Interrogating Protein Phosphatases with Chemical Activity Probes.
Interrogating Protein Phosphatases with Chemical Activity Probes.
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DOI：
10.1002/chem.201705194
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发表时间：
2018-06-04
期刊：
影响因子：
--
通讯作者：
Stains CI
中科院分区：
文献类型：
--
作者：
Casey GR;Stains CI
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。这篇小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。蛋白磷酸酶逐渐被认为是正常和疾病生理学中的关键信号酶。酶活性的化学报告基因有望为这些重要信号酶的化学生物学提供深入的见解。蛋白磷酸酶和蛋白激酶的活性负责维持磷酸化蛋白质组。尽管蛋白激酶长期以来一直受到关注，但蛋白磷酸酶最近被认为是正常和疾病生理学中的重要信号酶。本小型综述旨在强调蛋白质磷酸酶化学活性探针开发的进展和机遇。
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. Protein phosphatases are becoming recognized as critical signaling enzymes in both normal and disease physiology. Chemical reporters of enzymatic activity are poised to provide insights into the chemical biology of these important signaling enzymes. The activities of protein phosphatases and protein kinases are responsible for maintaining the phosphoproteome. Although protein kinases have long enjoyed the spotlight, protein phosphatases have more recently been recognized as important signaling enzymes in both normal and disease physiology. This Minireview aims to highlight advances and opportunities for the development of chemical activity probes for protein phosphatases.
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影响因子：
7.3
作者：
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通讯作者：
Manning, Gerard
影响因子：
4
作者：
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通讯作者：
Stains, Cliff I.
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作者：
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通讯作者：
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2.9
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通讯作者：
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影响因子：
56.9
作者：
Elchebly, M;Payette, P;Kennedy, BP
通讯作者：
Kennedy, BP