Selective Metal-Site-Guided Arylation of Proteins

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• 作者：Jens Willwacher ; Ritu Raj ; Shabaz Mohammed ; Benjamin G. Davis
• 刊名：Journal of the American Chemical Society
• 出版年：2016
• 出版时间：July 20, 2016
• 年：2016
• 卷：138
• 期：28
• 页码：8678-8681
• 全文大小：412K
• 年卷期：0
• ISSN：1520-5126

文摘

We describe palladium-mediated S-arylation that exploits natural metal-binding motifs to ensure high site selectivity for a proximal reactive residue. This allows the chemical identification not only of proteins that bind metals but also the environment of the metal-binding site itself through proteomic analysis of arylation sites. The transformation is easy to perform under standard conditions, does not require the isolation of a reactive Ar–Pd complex, is broad in scope, and is applicable in cell lysates as well as to covalent inhibition/modulation of metal-dependent enzymatic activity.