kingdom.
ACS Chem Biol. 2023 Feb 17;18(2):285-295. doi: 10.1021/acschembio.2c00633. Epub 2023 Jan 17.
Here, we report a comprehensive profiling of sulfur(VI) fluorides (S-Fs) as reactive groups for chemical biology applications. S-Fs are reactive functionalities that modify lysine, tyrosine, histidine, and serine sidechains. A panel of S-Fs were studied with respect to hydrolytic stability and reactivity with nucleophilic amino acid sidechains. The use of S-Fs to covalently modify carbonic anhydrase II (CAII) and a range of kinases was then investigated. Finally, the S-F panel was used in live cell chemoproteomic workflows, identifying novel protein targets based on the type of S-F used. This work highlights how S-F reactivity can be used as a tool to expand the liganded proteome.
在这里，我们全面描绘了硫（VI）氟化物（S-Fs）作为化学生物学应用的反应基团。S-Fs 是一种反应性官能团，可修饰赖氨酸、酪氨酸、组氨酸和丝氨酸侧链。我们研究了一组 S-Fs，以了解其水解稳定性和与亲核氨基酸侧链的反应性。然后，我们研究了 S-F 用于共价修饰碳酸酐酶 II（CAII）和一系列激酶的用途。最后，该 S-F 试剂组用于活细胞化学蛋白质组学工作流程，根据所使用的 S-F 的类型鉴定新的蛋白质靶标。这项工作强调了 S-F 的反应性如何可以用作扩展配体蛋白质组的工具。
