Optimal Sox-based fluorescent chemosensor design for serine/threonine protein kinases
Optimal Sox-based fluorescent chemosensor design for serine/threonine protein kinases
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DOI：
10.1016/j.ab.2006.03.003
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发表时间：
2006-05-15
影响因子：
2.9
通讯作者：
Imperiali, Barbara
中科院分区：
文献类型：
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作者：
Shults, Melissa D.;Carrico-Moniz, Dora;Imperiali, Barbara
蛋白激酶活性的荧光化学传感器为研究这些酶的作用提供了连续的高通量传感格式，这些酶对于调节细胞功能至关重要。具体而言，使用非天然氨基酸，Sox，和生理Mg 2+水平的化学传感器报告磷酸化与戏剧性的荧光变化，是适合实时和高通量分析。在这篇文章中，我们报告了15个探针，共6个不同的丝氨酸/苏氨酸激酶与大的荧光增加和良好的反应性对目标激酶。详细分析了传感机理，确定了最佳传感基序。这些多功能和强大的传感器为研究人员提供了工具，研究目标激酶在信号转导中的作用，设计原则为未来任何丝氨酸/苏氨酸激酶的荧光化学传感器的产生提供了指导。(c)2006年爱思唯尔公司All rights reserved.
Fluorescent chemosensors of protein kinase activity provide a continuous, high-throughput sensing format for the study of the roles of these enzymes, which are crucial for regulating cellular function. Specifically, chemosensors using the nonnatural amino acid, Sox, and physiological Mg2+ levels report phosphorylation with dramatic fluorescence changes that are amenable to real-time and high-throughput analysis. In this article, we report 15 probes for a total of six distinct serine/threonine kinases with large fluorescence increases and good reactivity toward the target kinase. The sensing mechanism is detailed, and the optimal sensing motif is determined. These versatile and powerful sensors provide tools for researchers studying the roles of the targeted kinases in signal transduction, and the design principles provide guidelines for the generation Of future fluorescent chemosensors for any serine/threonine kinase. (c) 2006 Elsevier Inc. All rights reserved.