Interrogating Protein Phosphatases with Chemical Activity Probes,Chemistry - A European Journal

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Interrogating Protein Phosphatases with Chemical Activity Probes
Chemistry - A European Journal ( IF 3.9 ) Pub Date : 2018-03-08 , DOI: 10.1002/chem.201705194
Garrett R Casey ₁ , Cliff I Stains ₁

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Protein phosphatases, while long overlooked, have recently become appreciated as drivers of both normal‐ and disease‐associated signaling events. As a result, the spotlight is now turning torwards this enzyme family and efforts geared towards the development of modern chemical tools for studying these enzymes are well underway. This Minireview focuses on the evolution of chemical activity probes, both optical and covalent, for the study of protein phosphatases. Small‐molecule probes, global monitoring of phosphatase activity through the use of covalent modifiers, and targeted fluorescence‐based activity probes are discussed. We conclude with an overview of open questions in the field and highlight the potential impact of chemical tools for studying protein phosphatases.

中文翻译：

用化学活性探针研究蛋白磷酸酶

蛋白磷酸酶虽然长期被忽视，但最近作为正常和疾病相关信号事件的驱动因素而受到重视。因此，现在人们的注意力转向了这个酶家族，并且开发用于研究这些酶的现代化学工具的努力正在顺利进行。本小型综述重点关注用于蛋白质磷酸酶研究的光学和共价化学活性探针的演变。讨论了小分子探针、通过使用共价修饰剂对磷酸酶活性进行全局监测以及基于荧光的靶向活性探针。最后，我们概述了该领域的悬而未决的问题，并强调了化学工具对研究蛋白质磷酸酶的潜在影响。

更新日期：2018-03-08

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