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Seeing Is Believing: Peptide-Based Fluorescent Sensors of Protein Tyrosine Kinase Activity

机译:眼见为实:蛋白酪氨酸激酶活性的基于肽的荧光传感器

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摘要

Protein tyrosine kinases are key biochemical effectors of the signaling pathways that drive both normal and aberrant cell behavior. The ability to visualize the activity of tyrosine kinases in both a continuous and sensitive fashion will have a dramatic impact on the identification and characterization of inhibitors, the elucidation of the biochemical role of protein tyrosine kinases in various biological processes, and the imaging of kinase action in cells, tissues, and whole organisms. Several chemical strategies have recently been described that translate the formation of a phosphorylated tyrosine residue into a fluorescent readout. The challenges associated with the design of protein tyrosine kinase sensors, as well as the scope and limitations of the currently available sensors, are described.
机译:蛋白质酪氨酸激酶是驱动正常和异常细胞行为的信号传导途径的关键生化效应子。以连续和敏感方式可视化酪氨酸激酶活性的能力将对抑制剂的鉴定和表征,蛋白质酪氨酸激酶在各种生物过程中的生化作用的阐明以及激酶作用的成像产生重大影响在细胞,组织和整个生物体内。最近已经描述了几种化学策略,其将磷酸化酪氨酸残基的形成转化为荧光读数。描述了与蛋白质酪氨酸激酶传感器设计有关的挑战,以及当前可用传感器的范围和局限性。

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