基于结构的硫氟交换（SuFEx）化学探针的设计与分析
Structure-based design and analysis of SuFEx chemical probes.
作者信息
Jones Lyn H, Kelly Jeffery W
机构信息
Center for Protein Degradation , Dana-Farber Cancer Institute , 360 Longwood Avenue , Boston , MA 02215 , USA . Email:
Departments of Chemistry and Molecular Medicine , The Scripps Research Institute , La Jolla , CA , USA.
出版信息
RSC Med Chem. 2020 Jan 6;11(1):10-17. doi: 10.1039/c9md00542k. eCollection 2020 Jan 1.
Abstract
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.
摘要
六价硫氟化物交换（SuFEx）化学的敏锐反应性，使得通过包含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异性标记。来自蛋白质-探针结构和蛋白质组图谱实验的新信息，有助于推动我们对决定可靶向氨基酸残基反应性的蛋白质微环境的理解。本综述探讨了这些新发现，这些发现应会影响未来SuFEx探针的合理设计，以用于化学生物学和药物发现中的多种应用。
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