Structure-based design and analysis of SuFEx chemical probes,RSC Medicinal Chemistry

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Structure-based design and analysis of SuFEx chemical probes
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020/01/06 , DOI: 10.1039/c9md00542k
Lyn H. Jones _{1,

2,

3,

4} , Jeffery W. Kelly _{4,

5,

6,

7}

Affiliation

The discerning reactivity of sulfur(VI)-fluoride exchange (SuFEx) chemistry has enabled the context-specific labeling of protein binding sites by chemical probes that incorporate these versatile warheads. Emerging information from protein-probe structures and proteomic mapping experiments is helping advance our understanding of the protein microenvironment that dictates the reactivity of targetable amino acid residues. This review explores these new findings that should influence the future rational design of SuFEx probes for a multitude of applications in chemical biology and drug discovery.

中文翻译：

SuFEx化学探针的基于结构的设计和分析

硫（VI）-氟化物交换（SuFEx）化学的敏锐反应性使结合了这些多功能弹头的化学探针能够对蛋白质结合位点进行上下文特定的标记。来自蛋白质探针结构和蛋白质组图谱实验的新兴信息正在帮助增进我们对蛋白质微环境的了解，该环境决定了可靶向氨基酸残基的反应性。这篇综述探索了这些新发现，这些发现将影响SuFEx探针在化学生物学和药物发现中的大量应用的未来合理设计。

更新日期：2020-02-13

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