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Fluorogenic probes for imaging cellular phosphatase activity.
Current opinion in chemical biology Pub Date : 2020-05-26 , DOI: 10.1016/j.cbpa.2020.04.004
Brandon S McCullough 1 , Amy M Barrios 1
Affiliation  

The ability to visualize enzyme activity in a cell, tissue, or living organism can greatly enhance our understanding of the biological roles of that enzyme. While many aspects of cellular signaling are controlled by reversible protein phosphorylation, our understanding of the biological roles of the protein phosphatases involved is limited. Here, we provide an overview of progress toward the development of fluorescent probes that can be used to visualize the activity of protein phosphatases. Significant advances include the development of probes with visible and near-infrared (near-IR) excitation and emission profiles, which provides greater tissue and whole-animal imaging capabilities. In addition, the development of peptide-based probes has provided some selectivity for a phosphatase of interest. Key challenges involve the difficulty of achieving sufficient selectivity for an individual member of a phosphatase enzyme family and the necessity of fully validating the best probes before they can be adopted widely.

中文翻译:


用于成像细胞磷酸酶活性的荧光探针。



可视化细胞、组织或活体中酶活性的能力可以极大地增强我们对该酶的生物学作用的理解。虽然细胞信号传导的许多方面是由可逆的蛋白质磷酸化控制的,但我们对所涉及的蛋白质磷酸酶的生物学作用的理解是有限的。在这里,我们概述了可用于可视化蛋白磷酸酶活性的荧光探针的开发进展。重大进展包括开发具有可见光和近红外(near-IR)激发和发射轮廓的探针,这提供了更强的组织和整体动物成像能力。此外,基于肽的探针的开发为感兴趣的磷酸酶提供了一定的选择性。主要挑战包括难以对磷酸酶家族的单个成员实现足够的选择性,以及在广泛采用之前充分验证最佳探针的必要性。
更新日期:2020-05-26
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